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| Gene | FGFR1 |
| Variant | amp |
| Impact List | none |
| Protein Effect | no effect |
| Gene Variant Descriptions | FGFR1 amplification indicates an increased number of copies of the FGFR1 gene. However, the mechanism causing the increase is unspecified. |
| Associated Drug Resistance |
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 | 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 | 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 | Advanced Solid Tumor | predicted - sensitive | Futibatinib | Phase I | Actionable | In a Phase I trial (FOENIX-101), Lytgobi (futibatinib) treatment demonstrated manageable safety profile, and resulted in a partial response in 6% (5/86) and stable disease in 48% (41/86) of patients with advanced solid tumors harboring FGF/FGFR aberrations, among whom 20% (15/74) harbored FGFR1 amplification (PMID: 32622884; NCT02052778). | 32622884 |
| 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 | breast cancer | predicted - sensitive | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lytgobi (futibatinib) treatment led to inhibition of cell proliferation in a breast cancer cell line harboring FGFR1 amplification in culture (PMID: 32973082). | 32973082 |
| 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 non-small cell 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 | 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 | Her2-receptor positive breast cancer | sensitive | Dovitinib | Phase II | Actionable | In a Phase II trial, Dovitinib (TKI258) promoted 6-month stable disease in Erbb2 (Her2)-positive breast cancer patients with FGFR1 amplification (PMID: 23658459). | 23658459 |
| 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 | lung non-small cell 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 | lung non-small cell carcinoma | sensitive | eFT226 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, eFT226 inhibited tumor growth in a cell line xenograft model of FGFR1-amplified non-small cell lung cancer (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133). | detail... |
| FGFR1 amp | lung non-small cell carcinoma | sensitive | Infigratinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) 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 | 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 | 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 | lung small cell carcinoma | sensitive | AZD4547 + Buparlisib | 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 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 | lung non-small cell 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 | transitional cell carcinoma | sensitive | AZD4547 + Buparlisib | 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 | 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 | 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 | 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 | triple-receptor negative breast cancer | predicted - sensitive | Lucitanib | Preclinical - Pdx | Actionable | In a preclinical study, Lucitanib (E-3810) treatment resulted in reduced tumor volume in FGFR1-amplified triple-negative breast cancer patient-derived xenograft (PDX) models (PMID: 34593528). | 34593528 |
| FGFR1 amp | lung non-small cell 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 | lung non-small cell carcinoma | sensitive | CPL304110 | Preclinical - Cell culture | Actionable | In a preclinical study, CPL304110 treatment inhibited proliferation of a non-small cell lung cancer cell line harboring FGFR1 amplification in culture (PMID: 33199155). | 33199155 |
| 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 non-small cell 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 | 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 non-small cell 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 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 | head and neck carcinoma | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase I trial, a patient with head and neck carcinoma harboring an FGFR1 amplification demonstrated a reduction in tumor size when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
| 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 | triple-receptor negative breast cancer | no benefit | Rogaratinib | Preclinical - Pdx | Actionable | In a preclinical study, Rogaratinib (BAY 1163877) treatment did not inhibit tumor growth in a patient-derived xenograft (PDX) model of triple-negative breast cancer with FGFR1 amplification (PMID: 34593528). | 34593528 |
| FGFR1 amp | lung squamous cell carcinoma | predicted - sensitive | Carboplatin + GSK3052230 + Paclitaxel | Phase I | Actionable | In a Phase Ib trial, the combination therapy of GSK3052230 (FP-1039), Taxol (paclitaxel), and Paraplatin (carboplatin) demonstrated safety and was well-tolerable, and resulted in an overall response rate of 47% (9/19), with 9 patients achieving a partial response, and a progression-free survival of 5.5 months in patients with stage IV or recurrent metastatic squamous non-small cell lung cancer harboring FGFR1 amplification (PMID: 31446228; NCT01868022). | 31446228 |
