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Profile Name FGFR2 N550S
Gene Variant Detail

FGFR2 N550S (gain of function)

Relevant Treatment Approaches FGFR Inhibitor (Pan) FGFR2 Inhibitor

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 rearrange intrahepatic cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 44.4% (4/9) in patients harboring FGFR2 rearrangements (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778). detail...
FGFR2 rearrange cholangiocarcinoma sensitive FGFR2 Inhibitor Pemigatinib Guideline Actionable Pemazyre (pemigatinib) is included in guidelines as subsequent-line therapy for patients with cholangiocarcinoma harboring FGFR2 fusions or rearrangements (NCCN.org). detail...
FGFR2 rearrange cholangiocarcinoma sensitive FGFR2 Inhibitor Pemigatinib FDA approved - Has Companion Diagnostic Actionable In a Phase II (FIGHT-202) trial, Pemazyre (pemigatinib) treatment resulted in an objective response in 35.5% (38/107, 3 complete response, 35 partial response) of patients with advanced cholangiocarcinoma harboring FGFR2 fusions or rearrangements, with a disease control rate of 82% (88/107), median time-to-response of 2.7 months, and a median progression-free survival of 6.9 months (PMID: 32203698; NCT02924376). detail... 32203698 detail...
FGFR2 rearrange cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in partial response in 2 patients with cholangiocarcinoma harboring FGFR2 rearrangements (Annals of Oncology, Volume 29, Issue suppl_5). detail...
FGFR2 amp FGFR2 rearrange cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in partial response in a patient with cholangiocarcinoma harboring FGFR2 rearrangement and FGFR2 amplification (Annals of Oncology, Volume 29, Issue suppl_5). detail...
FGFR2 W290_I291delinsC Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) prevented oncogenic transformation of cells expressing FGFR2 W290_I291delinsC (PMID: 26048680). 26048680
FGFR2 W290_I291delinsC Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited downstream phosphorylation of Akt and Erk1/2 in cells expressing Fgfr2 W290_I291delinsC (PMID: 26048680). 26048680
FGFR2 - TTC28 cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Pdx Actionable In a preclinical study, Infigratinib (BGJ398) treatment inhibited tumor growth in a patient-derived xenograft (PDX) model of cholangiocarcinoma harboring FGFR2-TTC28 fusion (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). detail...
FGFR2 L618M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 L618M were sensitive to treatment with Iclusig (ponatinib) (PMID: 23908597). 23908597
FGFR2 L618M Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 L618M demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 L618M Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 L618M demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 - ZMYM4 FGFR2 N550H FGFR2 N550K FGFR2 V565F FGFR2 E566A FGFR2 K660M intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-ZMYM4 fusion with FGFR2 V565F, K660M E566A, N550H, and N550K mutations, responded to TAS-120 for 7.2 months before progressing due to an acquired FGFR2 V563L mutation, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR2 - ZMYM4 FGFR2 N550H FGFR2 N550K FGFR2 V565F FGFR2 E566A FGFR2 K660M intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, a patient with intrahepatic cholangiocarcinoma harboring an FGFR2-ZMYM4 fusion developed progressive disease after initial response to Infigratinib (BGJ398) for 5.6 months and FGFR2 V565F, K660M E566A, N550H, and N550K mutations were identified in the post-progression cell-free DNA (PMID: 31109923). 31109923
FGFR2 - INA FGFR2 V565L FGFR2 E566A intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-INA fusion with FGFR2 H683L, L618V, N550H, N550T, M538I mutations, responded to TAS-120 for 5.1 months before progressing due to acquired FGFR2 V565L and E566A mutations, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR2 fusion FGFR2 E566A intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 E566A were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 E566A intrahepatic cholangiocarcinoma decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 E566A had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 E566A intrahepatic cholangiocarcinoma decreased response FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 E566A had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 amp stomach carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified gastric carcinoma cell lines were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR2 amp breast cancer sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of breast cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). 27627808
FGFR2 amp ovarian cancer sensitive Aprutumab ixadotin Preclinical - Pdx Actionable In a preclinical study, Aprutumab ixadotin (BAY1187982) inhibited tumor growth in patient-derived xenograft models of FGFR2 amplified ovarian cancer (PMID: 27543601). 27543601
FGFR2 amp colon cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp colorectal cancer predicted - sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified colorectal cancer cells in culture (PMID: 29573334). 29573334
FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor AZD4547 Phase II Actionable In a Phase II clinical trial, treatment with AZD4547 resulted in a 33% (3/9) response rate in patients with FGFR2-amplified gastroesophageal cancer, and high-level amplification was associated with clinical response (PMID: 27179038). 27179038
FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited FGFR signaling, and decreased proliferation and induced cell-cycle arrest in gastric cancer cells with amplification and over expression of FGFR2 in culture (PMID: 22869148). 22869148
FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). 30045926
FGFR2 amp breast cancer sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in a stable disease with 19.4% reduction of tumor size and 41% decrease of DUSP6 score in a patient with lung squamous cell carcinoma harboring FGFR2 amplification (PMID: 30745300; NCT01948297). 30745300
FGFR2 amp breast cancer sensitive FGFR2 Inhibitor Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of breast cancer cell lines harboring FGFR2 amplification in culture (PMID: 25169980). 25169980
FGFR2 amp myxoid liposarcoma sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) increased apoptosis, and inhibited cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 amp colorectal cancer sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Balversa (erdafitinib) inhibited tumor growth in an FGFR2-amplified colorectal cancer cell line xenograft model (PMID: 28341788). 28341788
FGFR2 amp myxoid liposarcoma sensitive FGFR Inhibitor (Pan) Dovitinib + Trabectedin Preclinical Actionable In a preclinical study, Dovitinib (TKI258) and Yondelis (trabectedin) worked synergistically to increase apoptosis, inhibit cell proliferation and migration of myxoid liposarcoma cell lines harbors FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor E7090 Case Reports/Case Series Actionable In a Phase I trial, treatment with E7090 demonstrated safety and was well-tolerable in patients with advanced solid tumors, and led to a partial response including a 71% decrease in diameter of the target lesion in a patient with gastric cancer previously treated with three lines of chemotherapy and harboring FGFR2 amplification (PMID: 31797489; NCT02275910). 31797489
FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a gastric cancer cell line harboring FGFR2 amplification demonstrated decreased cell viability in culture and antitumor activity in xenograft models when treated with E7090 (PMID: 27535969). 27535969
FGFR2 amp colon cancer sensitive FGFR Inhibitor (Pan) Nintedanib Preclinical Actionable In a preclinical study, Ofev (nintedanib) inhibited growth of colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp stomach cancer predicted - sensitive PRN1109 Preclinical - Cell line xenograft Actionable In a preclinical study, PRN1109 treatment resulted in tumor regression in gastric cancer cell line xenograft models harboring FGFR2 amplification (Eu J Cancer 2014 Vol 50, Suppl 6:157). detail...
FGFR2 amp Advanced Solid Tumor unknown FGFR2 Inhibitor AZD4547 Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 2 of 3 of patients with advanced solid tumors harboring FGFR2 amplification, with a 6-month progression-free survival rate of 0% (PMID: 32463741; NCT02465060). 32463741
FGFR2 amp stomach cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). 30045926
FGFR2 amp stomach cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) inhibited proliferation of gastric cancer cell lines harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 amp myxoid liposarcoma sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) increased apoptosis, inhibited cell proliferation and migration of myxoid liposarcoma cell lines harbors FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 amp stomach cancer sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of FGFR2-amplified gastric cancer cells in culture, and inhibited tumor growth in FGFR2-amplified gastric cancer cell line xenograft models (PMID: 22238366). 22238366
FGFR2 amp cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a Phase II trial, Infigratinib (BGJ398) treatment demonstrated manageable toxicity, and resulted in a 27% tumor size reduction in a patient with advanced cholangiocarcinoma harboring FGFR2 amplification (PMID: 29182496; NCT02150967). 29182496
FGFR2 amp colon cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified colon cancer cells in culture (PMID: 27550940). 27550940
FGFR2 amp breast cancer predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment resulted in a partial response in a patients with breast cancer harboring FGFR2 amplification, with 37% tumor shrinkage (Annals of Oncology (2020) 31 (suppl_4): S475). detail...
