Molecular Profile Detail

Profile Name FGFR1 positive
Gene Variant Detail

FGFR1 positive (unknown)

Relevant Treatment Approaches

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR1 over exp head and neck squamous cell carcinoma sensitive BGJ398 Preclinical Actionable In a preclinical study, BGJ398 inhibited cell growth and induced apoptosis in HNSCC cells over expressing Fgfr1 in culture and in xenograft models (PMID: 26015511). 26015511
FGFR1 over exp Advanced Solid Tumor sensitive PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing wild-type FGFR1 in culture (PMID: 28978721). 28978721
FGFR1 over exp uterus leiomyosarcoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 over exp uterus leiomyosarcoma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 over exp thyroid cancer sensitive Lenvatinib Preclinical Actionable In a preclinical study, Lenvima (lenvatinib) inhibited FGFR1 phosphorylation and signaling in thyroid cancer cells overexpressing FGFR1 (PMID: 25295214). 25295214
FGFR1 over exp renal cell carcinoma not applicable Sorafenib Phase II Emerging In a clinical analysis of a Phase II trial, high Fgfr1 expression level was associated with decreased progression free survival in renal cell carcinoma patients treated with Nexavar (sorafenib) (PMID: 25900027). 25900027
FGFR1 over exp uterus leiomyosarcoma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 over exp Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr1 in culture (PMID: 27627808). 27627808
FGFR1 amp MET dec exp lung cancer sensitive Rogaratinib Preclinical - Cell culture Actionable In a preclinical study, Rogaratinib (BAY 1163877) inhibited Erk signaling and proliferation of FGFR1-amplified lung cancer cell lines with undetectable Met expression in culture (PMID: 27429073). 27429073
FGFR1 amp MET dec exp lung cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Erk signaling and proliferation of FGFR1-amplified lung cancer cell lines with undetectable Met expression in culture (PMID: 27429073). 27429073
FGFR1 amp KRAS G12V non-small cell lung carcinoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, overexpression of KRAS G12V in FGFR1-amplified non-small cell lung carcinoma cells resulted in decreased response to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp KRAS G12V lung cancer resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, a lung cancer cell line harboring FGFR1 amplification and KRAS G13C demonstrated insensitivity to Erdafitinib (JNJ-42756493) in culture (PMID: 28341788). 28341788
FGFR1 amp KRAS G12V non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling, resulting in growth inhibition in FGFR1-amplified non-small cell lung carcinoma cells overexpressing KRAS G12V in culture (PMID: 28630215). 28630215
FGFR1 amp MET amp lung cancer sensitive AZD4547 + Crizotinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Xalkori (crizotinib) synergistically inhibited proliferation of FGFR1 amplified lung cancer cells that acquired resistance to AZD4547 through MET amplification in culture (PMID: 27429073). 27429073
FGFR1 amp MET amp lung squamous cell carcinoma predicted - resistant BGJ398 Phase I Actionable In a Phase I trial, MET amplification was detected in a squamous cell lung cancer patient harboring FGFR1 amplification whose disease relapsed after 17 months of BGJ398 treatment, supporting a role of MET amplification in drug resistance in FGFR1-amplified lung cancer (PMID: 28630215). 28630215
FGFR1 amp MET amp lung cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, MET amplification was identified as the mechanism mediating acquired AZD4547 resistance in a FGFR1 amplified lung cancer cell line in culture (PMID: 27429073). 27429073
EML4-ALK FGFR1 amp non-small cell lung carcinoma predicted - resistant Brigatinib Clinical Study Actionable In a clinical study, a non-small cell lung carcinoma patient harboring EML4-ALK treated with Alunbrig (brigatinib) responded, but eventually progressed, and was subsequently found to harbor a presumed resistance alteration, FGFR1 amplification (PMID: 29636358). 29636358
AKT1 S266L FGFR1 amp lung cancer predicted - resistant PD173074 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification demonstrated resistance to increasing concentrations of PD173074 in culture and was subsequently, found to have acquired AKT1 S266L (PMID: 30140389). 30140389