| 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 | lung squamous cell carcinoma | predicted - sensitive | Debio 1347 | Case Reports/Case Series | Actionable | In a Phase I trial, Debio 1347 treatment resulted in a stable disease with 26.7% reduction of tumor size and 100% decrease of DUSP6 score in a patient with lung squamous cell carcinoma harboring FGFR1 amplification (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR1 amp | lung non-small cell carcinoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215). | 28630215 |
| 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 | 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 | Her2-receptor negative breast cancer | predicted - sensitive | Pazopanib | Case Reports/Case Series | 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 | Advanced Solid Tumor | predicted - sensitive | HQP1351 | Preclinical - Cell culture | Actionable | In a preclinical study, GZD824 (HQP1351) treatment inhibited cell growth, Fgfr1 phosphorylation, and downstream pathway signaling in cell lines with FGFR1 amplification in culture (PMID: 34114373). | 34114373 |
| FGFR1 amp | lung squamous cell carcinoma | sensitive | Infigratinib | 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 Truseltiq (infigratinib), resulting in 14 patients with stable disease and 4 patients with a partial response (PMID: 27870574). | 27870574 |
| FGFR1 amp | synovial sarcoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited survival of FGFR1-amplified synovial sarcoma cells in culture (PMID: 27535980). | 27535980 |
| FGFR1 amp | Advanced Solid Tumor | unknown | AZD4547 | Phase II | Actionable | In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 7 of 17 patients with advanced solid tumors harboring FGFR1 amplification, with 6 of the 17 patients experiencing progressive disease and 4 not evaluable for response, and a 6-month progression-free survival rate of 0% (PMID: 32463741; NCT02465060). | 32463741 |
| 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 | lung squamous cell carcinoma | sensitive | AZD4547 + Buparlisib | 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 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 | 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 | 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 | 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 | 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 | Advanced Solid Tumor | predicted - sensitive | 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 |
| FGFR1 amp | lung cancer | predicted - sensitive | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Lytgobi (futibatinib) treatment led to inhibition of cell proliferation in lung cancer cell lines harboring FGFR1 amplification in culture, and led to inhibition of tumor growth in a cell line xenograft model with a daily dosing regimen, but not with an intermittent dosing regimen (PMID: 32973082). | 32973082 |
| FGFR1 amp | breast cancer | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, 28% (9/32) of breast cancer patients harboring FGFR1 amplification demonstrated stable disease when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
| FGFR1 amp | lung non-small cell 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 | 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 | lung non-small cell 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 | 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 | predicted - sensitive | Erdafitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Balversa (erdafitinib) 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 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 | 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 | Her2-receptor negative breast cancer | predicted - sensitive | Lucitanib | Phase II | Actionable | In a Phase II (FINESSE) trial, Lucitanib (E-3810) treatment resulted in an objective response rate (ORR) of 19% (6/32) and a clinical benefit rate of 41% (13/32) in patients with metastatic hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring FGFR1 amplification, ORR was improved (22%, 5/23 vs 9%, 5/53) in patients with high level FGFR1 amplification (FGFR1/centromere ratio>=4) compared to those without (PMID: 31619444; NCT02053636). | 31619444 |
| FGFR1 amp | breast cancer | predicted - sensitive | Sunitinib | Phase II | Actionable | In a Phase II trial, Sutent (sunitinib) treatment demonstrated antitumor activity in metastatic breast cancer patients with FGFR1 amplification (n = 28), FGFR1 mutation (n = 1), or both (n = 1), and led to an objective response rate of 7% (2/30, including 2 partial responses), stable disease greater than 16 weeks in 5 patients, and a disease control rate of 29% (Cancer Res 2021;81(13_Suppl):Abstract nr CT173). | detail... |