FGFR2 amp stomach cancer sensitive FGFR Inhibitor (Pan) ODM-203 Preclinical - Cell line xenograft Actionable In a preclinical study, ODM-203 inhibited FGFR signaling and proliferation in a gastric cancer cell line with amplification of FGFR2, and inhibited tumor growth in xenograft models (PMID: 30301864). 30301864
FGFR2 amp estrogen-receptor negative breast cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of estrogen receptor (ER)-negative breast cancer cells with FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp colon cancer sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp endometrial cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified endometrial cancer cells in cell line xenograft models (PMID: 27550940). 27550940
FGFR2 amp breast cancer sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in ER-negative breast cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp stomach carcinoma sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell line xenograft Actionable In a preclinical study, PRN1371 inhibited proliferation of FGFR2 amplified gastric carcinoma cells in culture and tumor growth in cell line xenograft models (PMID: 28978721). 28978721
FGFR2 amp breast cancer predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a Phase I trial, a breast cancer patient harboring an FGFR2 amplification demonstrated stable disease when treated with Infigratinib (BGJ398) (PMID: 27870574). 27870574
FGFR2 amp stomach cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in gastric cancer cell lines harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp stomach carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified gastric carcinoma cell lines were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 amp colorectal adenocarcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified colorectal adenocarcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR2 amp myxoid liposarcoma sensitive PD173074 + Trabectedin Preclinical Actionable In a preclinical study, PD173034 and Yondelis (trabectedin) worked synergistically to increase apoptosis, inhibit cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 amp stomach cancer sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Balversa (erdafitinib) inhibited proliferation of a gastric cancer cell line with FGFR2 amplification in culture, and inhibited tumor growth in xenograft models (PMID: 28341788). 28341788
FGFR2 amp Advanced Solid Tumor predicted - sensitive FGFR2 Inhibitor Debio 1347 Phase I Actionable In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297). 30745300
FGFR2 amp stomach cancer no benefit MK2206 Preclinical - Cell culture Actionable In a preclinical study, a gastric cancer cell line harboring an FGFR2 amplification was not sensitive to MK2206 treatment in culture (PMID: 30045926). 30045926
FGFR2 amp stomach cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp stomach cancer resistant Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD-6244) did not inhibit growth of gastric cancer cells with FGFR2 amplification in culture (PMID: 19755509). 19755509
FGFR2 amp colon cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) reduced Myc expression, induced cell-cycle arrest, and inhibited growth of a colon cancer cell line with FGFR2 amplification in culture (PMID: 27401245). 27401245
FGFR2 amp breast cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Pdx & cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell growth of an FGFR2 amplified breast cancer cell line in culture and prevented tumor growth and induced tumor regression in FGFR2 amplified breast cancer patient derived xenograft (PDX) models (PMID: 23658459). 23658459
FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited proliferation of FGFR-amplified gastric cancer cells in culture and inhibited tumor growth in cell line xenograft models of gastric cancer harboring FGFR2 amplification (PMID: 25169980). 25169980
FGFR2 amp myxoid liposarcoma sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 increased apoptosis, inhibited cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 amp breast cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified breast cancer cells in culture (PMID: 27550940). 27550940
FGFR2 amp stomach cancer sensitive Regorafenib Preclinical - Cell line xenograft Actionable In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified gastric cancer cell lines in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 29573334). 29573334
FGFR2 amp stomach cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). 30045926
FGFR2 amp stomach cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, FGFR2-amplified gastric cancer cell lines demonstrated sensitivity to PD173074 in culture, with cell lines with high-level FGFR2 amplification displaying higher sensitivity compared to cell lines with low-level amplification (PMID: 27179038). 27179038
FGFR2 amp stomach cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited proliferation of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). 27627808
FGFR2 amp stomach cancer sensitive Cediranib Preclinical - Cell culture Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). 30045926
FGFR2 amp stomach cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp colorectal adenocarcinoma predicted - sensitive RO5126766 Preclinical - Cell culture Actionable In a preclinical study, RO5126766 inhibited proliferation of FGFR2 amplified colorectal adenocarcinoma cells in culture (PMID: 26438159). 26438159
FGFR2 amp colorectal adenocarcinoma decreased response RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified colorectal adenocarcinoma cells demonstrated decreased response to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 amp colon cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp gastric signet ring cell adenocarcinoma sensitive M-COPA Preclinical - Cell culture Actionable In a preclinical study, treatment with M-COPA resulted in decreased Fgfr2 cell surface expression and phosphorylation and reduced growth of an FGFR2-amplified signet cell gastric cancer cell line in culture (PMID: 27197184). 27197184
FGFR2 amp stomach cancer sensitive FGFR Inhibitor (Pan) FIIN-1 Preclinical Actionable In a preclinical study, FIIN-01 inhibited Fgfr2-dependent cell proliferation of gastric cancer cell lines harboring FGFR2 amplification (PMID: 20338520). 20338520
FGFR2 amp gastric adenocarcinoma no benefit FGFR2 Inhibitor AZD4547 Phase II Actionable In a Phase II trial (SHINE), AZD4547 treatment did not improve progression-free survival compared to Taxol (paclitaxel) (1.8 vs 3.5 months, p=0.9581) in advanced gastric adenocarcinoma patients with FGFR2 amplification (PMID: 29177434; NCT01457846). 29177434
FGFR2 amp uterine cancer predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in a stable disease with 3.9% change of tumor size and 60% decrease of DUSP6 score in a patient with uterine cancer harboring FGFR2 amplification (PMID: 30745300; NCT01948297). 30745300
FGFR2 amp colorectal cancer sensitive eFT226 Preclinical - Cell line xenograft Actionable In a preclinical study, eFT226 inhibited cell growth, and induced apoptosis in a FGFR2-amplified colorectal cancer cell line in culture, and inhibited tumor growth, and induced regression in a cell line xenograft model (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133). detail...
FGFR2 amp colon cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp stomach carcinoma sensitive FGFR2 Inhibitor Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited tumor growth in cell line xenograft models of FGFR2 amplified gastric carcinoma (PMID: 26438159). 26438159
FGFR2 amp stomach cancer predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment resulted in a partial response in 2 patients with gastric cancer harboring FGFR2 amplification, with 59% and 90% tumor shrinkage, respectively (Annals of Oncology (2020) 31 (suppl_4): S475). detail...
FGFR2 amp stomach cancer predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Phase I Actionable In a Phase I trial, Futibatinib (TAS-120) treatment resulted in clinical response in a gastric cancer patient harboring FGFR2 amplification (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). detail...
FGFR2 amp stomach cancer no benefit Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a gastric cancer cell line harboring an FGFR2 amplification was not sensitive to Pictilisib (GDC-0941) treatment in culture (PMID: 30045926). 30045926
FGFR2 amp Her2-receptor positive breast cancer sensitive FGFR Inhibitor (Pan) Dovitinib Phase I Actionable In a Phase I trial, Dovitinib (TKI258) displayed safety and preliminary efficacy resulting in tumor regression of 28.2% and 18.5% in two patients with FGFR2 amplified Erbb2 (Her2)-receptor positive breast cancer (PMID: 23658459). 23658459
FGFR2 amp colorectal cancer sensitive FGFR2 Inhibitor Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of colorectal cancer cell lines harboring FGFR2 amplification in culture (PMID: 25169980). 25169980
FGFR2 amp lung non-small cell carcinoma sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 67.5% tumor growth inhibition in patient-derived xenograft models of FGFR2-amplified non-small cell lung cancer (PMID: 28978721). 28978721
FGFR2 amp myxoid liposarcoma sensitive FGFR Inhibitor (Pan) Infigratinib + Trabectedin Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) and Yondelis (trabectedin) worked synergistically to increase apoptosis, inhibit cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). 26036639
FGFR2 fusion FGFR2 amp stomach cancer sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell line xenograft Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of gastric cancer cells harboring FGFR2 amplification and PDHX-FGFR2 fusion in culture, resulted in tumor regression in cell line xenograft models (PMID: 27627808). 27627808
FGFR2 fusion FGFR2 amp breast cancer sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in tumor growth inhibition in patient-derived xenograft models of FGFR2-amplified breast cancer harboring FGFR2-GAB2 fusion (AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1249). detail...
