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Profile Name FGFR3 V555M
Gene Variant Detail

FGFR3 V555M (gain of function)

Relevant Treatment Approaches FGFR Inhibitor (Pan) FGFR3 Inhibitor

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR3 fusion urinary bladder cancer sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 fusion in culture (PMID: 27550940). 27550940
FGFR3 fusion transitional cell carcinoma predicted - sensitive Docetaxel + Vofatamab Phase Ib/II Actionable In a Phase I/II trial, Vofatamab (B-701) in combination with Taxotere (docetaxel) demonstrated safety and preliminary efficacy, resulted in enhanced activity in patients with locally advanced or metastatic urothelial carcinoma harboring FGFR3 mutations or fusions comparing to wild-type patients (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 4534-4534; NCT02401542). detail...
FGFR3 fusion Advanced Solid Tumor predicted - sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell line xenograft Actionable In a preclinical study, TAS-120 demonstrated growth inhibition and reduced FGFR phosphorylation in human cancer cell lines and xenograft models harboring FGFR mutations (Mol Cancer Ther 2013;12(11 Suppl):A270). detail...
FGFR3 fusion Advanced Solid Tumor predicted - sensitive FGFR3 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
FGFR3 fusion transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Phase I Actionable In a Phase I trial, Infigratinib (BGJ398) treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517)). detail...
FGFR3 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
FGFR3 rearrange myeloid neoplasm sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of myeloma cells harboring FGFR3 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
FGFR3 rearrange myeloid neoplasm sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of myeloma cells harboring FGFR3 rearrangements in culture (AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1249). detail...
FGFR3 K650M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR3 K650M in culture (PMID: 28978721). 28978721
FGFR3 K650E Advanced Solid Tumor sensitive PD98059 Preclinical Actionable In a preclinical study, PD98059 inhibited FGFR3 K650E-induced transformation of cells in culture (PMID: 14534538). 14534538
FGFR3 K650E myeloid neoplasm sensitive FGFR3 Inhibitor SU5402 Preclinical - Cell culture Actionable In a preclinical study, SU5402 inhibited proliferation of myeloma cells expressing FGFR3 K650E in culture (PMID: 23597562). 23597562
FGFR3 K650E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, FIIN-2 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited proliferation of transformed cells expressing FGFR3 K560E in culture (PMID: 26992226). 26992226
FGFR3 K650E myeloid neoplasm sensitive FGFR3 Inhibitor Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 K650E in culture (PMID: 25169980). 25169980
FGFR3 K650E Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to Infigratinib (BGJ398) in culture (PMID: 28034880). 28034880
FGFR3 K650E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) LY2874455 Preclinical - Cell culture Actionable In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E Advanced Solid Tumor sensitive FGFR3 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E myeloid neoplasm no benefit FGFR Inhibitor (Pan) SSR128129E Preclinical Actionable In a preclinical study, SSR128129E did not inhibit proliferation of myeloma cells expressing FGFR3 K650E in culture (PMID: 23597562). 23597562
FGFR3 K650E Advanced Solid Tumor decreased response FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR3 K650E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR3 K650E FGFR3 over exp HRAS K117E myeloid neoplasm sensitive FGFR3 Inhibitor AZ8010 Preclinical Actionable In a preclinical study, AZ8010 inhibited Fgfr3 signaling and decreased proliferation of myeloma cells with HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). 22869148
FGFR3 K650E FGFR3 over exp HRAS K117E multiple myeloma sensitive FGFR3 Inhibitor PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells harboring HRAS H117E and over expression of FGFR3 K650E in culture (PMID: 22869148). 22869148
FGFR3 G372C Advanced Solid Tumor sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-dependent proliferation in cells expressing FGFR3 G372C (PMID: 19381019). 19381019
FGFR3 N540K Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) LY2874455 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to LY2874455 in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor decreased response FGFR3 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K were resistant to Infigratinib (BGJ398) in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 N540K in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 N540K in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to FIIN-2 in culture (PMID: 28034880). 28034880
FGFR3 N540K Advanced Solid Tumor resistant FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K were reistant to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR3 N540K Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinicl study, Balversa (erdafitinib) inhibited proliferation of transformed cells expressing FGFR3 N540K in culture (PMID: 26992226). 26992226