| 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 | lung non-small cell 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 | 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 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 | 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 | 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 | uterine carcinosarcoma | predicted - sensitive | Pazopanib | Case Reports/Case Series | Actionable | In a clinical case study, Votrient (pazopanib) treatment resulted in disease control for approximately 7 months in a patient with refractory uterine carcinosarcoma with FGFR1 amplification (PMID: 35586703). | 35586703 |
| 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 FGFR2 amp | breast cancer | sensitive | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Lytgobi (futibatinib) treatment led to inhibition of cell proliferation in breast cancer cell lines harboring FGFR1 and FGFR2 amplification in culture, and led to inhibition of tumor growth in a cell line xenograft model (PMID: 32973082). | 32973082 |
| FGFR1 amp FGFR2 amp | breast cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line with FGFR1 and FGFR2 amplification was sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth in culture (PMID: 33563752). | 33563752 |
| FGFR1 amp NRAS amp | lung non-small cell carcinoma | sensitive | Infigratinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) 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 | lung non-small cell carcinoma | resistant | Infigratinib | 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 Truseltiq (infigratinib) in culture (PMID: 28630215). | 28630215 |
| FGFR1 amp NRAS amp | lung non-small cell 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 over exp | lung non-small cell carcinoma | sensitive | Infigratinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) 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 amp NRAS over exp | lung non-small cell carcinoma | decreased response | Infigratinib | 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 Truseltiq (infigratinib) in culture (PMID: 28630215). | 28630215 |
| EML4 - ALK FGFR1 amp | lung non-small cell carcinoma | predicted - resistant | Brigatinib | Case Reports/Case Series | 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 |
| FGFR2 fusion FGFR1 amp | colon cancer | predicted - sensitive | Debio 1347 | Case Reports/Case Series | Actionable | In a Phase I trial, Debio 1347 treatment resulted in a partial response with 49.5% reduction of tumor size and 66% decrease of DUSP6 score in a patient with colon cancer harboring FGFR1 amplification and FGFR2 fusion (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR1 amp FGFR1 over exp | lung cancer | sensitive | Docetaxel + Rogaratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with Rogaratinib (BAY 1163877) and Taxotere (docetaxel) resulted in an increased percentage of partial responses from 40% to 70% and one complete response compared to Taxotere (docetaxel) alone in lung cancer cell line xenograft models with FGFR1 amplification and FGFR1 overexpression (PMID: 30807645). | 30807645 |
| FGFR1 amp FGFR1 over exp | lung cancer | sensitive | Carboplatin + Paclitaxel + Rogaratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination therapy of Rogaratinib (BAY 1163877), Paraplatin (carboplatin), and Taxol (paclitaxel) resulted in an increased percentage of partial responses, from 30% to 70%, when compared to chemotherapy alone in lung cancer cell line xenograft models with FGFR1 amplification and FGFR1 overexpression (PMID: 30807645). | 30807645 |
| FGFR1 amp FGFR1 over exp | lung cancer | sensitive | Rogaratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with Rogaratinib (BAY 1163877) in a lung cancer cell line xenograft model with FGFR1 amplification and FGFR1 overexpression resulted in inhibition of tumor growth (PMID: 30807645). | 30807645 |
| FGFR1 W4C FGFR1 amp | estrogen-receptor positive breast cancer | predicted - sensitive | Lucitanib | Preclinical - Pdx | Actionable | In a preclinical study, Lucitanib (E-3810) treatment resulted in reduced tumor volume in an ER-positive breast cancer patient-derived xenograft (PDX) model harboring FGFR1 W4C and FGFR1 amplification (PMID: 34593528). | 34593528 |
| FGFR1 W4C FGFR1 amp | estrogen-receptor positive breast cancer | no benefit | Rogaratinib | Preclinical - Pdx | Actionable | In a preclinical study, Rogaratinib (BAY 1163877) treatment did not inhibit tumor growth in an ER-positive breast cancer patient-derived xenograft (PDX) model with FGFR1 W4C and FGFR1 amplification (PMID: 34593528). | 34593528 |
| Molecular Profile | Protein Effect | Treatment Approaches |
|---|---|---|
| FGFR1 amp | no effect | FGFR Inhibitor (Pan) FGFR1 Inhibitor GSK3052230 |
| FGFR1 amp FGFR2 amp | ||
| FGFR1 amp PIK3CA mut | ||
| FGFR1 amp NRAS amp | ||
| FGFR1 amp NRAS over exp | ||
| EML4 - ALK FGFR1 amp | ||
| FGFR2 fusion FGFR1 amp | ||
| FGFR1 amp FGFR1 over exp | ||
| FGFR1 W4C FGFR1 amp |