FGFR1 amp FGFR2 amp breast cancer sensitive FGFR2 Inhibitor E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line, harboring FGFR1 amplification and FGFR2 amplification, treated with E7090 demonstrated decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR2 amp FGFR2 over exp colon cancer sensitive FGFR Inhibitor (Pan) Rogaratinib Preclinical - Cell line xenograft Actionable In a preclinical study, a colon cancer cell line xenograft model with FGFR2 amplification and FGFR2 overexpression demonstrated antitumor efficacy when treated with Rogaratinib (BAY 1163877), with a partial response in one of eight at one dose and five of eight at a different dose (PMID: 30807645). 30807645
FGFR2 amp FGFR2 over exp stomach cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Pdx Actionable In a preclinical study, AZD4547 decreased Myc expression and inhibited tumor growth in patient-derived xenograft (PDX) models of gastric cancer with FGFR2 amplification and over expression (PMID: 27401245). 27401245
FGFR2 amp FGFR2 over exp stomach cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Pdx Actionable In a preclinical study, Infigratinib (BGJ398) decreased Myc expression and inhibited tumor growth in patient-derived xenograft (PDX) models of gastric cancer with FGFR2 amplification and over expression (PMID: 27401245). 27401245
ERBB2 amp FGFR2 amp esophagus adenocarcinoma sensitive FGFR2 Inhibitor AZD4547 + Lapatinib Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD-4547 and Tykerb (lapatinib) worked synergistically to inhibit growth of an esophageal adenocarcinoma cell line with ERBB2 (HER2) and FGFR2 amplification in culture (PMID: 27595477). 27595477
FGFR2 - COL14A1 FGFR2 amp colon cancer sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell line xenograft Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of colon cancer cells harboring FGFR2 amplification and FGFR2-COL14A1 fusion in culture and in cell line xenograft models (PMID: 27627808). 27627808
FGFR2 - COL14A1 FGFR2 amp colorectal adenocarcinoma sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of colorectal adenocarcinoma cells harboring FGFR2 amplification and FGFR2-COL14A1 fusion in culture (PMID: 28978721). 28978721
FGFR2 - GAB2 FGFR2 amp breast cancer sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 60.6% tumor growth inhibition in patient-derived xenograft models of breast cancer harboring FGFR2 amplification and FGFR2-GAB2 fusion (PMID: 28978721). 28978721
FGFR2 amp FGFR2 mut cervical adenocarcinoma predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in a partial response with 50% reduction of tumor size and 56% decrease of DUSP6 score in a patient with cervical adenocarcinoma harboring FGFR2 amplification and FGFR2 mutation (PMID: 30745300; NCT01948297). 30745300
FGFR2 - ZMYM4 FGFR2 N549H FGFR2 N549K FGFR2 V564F FGFR2 E565A FGFR2 K659M cholangiocarcinoma predicted - resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, FGFR2 mutations E565A, K659M, N549H, N549K and V564F were identified in the cell-free DNA of a cholangiocarcinoma patient harboring FGFR2-ZMYM4 fusion after the patient progressed while on Infigratinib (BGJ398) treatment (PMID: 28034880). 28034880
FGFR2 - OPTN FGFR2 N549H FGFR2 V564F FGFR2 E565A FGFR2 L617V FGFR2 K641R cholangiocarcinoma predicted - resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, FGFR2 mutations E565A, K641R, L617V, N549H and V564F were identified in the cell-free DNA of a cholangiocarcinoma patient harboring FGFR2-OPTN fusion after the patient progressed while on Infigratinib (BGJ398) treatment (PMID: 28034880). 28034880
FGFR2 - CLIP1 FGFR2 N549H Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, a transformed cell line expressing both FGFR2-CLIP1 and FGFR2 N549H demonstrated resistance to Dovitinib (TKI258) treatment in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 FGFR2 N549H Advanced Solid Tumor resistant FGFR2 Inhibitor Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, a transformed cell line expressing both FGFR2-CLIP1 and FGFR2 N549H demonstrated resistance to Pemazyre (pemigatinib) treatment in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 FGFR2 N549H cholangiocarcinoma predicted - resistant FGFR2 Inhibitor Pemigatinib Case Reports/Case Series Actionable In a clinical case study, a cholangiocarinoma patient harboring FGFR2-CLIP1 demonstrated an initial partial response following treatment with Pemazyre (pemigatinib), but progressed after 5 months, and was determined to have an acquired FGFR2 N549H mutation (PMID: 31371345). 31371345
FGFR2 - CLIP1 FGFR2 N549H Advanced Solid Tumor resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, a transformed cell line expressing both FGFR2-CLIP1 and FGFR2 N549H demonstrated resistance to AZD4547 treatment in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 FGFR2 N549H Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, a transformed cell line expressing both FGFR2-CLIP1 and FGFR2 N549H demonstrated resistance to Infigratinib (BGJ398) treatment in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 FGFR2 N549H Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) treatment inhibited viability of a transformed cell line expressing both FGFR2-CLIP1 and FGFR2 N549H in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 FGFR2 N549H Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, a transformed cell line expressing both FGFR2-CLIP1 and FGFR2 N549H demonstrated resistance to Balversa (erdafitinib) treatment in culture (PMID: 31371345). 31371345
FGFR2 V564L Advanced Solid Tumor resistant FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 did not inhibit Fgfr2 phosphorylation in transformed cells over expressing FGFR2 V564L in culture (PMID: 25169980). 25169980
FGFR2 - PPHLN1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth of transformed cells expressing FGFR2-PPHLN1 in culture (PMID: 25608663). 25608663
FGFR2 - PPHLN1 cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited viability and migration of cholangiocarcinoma cells expressing FGFR2-PPHLN1 in culture (PMID: 25608663). 25608663
FGFR2 H167_N173del FGFR2 L617F intrahepatic cholangiocarcinoma predicted - resistant FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a clinical study, a patient with intrahepatic cholangiocarcinoma harboring FGFR2 H167_N173del developed resistance to Debio 1347 treatment after initial response, FGFR2 L617F was identified as an acquired mutation at disease progression (J Clin Oncol 38, 2020 (suppl 4; abstr 567)). detail...
FGFR2 - DDX21 cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in stable disease in a patient with cholangiocarcinoma harboring FGFR2-DDX21 (PMID: 30745300; NCT01948297). 30745300
FGFR2 M536I Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M536I demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 M536I Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M536I demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 M536I Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr2 phosphorylation and proliferation in transformed cells expressing FGFR2 M536I (PMID: 23908597). 23908597
FGFR2 - MBIP lung non-small cell carcinoma predicted - sensitive FGFR2 Inhibitor AZD4547 Case Reports/Case Series Actionable In a Phase II trial (NLMT), AZD4547 treatment resulted in a confirmed response for over 20 months in a patient with non-small cell lung cancer harboring FGFR2-MBIP fusion (PMID: 32669708, NCT02664935). 32669708
FGFR2 S252W endometrial cancer sensitive FGFR Inhibitor (Pan) Nintedanib Preclinical Actionable In a preclinical study, Ofev (Nintedanib) inhibited cell proliferation in endometrial cancer cells harboring FGFR2 S252W mutation in culture (PMID: 22238366). 22238366
FGFR2 S252W endometrial cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of endometrial cancer cells harboring FGFR2 S252W in culture (PMID: 22238366). 22238366
FGFR2 S252W endometrial cancer sensitive Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) inhibited growth of endometrial cancer cells harboring FGFR2 S252W in culture (PMID: 22238366). 22238366
FGFR2 S252W endometrial carcinoma sensitive RO5126766 Preclinical - Cell culture Actionable In a preclinical study, RO5126766 inhibited proliferation of endometrial carcinoma cells harboring FGFR2 S252W in culture (PMID: 26438159). 26438159
FGFR2 S252W endometrial carcinoma sensitive GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK3052230 (FP-1039) treatment resulted in greater tumor growth inhibition (95% vs 30%) in cell line xenograft models of endometrial carcinoma harboring FGFR2 S252W compared to FGFR2 wild-type models (PMID: 23536011). 23536011
FGFR2 S252W Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 S252W were sensitive to Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 S252W endometrial cancer sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of endometrial cancer cells harboring FGFR2 S252W in culture (PMID: 27627808). 27627808
FGFR2 S252W endometrial cancer sensitive FGFR2 Inhibitor E7090 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 S252W (PMID: 18552176) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 18552176 27535969
FGFR2 S252W endometrial carcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 S252W demonstrated decreased sensitivity to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR2 S252W endometrial cancer decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) did not potently inhibit cell proliferation in endometrial cancer cells harboring FGFR2 S252W mutation in culture (PMID: 22238366). 22238366
FGFR2 S252W endometrial cancer decreased response FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells harboring Fgfr2 S252W were less sensitive to the anti-proliferative effects of AZD4547 than the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR2 S252W endometrial cancer sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr2 phosphorylation and cell proliferation in endometrial cancer cells harboring FGFR2 S252W in culture (PMID: 22238366). 22238366
FGFR2 S252W endometrial carcinoma decreased response RO4987655 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 S252W demonstrated decreased response to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 S252W endometrial cancer sensitive FGFR2 Inhibitor Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited proliferation of endometrial cancer cells harboring an FGFR2 S252W mutation in culture and inhibited tumor growth in FGFR2 S252W-positive endometrial cancer cell line xenograft models (PMID: 25169980). 25169980
FGFR2 - SHTN1 FGFR2 E565A FGFR2 L617M cholangiocarcinoma predicted - resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a Phase II trial, a patient with cholangiocarcinoma harboring FGFR2-SHTN1 initially responded to treatment with Infigratinib (BGJ398), but progressed after eight months and via repeat tissue biopsy was found to have acquired FGFR2 E565A, and via circulating tumor DNA testing, FGFR2 L617M (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A FGFR2 L617M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the addition of Sapanisertib (MLN0128) therapy restored the sensitivity of transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A to treatment with Infigratinib (BGJ398), demonstrating synergistic effects (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M cholangiocarcinoma resistant FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with Balversa (erdafitinib) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the addition of Sapanisertib (MLN0128) therapy restored the sensitivity of transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M to treatment with Balversa (erdafitinib), demonstrating synergistic effects (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the addition of Sapanisertib (MLN0128) therapy restored the sensitivity of transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M to treatment with Infigratinib (BGJ398), demonstrating synergistic effects (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with Infigratinib (BGJ398) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor sensitive FGFR2 Inhibitor AZD4547 + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the addition of Sapanisertib (MLN0128) therapy restored the sensitivity of transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M to treatment with AZD4547, demonstrating synergistic effects (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A were sensitive to treatment with Iclusig (ponatinib) in culture, demonstrating reduced cell viability (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with Infigratinib (BGJ398) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M cholangiocarcinoma resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with AZD4547 in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M cholangiocarcinoma resistant FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with Futibatinib (TAS-120) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M were sensitive to treatment with Iclusig (ponatinib) in culture, demonstrating reduced cell viability (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with AZD4547 in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the combination therapy of Iclusig (ponatinib) and Sapanisertib (MLN0128) resulted in synergistic effects in transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 L617M Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with Balversa (erdafitinib) in culture (PMID: 31911531). 31911531
FGFR2 Y376C intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor AZD4547 Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, including a partial response with 69% reduction in target lesion size and progression-free survival of 9.8 months in a patient with intrahepatic cholangiocarcinoma harboring FGFR2 Y376C (PMID: 32463741; NCT02465060). 32463741
FGFR2 - AFF3 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited Fgfr phosphorylation and downstream signaling, resulted in growth inhibition of transformed cells expressing FGFR2-AFF3 in culture (PMID: 28416604). 28416604
FGFR2 fusion intrahepatic cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Phase II Actionable In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 36.2% (21/58) in patients harboring FGFR2 fusions (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778). detail...