AKT1 S266L FGFR1 amp lung cancer predicted - sensitive GSK2141795 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification and AKT1 S266L demonstrated sensitivity to Uprosertib (GSK2141795) in culture, showing decreased phosphorylation of Akt1 targets and reduced cell growth (PMID: 30140389). 30140389
FGFR1 amp synovial sarcoma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 amp lung squamous cell carcinoma sensitive AZD4547 + BKM120 Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a squamous cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151). 28108151
FGFR1 amp lung squamous cell carcinoma no benefit Dovitinib Phase II Actionable In a Phase II clinical trial, dovitinib treatment resulted in a objective response rate of 11.5% (3/26, all partial responses) and disease control rate of 50% (13/26), and a median progression-free survival of 2.9 months in lung squamous cell carcinoma patients with FGFR1 amplification, and FGFR1 amplification was not determined to be a predictive biomarker for sensitivity (PMID: 27315356). 27315356
FGFR1 amp non-small cell lung carcinoma sensitive Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of non-small cell lung cancer cell lines harboring FGFR1 amplification in culture (PMID: 25169980). 25169980
FGFR1 amp estrogen-receptor positive breast cancer sensitive Lucitanib Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification demonstrated sensitivity to treatment with Lucitanib (E-3810) in culture (PMID: 27126994). 27126994
FGFR1 amp non-small cell lung carcinoma predicted - sensitive NGI-1 Preclinical - Cell culture Actionable In a preclinical study, NGI-1 inhibited FGFR1 phosphorylation and proliferation of a FGFR1-amplified cell line dependent on FGFR1 signaling in culture, however, did not inhibit proliferation of an FGFR1-amplified cell line not dependent on FGFR1 signaling (PMID: 27694802). 27694802
FGFR1 amp synovial sarcoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 amp Ewing sarcoma predicted - sensitive Ponatinib Preclinical - Cell culture Actionable In a preclinical study, Iclusig (ponatinib) inhibited proliferation of Ewing’s sarcoma cell lines with FGFR1 copy number gain in culture (PMID: 26179511). 26179511
FGFR1 amp lung small cell carcinoma sensitive AZD4547 + BKM120 Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a small cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151). 28108151
FGFR1 amp lung small cell carcinoma sensitive Cisplatin + Etoposide + GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, addition of GSK3052230 (FP-1039) to Platinol (cisplatin) and Vepesid (etoposide) resulted in improved tumor growth inhibition in cell line xenograft models of FGFR1 amplified lung small cell carcinoma (PMID: 23536011). 23536011
FGFR1 amp adrenocortical carcinoma sensitive Derazantinib Phase I Actionable In a Phase I trial, ARQ 087 treatment resulted in stable disease with a tumor reduction of 20% in an adrenocortical carcinoma patient harboring FGFR1 amplification, who remained on study for 3.5 years (PMID: 28972963; NCT01752920). 28972963
FGFR1 amp non-small cell lung carcinoma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215). 28630215
FGFR1 amp breast cancer no benefit AZD4547 Phase II Actionable In a Phase II clinical trial, treatment with AZD4547 resulted in a response rate of 12.5% (1/8) in patients with FGFR1-amplified breast cancer, and did not meet the predetermined criteria for efficacy (PMID: 27179038). 27179038
FGFR1 amp lung large cell carcinoma sensitive ODM-203 Preclinical - Cell line xenograft Actionable In a preclinical study, ODM-203 inhibited FGFR signaling and proliferation in a large cell lung cancer cell line with amplification of chromosome 8p12 leading to increased FGFR1 copy number, and inhibited tumor growth in xenograft models (PMID: 30301864). 30301864
FGFR1 amp lung carcinoma sensitive Lucitanib Preclinical - Cell line xenograft Actionable in a preclinical study, Lucitanib (E-3810) preferentially inhibited growth of FGFR1-amplified lung carcinoma cell lines in culture and in cell line xenograft models (PMID: 27988457). 27988457