FGFR3 Y373C myeloid neoplasm sensitive FGFR3 Inhibitor Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 Y373C in culture (PMID: 25169980). 25169980
FGFR3 Y373C bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 Y373C is included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 Y373C myeloid neoplasm no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR3 Y373C transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 Y373C is included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 Y373C myeloid neoplasm no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR3 Y373C myeloid neoplasm no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR3 Y373C multiple myeloma sensitive FGFR3 Inhibitor E7090 Preclinical - Cell culture Actionable In a preclinical study, a multiple myeloma cell line harboring FGFR3 Y373C (PMID: 19901323) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 19901323 27535969
FGFR3 Y373C FGFR3 over exp multiple myeloma sensitive FGFR3 Inhibitor AZ8010 Preclinical Actionable In a preclinical study, AZ8010 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). 22869148
FGFR3 Y373C FGFR3 over exp multiple myeloma sensitive FGFR3 Inhibitor PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited Fgfr3 signaling and decreased proliferation and survival of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). 22869148
AKT1 E17K FGFR3 Y373C urinary bladder cancer sensitive FGFR3 Inhibitor AZD4547 + Capivasertib Preclinical Actionable In a preclinical study, the combined therapy of AZD5363 and AZD4547 resulted in tumor regression in urinary bladder cancer xenograft models simultaneously harboring the mutations, AKT1 E17K and FGFR3 Y373C (PMID: 26351323). 26351323
FGFR3 A391E bladder urothelial carcinoma predicted - sensitive FGFR3 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 single nucleotide variants and a 6-month progression-free survival (PFS) rate of 6%, with stable disease in 2 of 7 patients with FGFR3 activating mutations, and a partial response in a patient with urinary bladder transitional cell carcinoma harboring FGFR3 A391E (reported as A393E) (PMID: 32463741; NCT02465060). 32463741
FGFR3 S249C urinary system cancer sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 decreased Myc expression and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture and in xenograft models (PMID: 27401245). 27401245
FGFR3 S249C renal pelvis transitional cell carcinoma predicted - sensitive FGFR3 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 stable disease for greater than 6 months in a patient with transitional cell carcinoma of the renal pelvis harboring FGFR2 S249C (PMID: 32463741; NCT02465060). 32463741
FGFR3 S249C urinary bladder cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 S249C mutation in culture (PMID: 22238366). 22238366
FGFR3 S249C urinary bladder cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of bladder cancer cells harboring FGFR3 S249C mutation in culture (PMID: 22238366). 22238366
FGFR3 S249C urinary bladder cancer sensitive FGFR3 Inhibitor Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited proliferation of bladder cancer cells harboring FGFR3 S249C in culture and inhibited tumor growth in FGFR3 S249C-positive bladder cancer cell line xenograft models (PMID: 25169980). 25169980
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR3 S249C urinary bladder cancer resistant FGFR Inhibitor (Pan) Nintedanib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3 S249C were resistant to Ofev (Nintedanib) induced inhibition of cell proliferation in culture (PMID: 22238366). 22238366
FGFR3 S249C transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 S249C is included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 S249C renal pelvis transitional cell carcinoma predicted - sensitive FGFR3 Inhibitor Pazopanib Clinical Study Actionable In a case study, a patient with urothelial carcinoma of the renal pelvis harboring FGFR3 S249C demonstrated a partial response lasting 9 months following treatment with Votrient (pazopanib) (PMID: 27271022). 27271022
FGFR3 S249C bladder carcinoma sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell line xenograft Actionable In a preclinical study, R3Mab decreased dimer formation and constitutive activation of FGFR3 S249C, and inhibited growth of bladder cancer cell lines harboring FGFR3 S249C in culture and in xenograft models (PMID: 19381019). 19381019
FGFR3 S249C Advanced Solid Tumor sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited proliferation of transformed cells expressing FGFR3 S249C in culture (PMID: 19381019). 19381019
FGFR3 S249C urinary bladder cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of bladder cancer cells harboring FGFR3 S249C in culture (PMID: 22238366). 22238366
FGFR3 S249C urinary system cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture (PMID: 27401245). 27401245
FGFR3 S249C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). 23786770
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR3 S249C urinary bladder cancer sensitive FGFR Inhibitor (Pan) ASP5878 Preclinical - Cell line xenograft Actionable In a preclinical study, ASP5878 treatment inhibited proliferation of a bladder cancer cell line harboring FGFR3 S249C in culture, and resulted in tumor regression in xenograft models (Mol Cancer Ther December 2015 14; A170). detail...