FGFR2 fusion intrahepatic cholangiocarcinoma sensitive FGFR2 Inhibitor Derazantinib Phase I Actionable In a Phase Ib/II trial, Derazantinib (ARQ 087) treatment resulted in an overall response rate of 20.7% (6/29), a disease control rate of 82.8% (24/29), and a median progression-free survival of 5.7 months in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (PMID: 30420614; NCT01752920). 30420614
FGFR2 fusion cholangiocarcinoma sensitive FGFR2 Inhibitor Pemigatinib Guideline Actionable Pemazyre (pemigatinib) is included in guidelines as subsequent-line therapy for patients with cholangiocarcinoma harboring FGFR2 fusions or rearrangements (NCCN.org). detail...
FGFR2 fusion cholangiocarcinoma sensitive FGFR2 Inhibitor Pemigatinib FDA approved - Has Companion Diagnostic Actionable In a Phase II (FIGHT-202) trial, Pemazyre (pemigatinib) treatment resulted in an objective response in 35.5% (38/107, 3 complete response, 35 partial response) of patients with advanced cholangiocarcinoma harboring FGFR2 fusions or rearrangements, with a disease control rate of 82% (88/107), median time-to-response of 2.7 months, and a median progression-free survival of 6.9 months (PMID: 32203698; NCT02924376). detail... 32203698 detail...
FGFR2 fusion biliary tract cancer predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in stable disease over 24 weeks in two biliary tract cancer patients harboring FGFR2 fusions (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). detail...
FGFR2 fusion Advanced Solid Tumor predicted - sensitive FGFR2 Inhibitor Debio 1347 Phase I Actionable In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297). 30745300
FGFR2 fusion cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a Phase I trial, two patients with cholangiocarcinoma harboring FGFR2 fusions demonstrated a decreased tumor burden when treated with Infigratinib (BGJ398) (PMID: 27870574). 27870574
FGFR2 fusion cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Phase II Actionable In a Phase II trial, Infigratinib (BGJ398) treatment demonstrated manageable toxicity, resulted in an objective response rate of 18.8% (9/48, 9 partial responses) and a disease control rate of 83.3% (40/48) in patients with advanced cholangiocarcinoma harboring FGFR2 fusions (PMID: 29182496; NCT02150967). 29182496
FGFR2 fusion transitional cell carcinoma predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Phase I Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 46% (12/26) in patients with urothelial carcinoma harboring FGFR genomic alterations, including 17 with FGFR3 mutations, and 11 with FGFR2 and/or FGFR3 fusions (PMID: 31088831; NCT01703481). 31088831
FGFR2 fusion cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Phase I Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 27% (3/11) in patients with cholangiocarcinoma harboring FGFR genomic alterations, including 1 with FGFR2 mutation, 2 with FGFR3 mutations, and 8 with FGFR2 fusions (PMID: 31088831; NCT01703481). 31088831
FGFR2 fusion cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in an objective response rate of 25% (7/28, 7 partial responses) in patients with cholangiocarcinoma harboring FGFR2 fusions, with 71% of patients experienced tumor shrinkage, 54% (15/28) achieved stable disease (Annals of Oncology, Volume 29, Issue suppl_5). detail...
FGFR2 fusion FGFR2 V564F cholangiocarcinoma predicted - resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, FGFR2 V564F was identified in the cell-free DNA of 3 cholangiocarcinoma patients harboring FGFR2 fusion after the patients progressed while on Infigratinib (BGJ398) treatment (PMID: 28034880). 28034880
FGFR2 fusion FGFR1 amp colon cancer predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in a partial response with 49.5% reduction of tumor size and 66% decrease of DUSP6 score in a patient with colon cancer harboring FGFR1 amplification and FGFR2 fusion (PMID: 30745300; NCT01948297). 30745300
FGFR2 fusion FGFR2 M538I intrahepatic cholangiocarcinoma decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 M538I had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 M538I intrahepatic cholangiocarcinoma decreased response FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 M538I had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 M538I intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 M538I were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 N550H intrahepatic cholangiocarcinoma decreased response FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550H had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 N550H intrahepatic cholangiocarcinoma decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550H had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 N550H intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550H were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 N550K intrahepatic cholangiocarcinoma resistant FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550K were resistant to treatment, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 N550K intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550K were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 N550K intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550K were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 V565F intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 V565F were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 V565F intrahepatic cholangiocarcinoma decreased response FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 V565F had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 V565F intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 V565F were resistant to treatment, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 L618V intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 L618V were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 L618V intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 L618V were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 L618V intrahepatic cholangiocarcinoma resistant FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 L618V were resistant to treatment, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 K660M intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K660M were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 K660M intrahepatic cholangiocarcinoma resistant FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K660M were resistant to treatment, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 K660M intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K660M were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 H683L intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 H683L were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 H683L intrahepatic cholangiocarcinoma decreased response FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 H683L had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 H683L intrahepatic cholangiocarcinoma decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 H683L had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 K715R intrahepatic cholangiocarcinoma sensitive FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K715R were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling, in in vitro assays (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 K715R intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K715R were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 fusion FGFR2 K715R intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K715R were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling, in in vitro assays (PMID: 31109923). 31109923
FGFR2 - FN1 liver cancer predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Pdx Actionable In a preclinical study, Infigratinib (BGJ398) treatment inhibited tumor growth in a patient-derived xenograft (PDX) model of liver cancer harboring FGFR2-FN1 (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). detail...
FGFR2 M538I Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M538I demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 M538I Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M538I demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 M538I Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M538I demonstrated a decreased response to treatment with Iclusig (ponatinib) (PMID: 23908597). 23908597
FGFR2 - INA FGFR2 M538I FGFR2 N550H FGFR2 N550T FGFR2 L618V FGFR2 H683L intrahepatic cholangiocarcinoma resistant FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a clinical case study, a patient with intrahepatic cholangiocarcinoma harboring an FGFR2-INA fusion developed progressive disease after initial response to Debio 1347 for 11.4 months and FGFR2 H683L, L618V, N550H, N550T, M538I mutations were identified post-progression (PMID: 31109923). 31109923
FGFR2 - INA FGFR2 M538I FGFR2 N550H FGFR2 N550T FGFR2 L618V FGFR2 H683L intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-INA fusion with FGFR2 H683L, L618V, N550H, N550T, M538I mutations, responded to TAS-120 for 5.1 months before progressing due to acquired FGFR2 V565L and E566A mutations, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR2 - CCDC6 liver cancer sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in tumor regression in patient-derived xenograft models of liver cancer harboring FGFR2-CCDC6 fusion (PMID: 28978721). 28978721
FGFR2 - CCDC6 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited Fgfr phosphorylation and downstream signaling, resulted in growth inhibition of transformed cells expressing FGFR2-CCDC6 in culture (PMID: 28416604). 28416604
FGFR2 - CCDC6 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-CCDC6 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - CCDC6 FGFR3 - TACC3 adrenal carcinoma predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted tumor shrinkage and no disease progression for 10 months in an adrenal carcinoma patient harboring FGFR3-TACC3 and FGFR2-CCDC6 fusions (PMID: 26324363; NCT01703481). 26324363
FGFR2 K310R FGFR2 N549K endometrial carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring both FGFR2 K310R and N549K were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR2 K310R FGFR2 N549K endometrial carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring both FGFR2 K310R and N549K were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 K310R FGFR2 N549K endometrial cancer sensitive FGFR2 Inhibitor Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of endometrial cancer cells harboring FGFR2 K310R and FGFR2 N549K mutations in culture (PMID: 25169980). 25169980
FGFR2 K310R FGFR2 N549K endometrial carcinoma sensitive FGFR Inhibitor (Pan) FIIN-1 Preclinical Actionable In a preclinical study, FIIN-01 inhibited proliferation of endometrial carcinoma cell lines harboring FGFR2 N549K and FGFR2 K310R mutations in culture (PMID: 20338520). 20338520
FGFR2 K310R FGFR2 N549K endometrial carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring both FGFR2 K310R and N549K were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Pdx & cell culture Actionable In a preclinical study, AZD4547 inhibited proliferation of endometrial cells and delayed tumor growth in cell-line derived xenografts harboring the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 N550K and K310R in culture (PMID: 30537101). 30537101