FGFR1 amp Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 59% (10/17) of patients with advanced solid tumors harboring FGFR amplification, with a 6-month progression-free survival rate of 15% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 amp lung squamous cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR1 amp lung squamous cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR1 amp non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215). 28630215
FGFR1 amp estrogen-receptor positive breast cancer sensitive Cediranib Preclinical Actionable In a preclinical study, Cediranib (AZD-2171) inhibited growth of estrogen receptor (ER)-positive breast cancer cells with FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp lung small cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR1 amp synovial sarcoma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 amp lung adenocarcinoma sensitive PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 64.6% tumor growth inhibition in patient-derived xenograft models of FGFR1-amplified lung adenocarcinoma (PMID: 28978721). 28978721
FGFR1 amp lung small cell carcinoma sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, a small cell lung cancer cell line harboring FGFR1 amplification demonstrated sensitivity to E7090, resulting in decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR1 amp lung cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of lung cancer cells with FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp non-small cell lung carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR1 amp non-small cell lung carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR1 amp non-small cell lung carcinoma sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a non-small cell lung cancer cell line, harboring FGFR1 amplification, treated with E7090 demonstrated decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR1 amp transitional cell carcinoma sensitive AZD4547 + BKM120 Preclinical - Cell culture 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 with FGFR1 amplification in culture, with increased efficacy over either agent alone (PMID: 28108151). 28108151
FGFR1 amp breast cancer sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in ER-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp estrogen-receptor positive breast cancer no benefit Brivanib Preclinical Actionable In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of estrogen receptor (ER)-positive breast cancer cells with FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp non-small cell lung carcinoma sensitive AZD4547 Preclinical - Pdx Actionable In a preclinical study, AZD4547 inhibited FGFR1 signaling and resulted in tumor regression in patient-derived xenograft models of non-small cell lung carcinoma harboring FGFR1 amplification, wild-type for EGFR, K-Ras and negative for EML4-ALK fusion (PMID: 23082000). 23082000
FGFR1 amp lung cancer sensitive GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK3052230 (FP-1039) treatment resulted in greater tumor growth inhibition (56% vs 22%) in cell line xenograft models of FGFR1 amplified lung cancer compared to FGFR1 non-amplified models (PMID: 23536011). 23536011
FGFR1 amp estrogen-receptor positive breast cancer resistant Alpelisib Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring an FGFR1 amplification demonstrated resistance to Alpelisib (BYL719) in culture (PMID: 27126994). 27126994
FGFR1 amp estrogen-receptor positive breast cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in estrogen receptor (ER)-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp lung small cell carcinoma sensitive GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK3052230 (FP-1039) treatment inhibited growth of FGFR1 amplified lung small cell carcinoma cell lines in culture and in cell line xenograft models (PMID: 23536011). 23536011
FGFR1 amp estrogen-receptor positive breast cancer sensitive Nintedanib Preclinical Actionable In a preclinical study, Ofev (nintedanib) inhibited the growth of ER-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR1 amp lung squamous cell carcinoma no benefit AZD4547 Phase I Actionable In a Phase Ib trial, AZD4547 demonstrated limited efficacy in patients with squamous cell lung cancer with FGFR1 amplification, resulting in an overall response rate of 8% (1/15) and a median overall survival of 4.9 months (PMID: 28615371; NCT00979134). 28615371