FGFR3 S249C bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Dovitinib Case Reports/Case Series Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in a patient with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 S249C (PMID: 27932416). 27932416
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR3 S249C urinary bladder cancer sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of bladder cancer cells harboring FGFR3 S249C in culture and in cell line xenograft models (PMID: 22238366). 22238366
FGFR3 S249C bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 S249C is included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 S249C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). 23786770
FGFR3 S249C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). 23786770
FGFR3 S249C FGFR3 over exp transitional cell carcinoma sensitive FGFR3 Inhibitor PD173074 Preclinical Actionable In a preclinical study, PD173074 inhibited growth of urothelial carcinoma (UC) cells expressing high levels of FGFR3 S249C, but had reduced efficacy against UC cells with low levels of FGFR3 S249C expression (PMID: 22869148). 22869148
FGFR3 G370C transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 G370C is included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 G370C bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 G370C is included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 dec exp FGFR3 wild-type HRAS G12V transitional cell carcinoma resistant FGFR3 Inhibitor PD173074 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to PD173074 in culture (PMID: 22869148). 22869148
FGFR3 dec exp FGFR3 wild-type HRAS G12V transitional cell carcinoma decreased response FGFR3 Inhibitor AZ8010 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZ8010 in culture (PMID: 22869148). 22869148
FGFR3 dec exp FGFR3 wild-type HRAS G12V transitional cell carcinoma resistant FGFR3 Inhibitor AZD4547 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZD4547 in culture (PMID: 22869148). 22869148
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response FGFR3 Inhibitor AZD4547 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZD4547 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response FGFR3 Inhibitor PD173074 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to PD173074 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response FGFR3 Inhibitor AZ8010 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZ8010 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR3 L608V Advanced Solid Tumor decreased response FGFR3 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to Infigratinib (BGJ398) in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, FIIN-2 inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) LY2874455 Preclinical - Cell culture Actionable In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 L608V Advanced Solid Tumor decreased response FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to AZD4547 in culture (PMID: 28034880). 28034880
FGFR3 V555M FGFR3 L608V transitional cell carcinoma resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with Infigratinib (BGJ398) and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) and FGFR3 L608V (also corresponds to L496V) (PMID: 29848605). 29848605
FGFR3 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
FGFR3 act mut urinary bladder cancer predicted - sensitive FGFR3 Inhibitor S-49076 Preclinical Actionable In a preclinical study, S-49076 inhibited autophosphorylation of FGFR3 and downstream signaling in bladder cancer cells over expressing constitutively active FGFR3 in culture (PMID: 23804704). 23804704
FGFR3 act mut Advanced Solid Tumor no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR3 in culture (PMID: 22238366). 22238366
FGFR3 act mut Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Nintedanib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR3 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR3 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 FGFR3 in culture (PMID: 22238366). 22238366
FGFR3 act mut Advanced Solid Tumor decreased response Cediranib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR3 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
FGFR3 act mut Advanced Solid Tumor sensitive FGFR3 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 FGFR3 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). detail...
FGFR3 act mut Advanced Solid Tumor predicted - sensitive FGFR3 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 7 patients with FGFR3 activating mutations (PMID: 32463741; NCT02465060). 32463741
FGFR3 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 FGFR3 in culture (PMID: 22238366). 22238366
FGFR3 wild-type bladder carcinoma sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell line xenograft Actionable In a preclinical study, R3Mab decreased wild-type FGFR3 activation, thereby inhibited cell proliferation of FGFR3 wild-type human bladder cancer cells in culture and in cell line xenograft models (PMID: 19381019). 19381019
FGFR3 wild-type myeloid neoplasm sensitive FGFR3 Inhibitor SU5402 Preclinical - Cell culture Actionable In a preclinical study, SU5402 inhibited proliferation of myeloma cells expressing wild-type FGFR3 in culture (PMID: 23597562). 23597562
FGFR3 wild-type myeloid neoplasm sensitive FGFR Inhibitor (Pan) SSR128129E Preclinical Actionable In a preclinical study, SSR128129E inhibited proliferation of myeloma cells expressing wild-type FGFR3 in culture (PMID: 23597562). 23597562
FGFR3 wild-type urinary bladder cancer resistant FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, bladder cancer cells with wild-type FGFR3 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer resistant Cediranib Preclinical Actionable In a preclinical study, bladder cancer cells harboring an FGFR3 Y375C mutation were resistant to growth inhibition by Cediranib (AZD-2171) in culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer resistant FGFR Inhibitor (Pan) Nintedanib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3 Y375C were resistant to growth inhibition by Ofev (Nintedanib) in culture (PMID: 22238366). 22238366
FGFR3 Y375C urinary bladder cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). 22238366
FGFR3 Y375C Advanced Solid Tumor sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-dependent proliferation of cells expressing FGFR3 Y375C in culture (PMID: 19381019). 19381019
FGFR3 D764H head and neck squamous cell carcinoma no benefit FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D764H in culture, however, cells expressing FGFR3 D764H did not demonstrate increased sensitivity to Infigratinib (BGJ398) compared to cells expressing wild-type FGFR3 (PMID: 27053219). 27053219
FGFR3 R248C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). 23786770
FGFR3 R248C Advanced Solid Tumor sensitive FGFR3 Inhibitor Pazopanib Preclinical - Cell culture Actionable In a preclinical study, Votrient (pazopanib) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). 23786770
FGFR3 R248C Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). 23786770
FGFR3 R248C transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 R248C is included in the companion diagnostic (PMID: 31340094; NCT02365597). 31340094 detail... detail...