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive FGFR Inhibitor (Pan) ABT-737 + Infigratinib Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 N550K and K310R demonstrated increased cell death following treatment with Infigratinib (BGJ398) and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell line xenograft Actionable In a preclinical study, Infigratinib (BGJ398) treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 N550K and K310R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 30537101). 30537101
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive ABT-737 + PD173074 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 N550K and K310R demonstrated increased cell death following treatment with PD173074 and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 N550K and K310R in culture (PMID: 30537101). 30537101
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive FGFR Inhibitor (Pan) Infigratinib + Navitoclax Preclinical - Cell line xenograft Actionable In a preclinical study, Infigratinib (BGJ398) and Navitoclax (ABT-263) combination treatment enhanced apoptosis, and inhibited tumor growth and induced regression in a cell line xenograft model of endometrial cancer harboring FGFR2 K310R and N550K compared to either agent alone (PMID: 30537101). 30537101
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive FGFR2 Inhibitor ABT-737 + AZD4547 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 N550K and K310R demonstrated increased cell death following treatment with AZD4547 and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 E566G Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 E566G were resistant to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 E566G Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr2 phosphorylation and proliferation in transformed cells expressing FGFR2 E566G (PMID: 23908597). 23908597
FGFR2 E566G Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 E566G were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 - CLIP1 Advanced Solid Tumor sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment inhibited viability of a transformed cell line expressing FGFR2-CLIP1 in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment inhibited viability of a transformed cell line expressing FGFR2-CLIP1 in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, a transformed cell line expressing FGFR2-CLIP1 demonstrated resistance to Dovitinib (TKI258) treatment in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) treatment inhibited viability of a transformed cell line expressing FGFR2-CLIP1 in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 Advanced Solid Tumor sensitive FGFR2 Inhibitor Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) treatment inhibited viability of a transformed cell line expressing FGFR2-CLIP1 in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) treatment inhibited viability of a transformed cell line expressing FGFR2-CLIP1 in culture (PMID: 31371345). 31371345
FGFR2 - CLIP1 cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Pemigatinib Case Reports/Case Series Actionable In a clinical case study, a cholangiocarinoma patient harboring FGFR2-CLIP1 demonstrated a partial response following treatment with Pemazyre (pemigatinib) (PMID: 31371345). 31371345
FGFR2 positive breast cancer predicted - sensitive FGFR Inhibitor (Pan) Rogaratinib Phase I Actionable In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR2-positive breast cancer (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR2 positive breast cancer sensitive Aprutumab ixadotin Preclinical - Pdx & cell culture Actionable In a preclinical study, Aprutumab ixadotin (BAY1187982) inhibited survival of Fgfr2 positive breast cancer cell lines in culture, and suppressed tumor growth in both cell line and patient-derived xenograft models (PMID: 27543601). 27543601
FGFR2 positive Advanced Solid Tumor sensitive Aprutumab ixadotin Preclinical - Pdx & cell culture Actionable In a preclinical study, sensitivity to Aprutumab ixadotin (BAY1187982) positively correlated with Fgfr2 expression level in a variety of cancer cell lines in culture, and in cell line or patient-derived xenograft models (PMID: 27543601). 27543601
FGFR2 positive stomach cancer sensitive Aprutumab ixadotin Preclinical - Pdx & cell culture Actionable In a preclinical study, Aprutumab ixadotin (BAY1187982) inhibited survival of gastric cancer cell lines with elevated Fgfr2 expression level in culture, and suppressed tumor growth in cell line or patient-derived xenograft models (PMID: 27543601). 27543601
FGFR1 pos FGFR2 pos hepatocellular carcinoma no benefit PHA-665752 Preclinical - Cell culture Actionable In a preclinical study, PHA-665752 treatment did not result in decreased colony formation or reduced phosphorylation levels of FGFR1 and FGFR2 in hepatocellular carcinoma cells in culture (PMID: 26351320). 26351320
FGFR1 pos FGFR2 pos hepatocellular carcinoma sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, hepatocellular carcinoma cell lines treated with AZD4547 demonstrated decreased phosphorylation of FGFR1 and FGFR2, reduced colony formation, and evidence of apoptotic activity in culture (PMID: 26351320). 26351320
FGFR2 pos FGFR3 pos breast carcinoma sensitive FGFR2 Inhibitor E7090 Preclinical Actionable In a preclinical study, a mouse breast carcinoma cell line xenograft model demonstrated inhibition of tumor growth when treated with E7090, a result of decreased FGFR2 and FGFR3 activity (PMID: 27535969). 27535969
FGFR2 - SORBS1 FGFR2 V565F intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion, responded to TAS-120 for 15.8 months before progressing due to an acquired FGFR2 V565F mutation, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR2 - CCAR2 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-CCAR2 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 over exp Advanced Solid Tumor sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell line xenograft Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr2 in culture and in cell line xenograft models (PMID: 27627808). 27627808
FGFR2 over exp colorectal cancer sensitive Aprutumab ixadotin Preclinical - Cell line xenograft Actionable In a preclinical study, Aprutumab ixadotin (BAY1187982) inhibited survival of colorectal cancer cells with over expressing Fgfr2 in culture, and suppressed tumor growth in cell line xenograft models (PMID: 27543601). 27543601
FGFR2 over exp Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing wild-type FGFR2 in culture (PMID: 28978721). 28978721
FGFR2 over exp breast cancer sensitive FGFR2 Inhibitor AZ8010 Preclinical Actionable In a preclinical study, AZ8010 inhibited downstream Erk phosphorylation and proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). 22869148
FGFR2 over exp Advanced Solid Tumor predicted - sensitive FGFR Inhibitor (Pan) Rogaratinib Phase I Actionable In a Phase I trial, treatment with Rogaratinib (BAY 1163877) was well-tolerated and resulted in objective response rate (ORR) of 15% (15/100) in patients with FGFR1, FGFR2, or FGFR3-overexpressing advanced solid tumors, including urothelial cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer, and led to an ORR of 67% (10/15) in patients with FGFR overexpression, but without an FGFR genetic aberration (PMID: 31405822). 31405822
FGFR2 over exp endometrial cancer resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells with Fgfr2 overexpression were resistant to the anti-proliferative effects of AZD4547 (PMID: 26294741). 26294741
FGFR2 over exp breast cancer sensitive PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). 22869148
FGFR2 over exp breast cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited downstream Erk phosphorylation and proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). 22869148
FGFR2 mutant endometrial cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) inhibited the growth of FGFR2-mutated endometrial cancer cells in vitro and in xenograft models (PMID: 23443805). 23443805
FGFR2 mutant Advanced Solid Tumor predicted - sensitive FGFR2 Inhibitor Debio 1347 Phase I Actionable In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297). 30745300
FGFR2 mutant cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Phase I Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 27% (3/11) in patients with cholangiocarcinoma harboring FGFR genomic alterations, including 1 with FGFR2 mutation, 2 with FGFR3 mutations, and 8 with FGFR2 fusions (PMID: 31088831; NCT01703481). 31088831
FGFR2 mutant cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a Phase I trial, a patient with cholangiocarcinoma harboring an FGFR2 mutation demonstrated a decreased tumor burden when treated with Infigratinib (BGJ398) (PMID: 27870574). 27870574
FGFR2 mutant transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib Guideline Actionable Balversa (erdafitinib) is included in the guidelines for patients with advanced or metastatic urothelial carcinoma harboring Fgfr2 alterations after progression on platinum-based regimens (NCCN.org). detail...
FGFR2 mutant transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - Has Companion Diagnostic Actionable In a Phase II trial (BCL2001) that supported FDA approval, Balversa (erdafitinib) treatment resulted in an objective response rate of 40% (40/99, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR2 mutant endometrial cancer sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of endometrial cancer cells harboring FGFR2 mutations in culture (AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1249). detail...
FGFR2 mutant Advanced Solid Tumor sensitive FGFR2 Inhibitor Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, a variety of cancer cell lines harboring mutations in FGFR1, FGFR2, and/or FGFR3 demonstrated sensitivity to Pemazyre (pemigatinib) in culture and in cell line xenograft models, resulting in inhibition of tumor growth (Cancer Res 2015;75(15 Suppl):Abstract nr 771). detail...
FGFR2 mutant bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - Has Companion Diagnostic Actionable In a Phase II trial (BCL2001) that supported FDA approval, Balversa (erdafitinib) treatment resulted in an objective response rate of 40% (40/99, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR2 mutant bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib Guideline Actionable Balversa (erdafitinib) is included in the guidelines for patients with advanced or metastatic urothelial carcinoma harboring Fgfr2 alterations after progression on platinum-based regimens (NCCN.org). detail...
FGFR2 K660N Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Lenvatinib Preclinical - Cell culture Actionable In a preclinical study, Lenvima (lenvatinib) inhibited growth of transformed cells expressing FGFR2 K660N in culture (PMID: 23786770). 23786770
FGFR2 K660N Advanced Solid Tumor sensitive Cediranib Preclinical - Cell culture Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of transformed cells expressing FGFR2 K660N in culture (PMID: 23786770). 23786770
FGFR2 K660N Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell line xenograft Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth of transformed cells expressing FGFR2 K660N in culture and inhibited tumor growth in xenograft models (PMID: 23786770). 23786770
FGFR2 K660N Advanced Solid Tumor sensitive FGFR2 Inhibitor Pazopanib Preclinical - Cell culture Actionable In a preclinical study, Votrient (pazopanib) inhibited growth of transformed cells expressing FGFR2 K660N in culture (PMID: 23786770). 23786770
FGFR2 K660N Advanced Solid Tumor sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 K660N in culture (PMID: 23786770). 23786770
FGFR2 K660N Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR2 K660N in culture (PMID: 28978721). 28978721 detail...