FGFR1 amp lung large cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a large cell lung cancer cell line harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR1 amp lung cancer sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of lung cancer cell lines harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR1 amp Her2-receptor positive breast cancer sensitive Dovitinib Phase I Actionable In a Phase I trial, Dovitinib (TKI258) promoted 6-month stable disease in Erbb2 (Her2)-positive breast cancer patients with FGFR1 amplification (PMID: 23658459). 23658459
FGFR1 amp estrogen-receptor positive breast cancer sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification (PMID: 7506125) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 7506125 27535969
FGFR1 amp lung squamous cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR1 amp non-small cell lung carcinoma sensitive PRN1371 Preclinical - Pdx Actionable In a preclinical study, PRN1371 treatment resulted in 96.1% tumor growth inhibition in patient-derived xenograft models of FGFR1-amplified non-small cell lung cancer (PMID: 28978721). 28978721
FGFR1 amp non-small cell lung carcinoma sensitive GSK3052230 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK3052230 (FP-1039) treatment inhibited growth of FGFR1 amplified non-small cell lung carcinoma cell lines in culture and in cell line xenograft models (PMID: 23536011). 23536011
FGFR1 amp Her2-receptor negative breast cancer sensitive Pazopanib Clinical Study Actionable In a clinical case study, a patient with ERBB2 (HER2)-receptor negative breast cancer harboring FGFR1 amplification demonstrated antitumor activity when treated with Votrient (pazopanib), including a near complete loss of brain lesions and improved function of the liver (PMID: 29223982). 29223982
FGFR1 amp lung squamous cell carcinoma sensitive BGJ398 Phase I Actionable In a Phase I trial, patients with lung squamous cell carcinoma harboring an FGFR1 amplification demonstrated a disease control rate of 50% (18/36) when treated with BGJ398, resulting in 14 patients with stable disease and 4 patients with a partial response (PMID: 27870574). 27870574
FGFR1 amp lung small cell carcinoma sensitive Debio 1347 Preclinical Actionable In a preclinical study, Debio 1347 inhibited proliferation of small cell lung cancer cell lines harboring FGFR1 amplification in culture (PMID: 25169980). 25169980
FGFR1 amp lung cancer sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, lung cancer cells harboring FGFR1 amplification were sensitive to PD173074 treatment in culture, demonstrating inhibition of cell growth (PMID: 30140389). 30140389
FGFR1 amp lung small cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR1 amp breast cancer sensitive BGJ398 Phase I Actionable In a Phase I trial, 28% (9/32) of breast cancer patients harboring FGFR1 amplification demonstrated stable disease when treated with BGJ398 (PMID: 27870574). 27870574
FGFR1 amp non-small cell lung carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR1 amp lung cancer predicted - sensitive Erdafitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Erdafitinib (JNJ-42756493) inhibited FGFR downstream signaling and proliferation of several lung cancer cell lines with FGFR1 amplification in culture, and inhibited tumor growth in an FGFR1-amplified lung cancer cell line xenograft model (PMID: 28341788). 28341788
FGFR1 amp lung small cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a small cell lung cancer cell line harboring FGFR1 amplification in culture (PMID: 23082000). 23082000
FGFR1 amp lung squamous cell carcinoma sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited growth of squamous cell lung cancer cell lines harboring FGFR1 amplification (PMID: 22238366). 22238366
FGFR1 amp NRAS amp non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling, resulting in growth inhibition in non-small cell lung carcinoma cells harboring both FGFR1 and NRAS amplification in culture (PMID: 28630215). 28630215
FGFR1 amp NRAS amp non-small cell lung carcinoma resistant Trametinib Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung carcinoma cells harboring both FGFR1 and NRAS amplification were resistant to Mekinist (trametinib) in culture (PMID: 28630215). 28630215