FGFR3 R248C bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3 R248C is included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 R248C Advanced Solid Tumor sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-independent proliferation induced by FGFR3 R248C in cultured cells (PMID: 19381019). 19381019
FGFR3 mutant transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Clinical Study Actionable In a clinical study, Infigratinib (BGJ398) treatment in patients with FGFR3 alterations led to 25.4% (17/67) confirmed responses and a disease control rate of 64% (43/67), which included complete responses, partial responses, and stable disease, and resulted in a median progression-free survival of 3.75 months and a median overall survival of 7.75 months (PMID: 29848605). 29848605
FGFR3 mutant transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Phase I Actionable In a Phase I trial, Infigratinib (BGJ398) treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517); NCT01004224). detail...
FGFR3 mutant Advanced Solid Tumor predicted - sensitive FGFR3 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
FGFR3 mutant transitional cell carcinoma predicted - sensitive Docetaxel + Vofatamab Phase Ib/II Actionable In a Phase I/II trial, Vofatamab (B-701) in combination with Taxotere (docetaxel) demonstrated safety and preliminary efficacy, resulted in enhanced activity in patients with locally advanced or metastatic urothelial carcinoma harboring FGFR3 mutations or fusions comparing to wild-type patients (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 4534-4534; NCT02401542). detail...
FGFR3 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 Fgfr3 alterations after progression on platinum-based regimens (NCCN.org). detail...
FGFR3 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...
FGFR3 mutant transitional cell carcinoma no benefit Atezolizumab Phase II Actionable In a Phase II trial (IMVigor 210, CheckMate 275), Tecentriq (atezolizumab) (n=119) treatment resulted in similar response rate (24% vs 21%, p=0.8) in patients with FGFR3 mutant or wild-type metastatic transitional cell carcinoma (PMID: 31272788). 31272788
FGFR3 mutant transitional cell carcinoma no benefit Nivolumab Phase II Actionable In a Phase II trial (CheckMate 275), Opdivo (nivolumab) (n=270) treatment resulted in similar response rate (20% vs 21%, p=0.2) in patients with FGFR3 mutant or wild-type metastatic transitional cell carcinoma (PMID: 31272788). 31272788
FGFR3 mutant bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in 33% (1/3) of patients with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 mutations (PMID: 27932416). 27932416
FGFR3 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...
FGFR3 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 Fgfr3 alterations after progression on platinum-based regimens (NCCN.org). detail...
FGFR3 mutant transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in 25% tumor shrinkage at week 8 in an urothelial cancer patient harboring FGFR3 mutations (PMID: 26324363; NCT01703481). 26324363
FGFR3 mutant transitional cell carcinoma 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
FGFR3 mutant Advanced Solid Tumor sensitive FGFR3 Inhibitor Pemigatinib Preclinical - Cell line xenograft 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...
FGFR3 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
FGFR3 mutant urinary bladder cancer sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 mutation in culture (PMID: 27550940). 27550940
FGFR3 mutant bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Phase I Actionable In a Phase I trial, patients with bladder urothelial carcinoma harboring an FGFR3 mutation demonstrated a disease control rate of 75% (6/8) when treated with Infigratinib (BGJ398), including 3 patients with a partial response and 3 with stable disease (PMID: 27870574; NCT01004224). 27870574
FGFR3 mutant Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, tumor cell lines with FGFR3 mutations demonstrated sensitivity to Infigratinib (BGJ398) in culture (PMID: 23002168). 23002168
FGFR3 mut FGFR3 over exp urinary bladder cancer sensitive FGFR Inhibitor (Pan) Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 33% (1/3) of non-muscle invasive bladder cancer patients harboring both FGFR3 mutations and FGFR3 over expression (J Clin Oncol 34, 2016 (suppl; abstr 4526)). detail...
FGFR3 over exp transitional cell carcinoma sensitive FGFR3 Inhibitor AZ8010 Preclinical Actionable In a preclinical study, AZ8010 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). 22869148
FGFR3 over exp urinary bladder cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Pdx Actionable In a preclinical study, treatment with Infigratinib (BGJ398) led to improved progression-free survival in a patient-derived xenograft (PDX) model of bladder cancer with FGFR3 over expression (PMID: 26270481). 26270481
FGFR3 over exp multiple myeloma sensitive Vofatamab Phase I Actionable In a Phase I trial, Vofatamab (B-701) demonstrated safety and resulted in stable disease in 42% (6/14) of multiple myeloma patients overexpressing FGFR3 (Blood (ASH Annual Meeting Abstracts) 2012 120: Abstract 4029). detail...