FGFR2 K660N Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of transformed cells expressing FGFR2 K660N in culture (PMID: 23786770). 23786770
FGFR2 C383R endometrial cancer sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 C383R in culture (PMID: 30537101). 30537101
FGFR2 C383R endometrial cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 C383R in culture (PMID: 30537101). 30537101
FGFR2 C383R endometrial cancer sensitive FGFR Inhibitor (Pan) ABT-737 + Infigratinib Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 C383R demonstrated increased cell death following treatment with Infigratinib (BGJ398) and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 C383R endometrial cancer sensitive FGFR2 Inhibitor ABT-737 + AZD4547 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 C383R demonstrated increased cell death following treatment with AZD4547 and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 C383R endometrial cancer sensitive ABT-737 + PD173074 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 C383R demonstrated increased cell death following treatment with PD173074 and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 C383R endometrial cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 C383R in culture (PMID: 30537101). 30537101
FGFR2 C383R FGFR2 N550K endometrial cancer resistant PD173074 Preclinical Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 C383R and expressing FGFR2 N550K demonstrated resistance when treated with PD173074 (PMID: 23908597). 23908597
FGFR2 V514L lung non-small cell carcinoma no benefit FGFR2 Inhibitor AZD4547 Case Reports/Case Series Actionable In a Phase II trial (NLMT), AZD4547 treatment did not result in a confirmed response or durable clinical benefit in a patient with non-small cell lung cancer harboring FGFR2 V515L (corresponds to V514L in the canonical isoform (PMID: 32669708, NCT02664935). 32669708
FGFR2 - AHCYL1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, treatment with Infigratinib (BGJ398) prevented transformation of cells expressing FGFR2-AHCYL1 in culture (PMID: 24122810). 24122810
FGFR2 - AHCYL1 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-AHCYL1 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - AHCYL1 Advanced Solid Tumor sensitive PD173074 Preclinical Actionable In a preclinical study, treatment with PD173074 prevented transformation of cells expressing FGFR2-AHCYL1 in culture (PMID: 24122810). 24122810
FGFR2 - WDR11 stomach cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Pdx Actionable In a preclinical study, Infigratinib (BGJ398) treatment inhibited tumor growth in a patient-derived xenograft (PDX) model of gastric cancer harboring FGFR2-WDR11 fusion (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). detail...
FGFR2 - SORBS1 FGFR2 K660M FGFR2 K715R intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, a patient with intrahepatic cholangiocarcinoma harboring an FGFR2-SORBS1 fusion developed progressive disease after initial response to Infigratinib (BGJ398) for 12.6 months and FGFR2 K660M and FGFR2 K715R were identified in the post-progression cell-free DNA (PMID: 31109923). 31109923
FGFR2 - SORBS1 FGFR2 K660M FGFR2 K715R intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion with FGFR2 K660M and K175R mutations, responded to TAS-120 for 15.8 months before progressing due to an acquired FGFR2 V565F mutation, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR2 - ROCK1 cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in stable disease in a patient with cholangiocarcinoma harboring FGFR2-ROCK1 (PMID: 30745300; NCT01948297). 30745300
FGFR2 - NRAP intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-NRAP fusion responded to Infigratinib (BGJ398) for 7.1 months before progressing (PMID: 31109923). 31109923
FGFR2 - NRAP intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-NRAP fusion responded to TAS-120 for 17.2 months before progressing due to an acquired FGFR2 N550K mutation, detected in cell-free DNA and the tumor biopsy (PMID: 31109923; NCT02052778). 31109923
FGFR2 - NRAP FGFR2 N550K intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-NRAP fusion responded to TAS-120 for 17.2 months before progressing due to an acquired FGFR2 N550K mutation, detected in cell-free DNA and the tumor biopsy (PMID: 31109923; NCT02052778). 31109923
FGFR2 I548V Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 I548V demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 I548V Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 I548V demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 I548V Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr2 phosphorylation and proliferation in transformed cells expressing FGFR2 I548V (PMID: 23908597). 23908597
FGFR2 - ZMYM4 FGFR2 V563L intrahepatic cholangiocarcinoma resistant FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion with FGFR2 V565F, K660M E566A, N550H, and N550K mutations, responded to TAS-120 for 7.2 months before progressing due to an acquired FGFR2 V563L mutation, detected in cell-free DNA and tumor biopsy (PMID: 31109923; NCT02052778). 31109923
FGFR2 - TACC1 intrahepatic cholangiocarcinoma predicted - resistant FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-TACC1 demonstrated progressive disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - OFD1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited Fgfr phosphorylation and downstream signaling, resulted in growth inhibition of transformed cells expressing FGFR2-OFD1 in culture (PMID: 28416604). 28416604
FGFR2 - BICC1 FGFR2 - OFD1 endometrial cancer predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in partial response in an endometrial cancer patient harboring FGFR2-BICC1 and FGFR2-OFD1 fusions (PMID: 26324363; NCT01703481). 26324363
FGFR2 dec exp breast cancer resistant Aprutumab ixadotin Preclinical - Cell culture Actionable In a preclinical study, Aprutumab ixadotin (BAY1187982) did not inhibit growth of breast cancer cells with very low Fgfr2 expression level in culture (PMID: 27543601). 27543601
FGFR2 V565I Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 V565I were resistant to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 V565I Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 V565I were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 V565I Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 V565I were resistant to treatment with Iclusig (ponatinib) (PMID: 23908597). 23908597
FGFR2 act mut Advanced Solid Tumor sensitive FGFR2 Inhibitor Debio 1347 Phase I Actionable In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR2 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). detail...
FGFR2 act mut Advanced Solid Tumor decreased response Cediranib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Cediranib (AZD-2171) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR2 act mut Advanced Solid Tumor predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Phase I Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in stable disease in 70% (16/23) and partial response in 22% (5/23) of patients with advanced solid tumors harboring FGFR 1-4 activating mutations (including amplifications, mutations and translocations), while no antitumor activity was observed in patients with unknown or no known changes in FGFR (PMID: 26324363; NCT01703481). 26324363
FGFR2 act mut Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR2 in culture (PMID: 22238366). 22238366
FGFR2 act mut Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR2 in culture (PMID: 22238366). 22238366
FGFR2 act mut Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Nintedanib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR2 act mut Advanced Solid Tumor predicted - sensitive FGFR2 Inhibitor AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, with a partial response in 1 and stable disease in 2 of 12 patients with FGFR2 activating mutations (PMID: 32463741; NCT02465060). 32463741
FGFR2 act mut endometrial cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell line xenograft Actionable In a preclinical study, both cell lines and cell line xenograft models of endometrial cancer with FGFR2 activating mutations showed greater sensitivity to Dovitinib (TKI258) as compared to FGFR2 wild-type (PMID: 23443805). 23443805
FGFR2 act mut Advanced Solid Tumor decreased response Brivanib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Brivanib (BMS-540215) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR2 act mut stomach carcinoma sensitive FGFR2 Inhibitor S-49076 Preclinical - Cell line xenograft Actionable In a preclinical study, S-49076 inhibited Met activation, resulting in growth inhibition of gastric carcinoma cells harboring FGFR2 activating mutations in culture and in cell line xenograft models (PMID: 23804704). 23804704
FGFR2 N550S Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr2 phosphorylation and proliferation in transformed cells expressing FGFR2 N550S (PMID: 23908597). 23908597
FGFR2 N550S Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550S demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 N550S Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550S demonstrated a decreased response to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 F276C intrahepatic cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a Phase II trial, Infigratinib (BGJ398) treatment resulted in partial response after 2 months of therapy and response was maintained for 4 months in a patient with advanced intrahepatic cholangiocarcinoma harboring a FGFR2 F276C mutation, which is consistent with inhibition of Erk signaling in cholangiocarcinoma cells expressing FGFR2 F274C in culture (JCO Precis Oncol 2017:1, 1-13; NCT02150967). detail...
FGFR2 - TACC2 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-TACC2 demonstrated sensitivity to treatment with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 K660E Advanced Solid Tumor sensitive FGFR2 Inhibitor Pazopanib Preclinical - Cell culture Actionable In a preclinical study, Votrient (pazopanib) inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). 23786770
FGFR2 K660E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23908597). 23908597
FGFR2 K660E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). 23786770
FGFR2 K660E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Lenvatinib Preclinical - Cell culture Actionable In a preclinical study, Lenvima (lenvatinib) inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). 23786770
FGFR2 K660E Advanced Solid Tumor decreased response PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 K660E demonstrated a decreased response when treated with PD173074 (PMID: 23908597). 23908597
FGFR2 K660E Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 K660E were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 K660E Advanced Solid Tumor sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). 23786770
FGFR2 K660E Advanced Solid Tumor sensitive Cediranib Preclinical - Cell culture Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). 23786770
FGFR2 K660E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR2 K660E in culture (PMID: 28978721). 28978721 detail...