FGFR1 amp NRAS amp non-small cell lung carcinoma resistant BGJ398 Preclinical - Cell culture Actionable In a preclinical study, amplification of NRAS was identified in a non-small cell lung cancer cell line harboring FGFR1 amplification that acquired resistance to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp MET pos lung cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, FGFR1-amplified lung cancer cell lines with Met expression were resistant to AZD4547 in culture (PMID: 27429073). 27429073
FGFR1 amp MET pos lung cancer resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, FGFR1-amplified lung cancer cell lines with Met expression were resistant to Rogaratinib (BAY 1163877) in culture (PMID: 27429073). 27429073
FGFR1 amp MET over exp lung cancer sensitive Crizotinib + Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Rogaratinib (BAY 1163877) and Xalkori (crizotinib) synergistically inhibited proliferation of FGFR1 amplified lung cancer cells that acquired resistance to Rogaratinib (BAY 1163877) through MET overexpression and activation in culture (PMID: 27429073). 27429073
FGFR1 amp MET over exp lung small cell carcinoma resistant BGJ398 Preclinical - Cell culture Actionable In a preclinical study, overexpression and activation of Met was identified in a small cell lung cancer cell line harboring FGFR1 amplification that acquired resistance to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp MET over exp lung small cell carcinoma sensitive BGJ398 + Crizotinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Xalkori (crizotinib) synergistically inhibited Erk signaling, resulted in growth inhibition in small cell lung carcinoma cells harboring FGFR1 amplification and Met overexpression in culture (PMID: 28630215). 28630215
FGFR1 amp MET over exp lung small cell carcinoma sensitive BGJ398 + EMD 1214063 Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and EMD 1214063 synergistically inhibited growth of small cell lung carcinoma cells harboring FGFR1 amplification and Met overexpression in culture (PMID: 28630215). 28630215
FGFR1 amp MET over exp lung cancer resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, MET overexpression and activation was identified as the mechanism mediating acquired Rogaratinib (BAY 1163877) resistance in a FGFR1 amplified lung cancer cell line in culture (PMID: 27429073). 27429073
FGFR1 amp FGFR2 amp breast cancer sensitive 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
FGFR1 amp KRAS amp lung cancer resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, a lung cancer cell line with co-amplification of FGFR1 and KRAS demonstrated insensitivity to Erdafitinib (JNJ-42756493) in culture (PMID: 28341788). 28341788
FGFR1 amp NRAS over exp non-small cell lung carcinoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, overexpression of Nras in FGFR1-amplified non-small cell lung carcinoma cells resulted in decreased response to BGJ398 in culture (PMID: 28630215). 28630215
FGFR1 amp NRAS over exp non-small cell lung carcinoma sensitive BGJ398 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, BGJ398 and Mekinist (trametinib) combination treatment inhibited Erk signaling, resulting in growth inhibition in FGFR1-amplified non-small cell lung carcinoma cells overexpressing Nras in culture (PMID: 28630215). 28630215
FGFR1 act mut Advanced Solid Tumor sensitive Erdafitinib Phase I Actionable In a Phase I trial, Erdafitinib (JNJ-42756493) 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). 26324363
FGFR1 act mut Advanced Solid Tumor sensitive Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor decreased response Cediranib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR1 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
FGFR1 act mut Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). 22238366
FGFR1 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 FGFR1 in culture (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor decreased response Nintedanib Preclinical Actionable In a preclinical study, transformed cells expressing constitutively active FGFR1 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor sensitive Debio 1347 Phase I Actionable In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR1 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). detail...