FGFR3 over exp Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation in transformed cells overexpressing wild-type FGFR3 in culture (PMID: 28978721). 28978721
FGFR3 over exp urinary bladder cancer sensitive FGFR3 Inhibitor SU5402 Preclinical Actionable In a preclinical study, SU5402 inhibited growth of bladder cancer cells over expressing wild-type FGFR3 in culture (PMID: 21119661). 21119661
FGFR3 over exp Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) LY2874455 Preclinical Actionable In a preclinical study, LY2874455 induced tumor regression in FGFR3-over expressing bladder and multiple myeloma xenograft models (PMID: 21900693). 21900693
FGFR3 over exp head and neck squamous cell carcinoma sensitive FGFR Inhibitor (Pan) Rogaratinib Preclinical Actionable In a preclinical study, Rogaratinib (BAY 1163877) inhibited tumor growth in a head and neck squamous cell carcinoma xenograft model with FGFR3 overexpression (Cancer Res August 1, 2015 75:772). detail...
FGFR3 over exp urinary bladder cancer sensitive FGFR Inhibitor (Pan) Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 8% (1/13) of non-muscle invasive bladder cancer patients over expressing FGFR3 (J Clin Oncol 34, 2016 (suppl; abstr 4526)). detail...
FGFR3 over exp glioblastoma multiforme sensitive U0126 Preclinical Actionable In a preclinical study, U0126 inhibited downstream signaling and growth of glioblastoma cells over-expressing Fgfr3 in culture (PMID: 23298836). 23298836
FGFR3 over exp urinary bladder cancer sensitive Dactolisib + Sorafenib Preclinical - Pdx Actionable In a preclinical study, the combination of BEZ235 and Nexavar (sorafenib) resulted in improved progression-free survival in an FGFR3-over expressing patient-derived xenograft (PDX) model of bladder cancer with secondary resistance to BGJ398 due to reactivation of downstream signaling, as evidenced by increased activation of Akt and Erk (PMID: 26270481). 26270481
FGFR3 over exp transitional cell carcinoma sensitive FGFR3 Inhibitor AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). 22869148
FGFR3 S756P lung non-small cell carcinoma no benefit FGFR3 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 FGFR3 S758P (corresponds to S756P in the canonical isoform (PMID: 32669708, NCT02664935). 32669708
FGFR3 K652E Advanced Solid Tumor sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell culture Actionable In a preclinical study, R3Mab inhibited ligand-dependent cell proliferation in cells expressing FGFR3 K652E in culture (PMID: 19381019). 19381019
FGFR3 K652E urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3 K652E in culture (PMID: 27627808). 27627808
FGFR3 - TACC3 malignant glioma sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Fgfr3 kinase activity in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture (PMID: 22837387). 22837387
FGFR3 - TACC3 transitional cell carcinoma predicted - sensitive FGFR3 Inhibitor AZD4547 Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with urothelial carcinoma harboring FGFR3-TACC3, with a 70% reduction in target lesions and a progression-free survival of 10.9 months (PMID: 32463741; NCT02465060). 32463741
FGFR3 - TACC3 urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cell lines harboring FGFR3-TACC3 fusion in culture (PMID: 27627808). 27627808
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR Inhibitor (Pan) FIIN-1 Preclinical Actionable In a preclinical study, FIIN-1 inhibited growth of the RT4 bladder cancer cell line, which has been demonstrated to harbor an FGFR3-TACC3 fusion, in culture (PMID: 20338520, PMID: 23175443). 23175443 20338520
FGFR3 - TACC3 urinary bladder cancer predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in a partial response with 38% shrinkage of tumor in a patient with metastatic bladder cancer harboring FGFR3-TACC3, who stayed on treatment for 10 months (PMID: 28416604; NCT01703481). 28416604
FGFR3 - TACC3 transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in partial response in 2 urothelial cancer patients harboring FGFR3-TACC3 (PMID: 26324363; NCT01703481). 26324363
FGFR3 - TACC3 transitional cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3-TACC3 v1 and v3 fusions are included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 - TACC3 glioblastoma multiforme sensitive U0126 Preclinical Actionable In a preclinical study, U0126 inhibited downstream signaling and growth of glioblastoma cells expressing the FGFR3-TACC3 fusion in culture (PMID: 23298836). 23298836
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR Inhibitor (Pan) ASP5878 Preclinical - Cell line xenograft Actionable In a preclinical study, ASP5878 treatment inhibited proliferation of bladder cancer cell lines harboring a FGFR3-TACC3 fusion in culture, and resulted in tumor regression in a FGFR3-TACC3 positive bladder cancer cell line xenograft model (Mol Cancer Ther December 2015 14; A170). detail...
