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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 | 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 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 | 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 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 | breast cancer | predicted - sensitive | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in a breast cancer cell line harboring FGFR1 amplification in culture (PMID: 32973082). | 32973082 |
| 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 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 | 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 | 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 | 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 | 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 | 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 | 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 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 | 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 | 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 | 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 | 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 | 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 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 | 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 | 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 | 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 | 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 | 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 | 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 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 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 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 | 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 | 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 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 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 | 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 | 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 | 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 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 | 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 | 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 | 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 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 | 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 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 | 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 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 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 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 | 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 | 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 | 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 | 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 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 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 | 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 | Advanced Solid Tumor | predicted - sensitive | Futibatinib | Phase I | Actionable | In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) 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 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 | 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 | lung cancer | predicted - sensitive | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Futibatinib (TAS-120) 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 | 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 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 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 | 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 | 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 | 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 | 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 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 | 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 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 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 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, Futibatinib (TAS-120) 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 | 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 | 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 | 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 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 | 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 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 Taxotere (docetaxel) 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 | 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 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 |