FGFR2 - CASP7 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited Fgfr phosphorylation and downstream signaling, resulted in growth inhibition of transformed cells expressing FGFR2-CASP7 in culture (PMID: 28416604). 28416604
FGFR2 - CASP7 Advanced Solid Tumor sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR2-CASP7 in culture (PMID: 27627808). 27627808
FGFR2 - BICC1 FGFR2 - CASP7 transitional cell carcinoma predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in partial response for more than 12 months in a urothelial cancer patient harboring FGFR2-BICC1 and FGFR2-CASP7 fusions (PMID: 26324363; NCT01703481). 26324363
FGFR2 - TNS1 triple-receptor negative breast cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell line xenograft Actionable In a preclinical study, triple-receptor negative breast cancer xenograft models harboring FGFR2-TNS1 demonstrated tumor regression when treated with Infigratinib (BGJ398) (PMID: 29203461). 29203461
FGFR2 - TNS1 triple-receptor negative breast cancer sensitive FGFR Inhibitor (Pan) Buparlisib + Infigratinib Preclinical - Cell line xenograft Actionable In a preclinical study, triple-receptor negative breast cancer xenograft models harboring FGFR2-TNS1 demonstrated rapid and complete tumor regression when treated with the combination of Infigratinib (BGJ398) and Buparlisib (BKM120) (PMID: 29203461). 29203461
FGFR2 - TNS1 triple-receptor negative breast cancer no benefit Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, triple-receptor negative breast cancer xenograft models harboring FGFR2-TNS1 demonstrated stable disease upon treatment with Buparlisib (BKM120), but also exhibited general toxicity (PMID: 29203461). 29203461
FGFR2 N550H Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr2 phosphorylation and proliferation in transformed cells expressing FGFR2 N550H (PMID: 23908597). 23908597
FGFR2 N550H Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550H were resistant to treatment with PD173074 (PMID: 23908597). 23908597
FGFR2 N550H Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550H demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 - BFSP2 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-BFSP2 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - ZMYM4 intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-ZMYM4 fusion responded to Infigratinib (BGJ398) for 5.6 months before progressing due to acquired FGFR2 V565F, K660M, E566A, N550H, and N550K mutations, detected in cell-free DNA (PMID: 31109923). 31109923
FGFR2 - CIT intrahepatic cholangiocarcinoma predicted - resistant FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-CIT demonstrated progressive disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - CIT Advanced Solid Tumor sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR2-CIT in culture (PMID: 27627808). 27627808
FGFR2 - FAM76A ovarian cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Patient cell culture Actionable In a preclincal study, Infigratinib (BGJ398) demonstrated enhanced inhibition of the survival in patient-derived ovarian cancer cells harboring FGFR2 - FAM76A in culture (PMID: 24563622). 24563622
FGFR2 W290C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of transformed cells expressing FGFR2 W290C in culture (PMID: 23786770). 23786770
FGFR2 W290C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell line xenograft Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth of transformed cells expressing FGFR2 W290C in culture and inhibited tumor growth in xenograft models (PMID: 23786770). 23786770
FGFR2 W290C Advanced Solid Tumor sensitive Cediranib Preclinical - Cell culture Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of transformed cells expressing FGFR2 W290C in culture (PMID: 23786770). 23786770
FGFR2 W290C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Lenvatinib Preclinical - Cell culture Actionable In a preclinical study, Lenvima (lenvatinib) inhibited growth of transformed cells expressing FGFR2 W290C in culture (PMID: 23786770). 23786770
FGFR2 W290C Advanced Solid Tumor sensitive FGFR2 Inhibitor Pazopanib Preclinical - Cell culture Actionable In a preclinical study, Votrient (pazopanib) inhibited growth of transformed cells expressing FGFR2 W290C in culture (PMID: 23786770). 23786770
FGFR2 W290C Advanced Solid Tumor sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 W290C in culture (PMID: 23786770). 23786770
FGFR2 - SH3GLB1 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-SH3GLB1 demonstrated a partial response when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 S267_D273dup Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) prevented oncogenic transformation of cells expressing FGFR2 S267_D273dup (PMID: 26048680). 26048680
FGFR2 S267_D273dup Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited downstream phosphorylation of Akt and Erk1/2 in cells expressing Fgfr2 S267_D273dup (PMID: 26048680). 26048680
FGFR2 - SORBS1 intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion responded to Infigratinib (BGJ398) for 12.6 months before progressing due to acquired FGFR2 K660M and K175R mutations, detected in cell-free DNA (PMID: 31109923). 31109923
FGFR2 N549K endometrial cancer sensitive FGFR2 Inhibitor Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of endometrial cancer cell lines harboring FGFR2 N549K in culture (PMID: 27627808). 27627808
FGFR2 N549K endometrial cancer resistant FGFR Inhibitor (Pan) Nintedanib Preclinical Actionable In a preclinical study, Ofev (Nintedanib) did not inhibit growth of endometrial cancer cells harboring FGFR2 N549K in cell culture (PMID: 22238366). 22238366
FGFR2 N549K endometrial cancer decreased response FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) did not potently inhibit proliferation of endometrial cancer cell lines harboring FGFR2 N549K in cell culture (PMID: 22238366). 22238366
FGFR2 N549K endometrial carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 N549K were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 N549K endometrial cancer sensitive FGFR2 Inhibitor Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of endometrial cancer cells harboring FGFR2 N549K mutation in culture (PMID: 25169980). 25169980
FGFR2 N549K endometrial carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 N549K were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR2 N549K endometrial cancer sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of endometrial cancer cells harboring FGFR2 N549K in culture and in cell line xenograft models (PMID: 22238366). 22238366
FGFR2 N549K endometrial cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of endometrial cancer cells harboring FGFR2 N549K in cell culture (PMID: 22238366). 22238366
FGFR2 N549K endometrial carcinoma sensitive FGFR Inhibitor (Pan) FIIN-1 Preclinical Actionable In a preclinical study, FIIN-01 inhibited proliferation of endometrial carcinoma cell lines harboring FGFR2 N549K mutation in culture (PMID: 20338520). 20338520
FGFR2 N549K endometrial carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 N549K were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR2 N549K endometrial adenocarcinoma sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of endometrial adenocarcinoma cells harboring FGFR2 N549K in culture (PMID: 28978721). 28978721
FGFR2 N549K endometrial cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of endometrial cancer cells harboring FGFR2 N549K in cell culture (PMID: 22238366). 22238366
FGFR2 - TACC3 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) prevented oncogenic transformation of cells expressing FGFR2-TACC3 (PMID: 26048680). 26048680
FGFR2 - TACC3 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) treatment induced apoptosis, and inhibited Fgfr and Erk phosphorylation, cell proliferation, and tumor growth in a mouse cell line allograft model expressing FGFR2-TACC3 (PMID: 30067876). 30067876
FGFR2 - TACC3 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ganetespib + Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) and Ganetespib combination treatment led to enhanced apoptosis, and inhibited Fgfr and Erk phosphorylation, cell proliferation, and tumor growth in a mouse cell line allograft model expressing FGFR2-TACC3, and demonstrated improved efficacy over either agent alone (PMID: 30067876). 30067876
FGFR2 - TACC3 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited downstream phosphorylation of Akt and Erk1/2 in cells expressing the fusion, FGFR2 - TACC3 (PMID: 26048680). 26048680
FGFR2 - TACC3 Advanced Solid Tumor sensitive Ganetespib Preclinical Actionable In a preclinical study, Ganetespib treatment induced apoptosis, and inhibited Fgfr and Erk phosphorylation, cell proliferation, and tumor growth in a mouse cell line allograft model expressing FGFR2-TACC3 (PMID: 30067876). 30067876
FGFR2 N550K Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr2 phosphorylation and proliferation in transformed cells expressing FGFR2 N550K (PMID: 23908597). 23908597
FGFR2 N550K Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550K were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 N550K endometrial cancer predicted - sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells harboring Fgfr2 N550K were less sensitive to the anti-proliferative effects of AZD4547 than the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR2 N550K endometrial cancer predicted - sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment induced cell death in an endometrial cancer cell line harboring FGFR2 N550K in culture (PMID: 30537101). 30537101
FGFR2 N550K Advanced Solid Tumor resistant PD173074 Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550K were resistant to PD173074 (PMID: 23908597). 23908597
FGFR2 N550K Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR2 N550K in culture (PMID: 28978721). 28978721
FGFR2 N550K endometrial cancer sensitive FGFR Inhibitor (Pan) ABT-737 + Infigratinib Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 N550K demonstrated increased cell death following treatment with Infigratinib (BGJ398) and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 N550K endometrial cancer predicted - sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 treatment induced cell death in an endometrial cancer cell line harboring FGFR2 N550K in culture (PMID: 30537101). 30537101
FGFR2 N550K endometrial cancer sensitive ABT-737 + PD173074 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 N550K demonstrated increased cell death following treatment with PD173074 and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 N550K endometrial cancer predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) treatment induced cell death in an endometrial cancer cell line harboring FGFR2 N550K in culture (PMID: 30537101). 30537101
FGFR2 N550K endometrial cancer sensitive FGFR2 Inhibitor ABT-737 + AZD4547 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 N550K demonstrated increased cell death following treatment with AZD4547 and ABT-737 combination compared to either agent alone in culture (PMID: 30537101). 30537101
FGFR2 wild-type breast cancer resistant FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, ER-negative breast cancer cells with wild-type FGFR2 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR2 wild-type endometrial carcinoma resistant FGFR Inhibitor (Pan) FIIN-1 Preclinical Actionable In a preclinical study, an endometrial carcinoma cell line harboring wild-type FGFR2 was resistant to FIIN-01-induced growth inhibition in culture (PMID: 20338520). 20338520
FGFR2 wild-type endometrial cancer resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells with Fgfr2 wild-type were resistant to the anti-proliferative effects of AZD4547 (PMID: 26294741). 26294741
FGFR2 wild-type colon cancer resistant FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, colon cancer cells with wild-type FGFR2 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR2 wild-type endometrial cancer resistant FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, endometrial cancer cells with wild-type FGFR2 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR2 wild-type stomach cancer resistant FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, gastric cancer cells with wild-type FGFR2 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR2 wild-type Advanced Solid Tumor predicted - sensitive FGFR Inhibitor (Pan) AZ6089 Preclinical Actionable In a preclinical study, AZ12576089 (AZ6089) inhibited FGF2-induced ERK1/2 phosphorylation and cell proliferation in transformed fibroblasts in culture (PMID: 22869148). 22869148
FGFR2 wild-type Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited Fgfr2 activity in transformed cells over expressing wild-type Fgfr2 in culture (AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1249). detail...