FGFR3 - TACC3 urinary bladder cancer sensitive BO-264 Preclinical - Cell culture Actionable In a preclinical study, BO-264 treatment inhibited Erk1/2 phosphorylation, induced mitotic arrest, and reduced viability of an urinary bladder cancer cell line harboring FGFR3-TACC3 in culture (PMID: 32217742). 32217742
FGFR3 - TACC3 malignant glioma sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Balversa (erdafitinib) inhibited proliferation of glioma cells harboring FGFR3-TACC3 fusion in culture and xenograft tumor growth in animal models (PMID: 25609060). 25609060
FGFR3 - TACC3 bladder transitional cell papilloma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR3 - TACC3 transitional cell carcinoma predicted - sensitive FGFR Inhibitor (Pan) Alpelisib + Infigratinib Phase I Actionable In a Phase Ib trial, Infigratinib (BGJ398) and Alpelisib (BYL719) combination treatment resulted in partial response and a complete shrinkage of target lesions lasting 4 months in one urothelial carcinoma patient harboring a FGFR3-TACC3 fusion (J Clin Oncol 34, 2016 (suppl; abstr 2500)). detail...
FGFR3 - TACC3 urinary bladder 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 bladder cancer cell line harboring FGFR3-TACC3 and inhibited tumor growth in xenograft models (PMID: 30301864). 30301864
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR3 Inhibitor Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 inhibited proliferation of bladder cancer cell lines harboring an FGFR3-TACC3 fusion in culture and inhibited tumor growth in FGFR3-TACC3-positive bladder cancer cell line xenograft models (PMID: 25169980). 25169980
FGFR3 - TACC3 bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib FDA approved - On 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 and FGFR3-TACC3 v1 and v3 fusions are included in the companion diagnostic (PMID: 31340094; NCT02365597). detail... 31340094 detail...
FGFR3 - TACC3 urinary bladder cancer no benefit Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3-TACC were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR3 Inhibitor AZ8010 Preclinical Actionable In a preclinical study, AZ12908010 (AZ8010) induced cell cycle arrest and inhibited proliferation of urothelial cancer cell lines that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 22869148, PMID: 23175443). 22869148 23175443
FGFR3 - TACC3 oligodendroglioma sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in tumor regression in patient-derived xenograft models of anaplastic oligodendroglioma harboring FGFR3-TACC3 fusion (PMID: 28978721). 28978721
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR3 Inhibitor Pazopanib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3-TACC3 demonstrated sensitivity to Votrient (pazopanib) in culture (PMID: 23558953). 23558953
FGFR3 - TACC3 urinary bladder cancer predicted - sensitive FGFR3 Inhibitor S-49076 Preclinical Actionable In a preclinical study, S-49076 inhibited autophosphorylation of FGFR3 and downstream signaling in bladder cancer cells that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 23804704, PMID: 23175443). 23175443 23804704
FGFR3 - TACC3 Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited proliferation of transformed cells FGFR3-TACC3 in culture (PMID: 26992226). 26992226
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR Inhibitor (Pan) LY2874455 Preclinical Actionable In a preclinical study, LY2874455 induced tumor regression in bladder cancer xenograft models that have been demonstrated to harbor an FGFR3-TACC3 fusion (PMID: 21900693, PMID: 23175443). 21900693 23175443
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of bladder cancer cell lines that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 24325461, PMID: 23175443). 23175443 24325461
FGFR3 - TACC3 malignant glioma sensitive FGFR3 Inhibitor PD173074 Preclinical - Cell line xenograft Actionable In a preclinical study, PD173074 inhibited Fgfr3 kinase activity and growth in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture and in cell line xenograft models (PMID: 22837387). 22837387
FGFR3 - TACC3 lung adenocarcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Infigratinib (BGJ398) inhibited growth and FGFR3 phosphorylation in cells expressing FGFR3-TACC3 fusion in culture (PMID: 25294908). 25294908
FGFR3 - TACC3 bladder transitional cell papilloma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR3 - TACC3 glioblastoma multiforme predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a Phase I trial, Balversa (erdafitinib) treatment resulted in partial response in a glioblastoma patient harboring FGFR3-TACC3 fusion (PMID: 26324363; NCT01703481). 26324363
FGFR3 - TACC3 glioblastoma multiforme predicted - sensitive FGFR Inhibitor (Pan) Erdafitinib Case Reports/Case Series Actionable In a clinical study, Balversa (erdafitinib) treatment resulted in tumor reduction and stable disease in 2 glioblastoma multiforme patients harboring FGFR3-TACC3 fusion (PMID: 25609060). 25609060
FGFR3 - TACC3 cervical squamous cell carcinoma predicted - sensitive FGFR3 Inhibitor AZD4547 Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with squamous cell carcinoma of the cervix harboring FGFR3-TACC3, with a 40% reduction in target lesion size and a progression-free survival of 4 months (PMID: 32463741; NCT02465060). 32463741
FGFR3 - TACC3 lung non-small cell carcinoma sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Pdx Actionable In a preclinical study, Balversa (erdafitinib) inhibited pERK signaling and tumor growth in a patient-derived xenograft (PDX) model of non-small cell lung cancer harboring FGFR3-TACC3 (PMID: 28341788). 28341788
FGFR3 - TACC3 gallbladder cancer predicted - sensitive FGFR3 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in stable disease in a patient with gallbladder cancer harboring FGFR3-TACC3 (PMID: 30745300; NCT01948297). 30745300
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR3 Inhibitor SU5402 Preclinical Actionable In a preclinical study, SU5402 induced cell-cycle arrest and inhibited proliferation of bladder cancer cells that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 21119661, PMID: 23175443). 21119661 23175443
FGFR3 - TACC3 urinary bladder cancer sensitive PRN1109 Preclinical - Cell line xenograft Actionable In a preclinical study, PRN1109 treatment resulted in tumor regression in bladder cancer cell line xenograft models harboring FGFR3-TACC3 fusion (Eu J Cancer 2014 Vol 50, Suppl 6:157). detail...