FGFR1 act mut breast cancer sensitive FIIN-01 Preclinical Actionable In a preclinical study, FIIN-01 inhibited Fgfr1 activation-induced proliferation and transformation of human breast epithelial cell lines in culture (PMID: 20338520). 20338520
FGFR1 wild-type lung cancer decreased response AZD4547 Preclinical Actionable In a preclinical study, FGFR1 non-amplified lung cancer cell lines demonstrated reduced sensitivity to AZD4547 induced growth inhibition in culture and in xenograft models (PMID: 23082000). 23082000
FGFR1 wild-type breast cancer resistant Ponatinib Preclinical Actionable In a preclinical study, ER-positive breast cancer cells with wild-type FGFR1 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). 22238366
FGFR1 dec exp KRAS wild-type lung cancer no benefit Trametinib Preclinical Actionable In a preclinical study, knocking down of Fgfr1 through shRNA did not sensitize KRAS wild-type lung cancer cells to Mekinist (trametinib) induced growth inhibition in culture (PMID: 27338794). 27338794
FGFR1 dec exp KRAS mut pancreatic cancer sensitive Trametinib Preclinical - Cell culture Actionable In a preclinical study, Mekinist (trametinib) treatment demonstrated enhanced growth inhibition of KRAS mutant pancreatic cancer cells with decreased Fgfr1 expression through shRNA knockdown in culture (PMID: 27338794). 27338794
FGFR1 dec exp KRAS mut colorectal cancer no benefit Trametinib Preclinical - Cell culture Actionable In a preclinical study, knocking down of Fgfr1 through shRNA did not sensitize KRAS mutant colorectal cancer cells to Mekinist (trametinib) induced growth inhibition in culture (PMID: 27338794). 27338794
FGFR1 dec exp KRAS mut lung cancer sensitive Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, Mekinist (trametinib) treatment demonstrated enhanced growth inhibition in KRAS mutant lung cancer cells with decreased Fgfr1 expression through shRNA knockdown in culture, and tumor regression in xenograft models (PMID: 27338794). 27338794
FGFR1 V561M Advanced Solid Tumor sensitive PRN1371 Preclinical - Cell culture Actionable In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR1 V561M in culture (PMID: 28978721). 28978721
FGFR1 V561M non-small cell lung carcinoma resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung cancer cells expressing FGFR1 V561M demonstrated resistance to AZD4547 in culture (PMID: 30257990). 30257990
FGFR1 V561M Advanced Solid Tumor sensitive FIIN-01 Preclinical Actionable In a preclinical study, FIIN-01 inhibited Fgfr1 autophosphorylation in a human transformed embryonic kidney cell line harboring FGFR1 V561M mutation in culture (PMID: 20338520). 20338520
EML4-ALK CDKN2A del FGFR1 T141R SMAD4 Q83* pancreatic ductal adenocarcinoma predicted - sensitive Alectinib Clinical Study Actionable In a clinical case study, a pancreatic ductal adenocarcinoma patient harboring EML4-ALK along with CDKN2A deletion, FGFR1 T141R, SMAD4 Q83*, and a TP53 splice site mutation, experienced disease progression after 2 months of Xalkori (crizotinib) treatment, then received Alecensa (alectinib) and remained on treatment for at least 3 months (PMID: 28476735). 28476735
EML4-ALK CDKN2A del FGFR1 T141R SMAD4 Q83* pancreatic ductal adenocarcinoma resistant Crizotinib Clinical Study Actionable In a clinical case study, a pancreatic ductal adenocarcinoma patient harboring EML4-ALK along with CDKN2A deletion, FGFR1 T141R, SMAD4 Q83*, and a TP53 splice site mutation, experienced disease progression after 2 months of Xalkori (crizotinib) treatment, then received Alecensa (alectinib) and remained on treatment for at least 3 months (PMID: 28476735). 28476735
FGFR1-TACC1 malignant glioma sensitive PD173074 Preclinical - Cell culture Actionable In a preclinical study, PD173074 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR1-TACC1 malignant glioma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR1-TACC1 malignant glioma sensitive BGJ398 Preclinical - Cell culture Actionable In a preclinical study, BJG398 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR1 rearrange myeloproliferative neoplasm sensitive Dovitinib Preclinical Actionable In a preclinical study, primary cells from 8p11 myeloproliferative syndrome patients harboring FGFR1 rearrangement were sensitive to Dovitinib (TKI258)-induced growth inhibition in culture (PMID: 17698633). 17698633
FGFR1 rearrange leukemia sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of leukemia cells harboring FGFR1 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
FGFR1 rearrange lung small cell carcinoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of small cell lung cancer cells harboring FGFR1 translocation in culture (PMID: 27550940). 27550940