ERBB2 amp FGFR2 wild-type stomach cancer resistant FGFR2 Inhibitor AZD4547 Preclinical Actionable In a preclinical study, gastric cancer cells with wild-type FGFR2 and ERBB2 (HER2) amplification were resistant to treatment with AZD4547 in culture (PMID: 22869148). 22869148
FGFR2 P253R head and neck squamous cell carcinoma predicted - sensitive FGFR2 Inhibitor Pazopanib Case Reports/Case Series Actionable In a clinical case study, treatment with Votrient (pazopanib) resulted in reduced tumor size in a patient with head and neck squamous cell carcinoma harboring FGFR2 P253R (PMID: 23786770). 23786770
FGFR2 - KIAA1217 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, treatment with Derazantinib (ARQ 087) in two patients with intrahepatic cholangiocarcinoma harboring FGFR2-KIAA1217 resulted in one with a partial response and one with stable disease (PMID: 30420614; NCT01752920). 30420614
FGFR2 - KIAA1217 cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in stable disease in a patient with cholangiocarcinoma harboring FGFR2-KIAA1217 (PMID: 30745300; NCT01948297). 30745300
FGFR2 - KIAA1217 intrahepatic cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Pdx Actionable In a preclinical study, TAS-120 treatment of an intrahepatic cholangiocarcinoma patient-derived xenograft model, harboring an FGFR2-KIAA1217 fusion, decreased tumor growth and suppressed MEK/ERK signaling (PMID: 31109923). 31109923
FGFR2 - BICC1 intrahepatic cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Case Reports/Case Series Actionable In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 33.3% (5/15) in patients harboring FGFR2-BICC1 fusion (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778). detail...
FGFR2 - BICC1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited Fgfr phosphorylation and downstream signaling, resulted in growth inhibition of transformed cells expressing FGFR2-BICC1 in culture (PMID: 28416604). 28416604
FGFR2 - BICC1 cholangiocarcinoma sensitive FGFR2 Inhibitor Pemigatinib Phase II Actionable In a Phase II (FIGHT-202) trial, Pemazyre (pemigatinib) treatment resulted in an objective response rate (ORR) of 35.5% (38/107, 3 complete response, 35 partial response) in patients with advanced cholangiocarcinoma harboring FGFR2 fusions or rearrangements, 29% (31/107) of the patients harbored FGFR2-BICC1 and achieved an ORR (32.3%, 10/31) and a median progression-free survival (6.80 vs 6.93 months) comparable to the entire group (PMID: 32203698; NCT02924376). 32203698
FGFR2 - BICC1 Advanced Solid Tumor sensitive PD173074 Preclinical Actionable In a preclinical study, treatment with PD173074 prevented transformation of cells expressing FGFR2-BICC1 in culture (PMID: 24122810). 24122810
FGFR2 - BICC1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, treatment with Infigratinib (BGJ398) prevented transformation of cells expressing FGFR2-BICC1 in culture (PMID: 24122810). 24122810
FGFR2 - BICC1 cholangiocarcinoma predicted - sensitive Sorafenib Case Reports/Case Series Actionable In a clinical case study, a patient with cholangiocarcinoma harboring FGFR2-BICC1 achieved a partial response with a reduction in tumor size after one month of Nexavar (sorafenib) treatment (PMID: 31807010). 31807010
FGFR2 - BICC1 intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, treatment with Derazantinib (ARQ 087) in four patients with intrahepatic cholangiocarcinoma harboring FGFR2-BICC1 resulted in one partial response, stable disease in two, and progressive disease in one (PMID: 30420614; NCT01752920). 30420614
FGFR2 - BICC1 FGFR2 V564F cholangiocarcinoma predicted - resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical case study, FGFR2 V564F was identified in the cell-free DNA of a cholangiocarcinoma patient harboring FGFR2-BICC1 fusion after the patient progressed while on Infigratinib (BGJ398) treatment (PMID: 28034880). 28034880
FGFR2 V564F Advanced Solid Tumor resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, transformed cells over expressing FGFR2 V564F were resistant to AZD4547 in culture and in cell line xenograft models (PMID: 25169980). 25169980
FGFR2 V564F Advanced Solid Tumor sensitive FGFR2 Inhibitor Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited proliferation of transformed cells over expressing FGFR2 V564F in culture and inhibited tumor growth in cell line xenograft models (PMID: 25169980). 25169980
FGFR2 V564F Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR2 V564F were resistant to Infigratinib (BGJ398) in culture (PMID: 28034880). 28034880
FGFR2 - SHTN1 cholangiocarcinoma sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing FGFR2-SHTN1 were sensitive to treatment with AZD4547, demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 cholangiocarcinoma predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a Phase II trial, a patient with cholangiocarcinoma harboring FGFR2-SHTN1 experienced a partial response according to RECIST criteria after four months of treatment with Infigratinib (BGJ398) (PMID: 31911531). 31911531
FGFR2 - SHTN1 cholangiocarcinoma resistant FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing FGFR2-SHTN1 demonstrated resistance to treatment with Dovitinib (TKI258) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FGFR2-SHTN1 demonstrated resistance to treatment with Dovitinib (TKI258) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing FGFR2-SHTN1 were sensitive to treatment with Iclusig (ponatinib), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FGFR2-SHTN1 were sensitive to treatment with Iclusig (ponatinib), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing FGFR2-SHTN1 were sensitive to treatment with Balversa (erdafitinib), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing FGFR2-SHTN1 were sensitive to treatment with Futibatinib (TAS-120), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FGFR2-SHTN1 were sensitive to treatment with Balversa (erdafitinib), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 Advanced Solid Tumor sensitive FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FGFR2-SHTN1 were sensitive to treatment with AZD4547, demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FGFR2-SHTN1 were sensitive to treatment with Futibatinib (TAS-120), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Dovitinib (TKI258) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Infigratinib (BGJ398) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A cholangiocarcinoma resistant FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Dovitinib (TKI258) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A cholangiocarcinoma resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with AZD4547 in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A were sensitive to treatment with Iclusig (ponatinib) in culture, demonstrating reduced cell viability (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A cholangiocarcinoma sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A were sensitive to treatment with Iclusig (ponatinib) in culture, demonstrating reduced cell viability (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A cholangiocarcinoma resistant FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Balversa (erdafitinib) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Futibatinib (TAS-120) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor sensitive FGFR2 Inhibitor AZD4547 + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the addition of Sapanisertib (MLN0128) therapy restored the sensitivity of transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A to treatment with AZD4547, demonstrating synergistic effects (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor resistant FGFR2 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with AZD4547 in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A cholangiocarcinoma resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Infigratinib (BGJ398) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the combination therapy of Iclusig (ponatinib) and Sapanisertib (MLN0128) resulted in synergistic effects in transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Balversa (erdafitinib) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A cholangiocarcinoma resistant FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Futibatinib (TAS-120) in culture (PMID: 31911531). 31911531
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib + Sapanisertib Preclinical - Cell culture Actionable In a preclinical study, the addition of Sapanisertib (MLN0128) therapy restored the sensitivity of transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A to treatment with Balversa (erdafitinib), demonstrating synergistic effects (PMID: 31911531). 31911531
FGFR2 - GAB2 breast cancer predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Pdx Actionable In a preclinical study, Infigratinib (BGJ398) treatment inhibited tumor growth in a patient-derived xenograft (PDX) model of breast cancer harboring FGFR2-GAB2 (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). detail...
FGFR2 H167_N173del intrahepatic cholangiocarcinoma predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a clinical study, Debio 1347 treatment resulted in durable partial response of 11 months in 2 patients with intrahepatic cholangiocarcinoma harboring FGFR2 H167_N173del (J Clin Oncol 38, 2020 (suppl 4; abstr 567)). detail...
FGFR2 - INA colon cancer predicted - sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in a partial response in 2 patient with colon cancer harboring FGFR2-INA (PMID: 30745300; NCT01948297). 30745300
FGFR2 - INA intrahepatic cholangiocarcinoma sensitive FGFR2 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a clinical case study, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-INA fusion responded to Debio 1347 for 11.4 months before progressing due to acquired FGFR2 H683L, L618V, N550H, N550T, and M538I mutations (PMID: 31109923). 31109923
FGFR2 V564I Advanced Solid Tumor resistant FGFR2 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 did not inhibit Fgfr2 phosphorylation in transformed cells over expressing FGFR2 V564I in culture (PMID: 25169980). 25169980
Clinical Trial Phase Therapies Title Recruitment Status