FGFR3 - TACC3 transitional cell carcinoma predicted - sensitive FGFR3 Inhibitor Debio 1347 Case Reports/Case Series Actionable In a Phase I trial, Debio 1347 treatment resulted in partial response in two patients with urothelial cancer harboring FGFR3-TACC3 (PMID: 30745300; NCT01948297). 30745300
FGFR3 - TACC3 transitional cell carcinoma sensitive FGFR3 Inhibitor AZD4547 + Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) worked synergistically to induce apoptosis and inhibit growth of a urothelial cell carcinoma cell line harboring FGFR3-TACC3 in culture, and inhibited tumor growth in xenograft models, with increased efficacy over either agent alone (PMID: 28108151). 28108151
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR3 Inhibitor E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, urinary bladder cancer cells harboring FGFR3-TACC3 demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability, and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR3 - TACC3 urinary bladder cancer predicted - sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell line xenograft Actionable In a preclinical study, Infigratinib (BGJ398) treatment inhibited tumor growth and Erk phosphorylation in a cell line xenograft model of bladder cancer harboring FGFR3-TACC3 (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). detail...
FGFR3 - TACC3 urinary bladder cancer sensitive FGFR3 Inhibitor R3Mab Preclinical - Cell line xenograft Actionable In a preclinical study, R3Mab inhibited FGFR3 signaling and tumor growth in bladder cancer cell line xenograft models harboring FGFR3-TACC3 (PMID: 25326231). 25326231
FGFR3 - TACC3 Advanced Solid Tumor sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited proliferation of transformed cells expressing FGFR3-TACC3 in culture (PMID: 26992226). 26992226
FGFR3 - TACC3 Advanced Solid Tumor sensitive FGFR3 Inhibitor AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in 22% (2/9) and stable disease in 55% (5/9) of patients with advanced solid tumors harboring FGFR fusions, with a 6-month progression-free survival rate of 56%, including partial responses in 2 patients and stable disease for greater than 6 months in 1 of 8 patients harboring FGFR3-TACC3 (PMID: 32463741; NCT02465060). 32463741
FGFR3 - TACC3 lung adenocarcinoma sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatanib) inhibited growth and FGFR3 phosphorylation in cells expressing FGFR3-TACC3 fusion in culture (PMID: 25294908). 25294908
FGFR3 - TACC3 malignant glioma sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BJG398) inhibited Fgfr3 kinase activity in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture (PMID: 22837387). 22837387
FGFR3 - TACC3 malignant glioma 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 glioma harboring FGFR3-TACC3 (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). detail...