FGFR1 positive uterus leiomyosarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 positive salivary gland adenoid cystic carcinoma predicted - sensitive 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 FGFR1-positive adenoid cystic carcinoma of the tongue (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR1 positive leiomyosarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 positive leiomyosarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR1 positive lung adenocarcinoma sensitive AZD4547 + Vistusertib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 and Vistusertib (AZD2014) synergistically inhibited survival of FGFR1-dependent lung adenocarcinoma cells in culture and in cell line xenograft models (PMID: 26359452). 26359452
FGFR1 positive lung large cell carcinoma sensitive AZD4547 + Vistusertib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 and Vistusertib (AZD2014) synergistically inhibited survival of FGFR1-dependent lung large cell carcinoma cells in culture and in cell line xenograft models (PMID: 26359452). 26359452
FGFR1 positive synovial sarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 positive lung large cell carcinoma sensitive AZD4547 + Sirolimus Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Rapamune (sirolimus) synergistically inhibited survival of FGFR1-dependent lung large cell carcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive head and neck squamous cell carcinoma sensitive AZD4547 + Vistusertib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Vistusertib (AZD2014) synergistically inhibited survival of FGFR1-dependent head and neck squamous cell carcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive lung adenocarcinoma sensitive AZD4547 + Sirolimus Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and Rapamune (sirolimus) synergistically inhibited survival of FGFR1-dependent lung adenocarcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive lung large cell carcinoma sensitive AZD4547 + AZD8055 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and AZD8055 synergistically inhibited survival of FGFR1-dependent lung large cell carcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 positive synovial sarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR1 positive uterus leiomyosarcoma decreased response PD173074 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to PD173074 in culture (PMID: 27535980). 27535980
FGFR1 positive leiomyosarcoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to BGJ398 in culture (PMID: 27535980). 27535980
FGFR1 positive hemangioma predicted - sensitive 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 with resolution of edema in a patient with FGFR1-positive hemangioendothelioma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). detail...
FGFR1 positive uterus leiomyosarcoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to BGJ398 in culture (PMID: 27535980). 27535980
FGFR1 positive synovial sarcoma decreased response BGJ398 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to BGJ398 in culture (PMID: 27535980). 27535980
FGFR1 positive lung adenocarcinoma sensitive AZD4547 + AZD8055 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 and AZD8055 synergistically inhibited survival of FGFR1-dependent lung adenocarcinoma cells in culture (PMID: 26359452). 26359452
FGFR1 pos FGFR2 pos hepatocellular carcinoma sensitive 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
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 mutant Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 40% (6/16) of patients with advanced solid tumors harboring FGFR single nucleotide variants, with a 6-month progression-free survival rate of 8% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 mutant transitional cell carcinoma predicted - sensitive Erdafitinib Phase II Actionable In a Phase II trial, Erdafitinib (JNJ-42756493) treatment resulted in an objective response rate of 42% (40/96, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations (J Clin Oncol 36, 2018 (suppl; abstr 4503); NCT02365597). detail...
FGFR1 mutant Advanced Solid Tumor sensitive 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 INCB054828 in culture and in cell line xenograft models, resulting in inhibition of tumor growth (Cancer Res 2015;75(15 Suppl):Abstract nr 771). detail...
FGFR1 fusion Advanced Solid Tumor predicted - sensitive 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 42% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 fusion Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited Erk, Stat5 signaling and survival of transformed cell lines overexpressing FGFR1 fusion proteins (ZMYM2-FGFR1 or BCR-FGFR1) in culture (PMID: 17698633). 17698633
FGFR1 fusion acute myeloid leukemia sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) increased apoptosis and inhibited survival of acute myelogenous leukemia cell lines harboring FGFR1OP2-FGFR1 fusion in culture (PMID: 17698633). 17698633
FGFR1 fusion hematologic cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of hematologic cancer cells harboring FGFROP2-FGFR1 fusion in culture (PMID: 27627808). 27627808
Clinical Trial Phase Therapies Title Recruitment Status