FGFR3 - TACC3 bladder urothelial carcinoma sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Cell line xenograft Actionable In a preclinical study, PRN1371 inhibited proliferation of bladder transitional cell carcinoma cell lines harboring FGFR3-TACC3 fusion in culture and tumor growth in cell line xenograft models (PMID: 28978721). 28978721
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
FGFR3 P573S lung non-small cell carcinoma no benefit FGFR3 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 FGFR3 P575S (corresponds to P573S in the canonical isoform (PMID: 32669708, NCT02664935). 32669708
FGFR3 S131L head and neck squamous cell carcinoma decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, a head and neck squamous cell carcinoma cell line expressing FGFR3 S131L demonstrated decreased sensitivity to Infigratinib (BGJ398) compared to cells expressing wild-type FGFR3 in culture (PMID: 27053219). 27053219
FGFR3 positive lung squamous cell carcinoma 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 FGFR3-positive lung squamous cell carcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR3 positive lung adenocarcinoma 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 FGFR3-positive lung adenocarcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR3 positive head and neck squamous cell carcinoma 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 a partial remission in a patient with FGFR3-positive head and neck squamous cell carcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR3 positive stomach 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 FGFR3-positive gastric cancer (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR2 pos FGFR3 pos breast carcinoma sensitive FGFR3 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
FGFR3 V555L Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555L demonstrated reduced sensitivity to Infigratinib (BGJ398) in culture (PMID: 28034880). 28034880
FGFR3 V555L transitional cell carcinoma resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical study, two patients with metastatic urothelial carcinoma progressed while being treated with Infigratinib (BGJ398) and subsequent cell-free DNA testing revealed FGFR3 V555L (also corresponds to V443L) (PMID: 29848605). 29848605
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive FGFR3 Inhibitor Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 decreased phosphorylation of ERK and FRS and inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture, and inhibited tumor growth in bladder cancer cell line xenograft models with FGFR3-BAIAP2L1 (PMID: 25589496) 25589496
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive FGFR3 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, Debio 1347 inhibited proliferation of a bladder cancer cell line harboring an FGFR3-BAIAP2L1 fusion in culture (PMID: 25169980). 25169980
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 - BAIAP2L1 Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR3-BAIAP2L1 in culture (PMID: 27627808). 27627808
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive FGFR Inhibitor (Pan) ASP5878 Preclinical - Cell culture Actionable In a preclinical study, ASP5878 treatment inhibited proliferation of a bladder cancer cell line harboring an FGFR3-BAIAP2L1 fusion in culture (Mol Cancer Ther December 2015 14; A170). detail...
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive Cediranib Preclinical - Cell culture Actionable In a preclinical study, Cediranib (AZD-2171) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3-BAIAP2L1 fusion in culture (PMID: 27627808). 27627808
FGFR3 - BAIAP2L1 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 FGFR3-BAIA2PL1 in culture (PMID: 28416604). 28416604
FGFR3 - BAIAP2L1 urinary bladder cancer sensitive FGFR3 Inhibitor PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 D788N head and neck squamous cell carcinoma no benefit FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D788N in culture, however, cells expressing FGFR3 D788N did not demonstrate increased sensitivity to Infigratinib (BGJ398) compared to cells expressing wild-type FGFR3 (PMID: 27053219). 27053219
FGFR3 V555M Advanced Solid Tumor resistant FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to AZD4547 in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). 28034880
FGFR3 V555M transitional cell carcinoma resistant FGFR Inhibitor (Pan) Infigratinib Case Reports/Case Series Actionable In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with Infigratinib (BGJ398) and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) (PMID: 29848605). 29848605
FGFR3 V555M Advanced Solid Tumor resistant FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to Infigratinib (BGJ398) in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor decreased response FGFR3 Inhibitor Debio 1347 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) LY2874455 Preclinical - Cell culture Actionable In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). 28034880
FGFR3 V555M Advanced Solid Tumor decreased response FGFR Inhibitor (Pan) FIIN-2 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M demonstrated reduced sensitivity to FIIN-2 in culture (PMID: 28034880). 28034880
FGFR3 F386L myeloid neoplasm sensitive FGFR3 Inhibitor Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 F386L in culture (PMID: 25169980). 25169980
FGFR3 amp urinary system cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Infigratinib (BGJ398) decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). 27401245
FGFR3 amp urinary system cancer sensitive FGFR3 Inhibitor AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). 27401245
FGFR3 amp lung non-small cell carcinoma sensitive FGFR Inhibitor (Pan) PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 28.2% tumor growth inhibition in patient-derived xenograft models of FGFR3-amplified non-small cell lung cancer (PMID: 28978721). 28978721
FGFR3 amp Advanced Solid Tumor predicted - sensitive FGFR3 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
FGFR3 amp Advanced Solid Tumor predicted - sensitive FGFR Inhibitor (Pan) Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of several tumor cell lines with FGFR alterations in culture (Cancer Res April 15, 2011 71:3560). detail...
ROS1 fusion ERBB2 amp FGFR3 amp RET amp lung non-small cell carcinoma predicted - resistant Crizotinib Case Reports/Case Series Actionable In a clinical study, a non-small cell lung carcinoma patient harboring a ROS1 fusion treated with Xalkori (crizotinib) responded, but eventually progressed, and was subsequently found to harbor presumed resistance alterations, including amplification of ERBB2 (HER2), FGFR3, and RET (PMID: 29636358). 29636358
Clinical Trial Phase Therapies Title Recruitment Status