Molecular Profile Detail

Profile Name FGFR1 amp
Gene Variant Detail

FGFR1 amp (no effect)

Relevant Treatment Approaches FGFR Inhibitor (Pan) FGFR1 Inhibitor GSK3052230

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR1 amp non-small cell lung carcinoma sensitive FGFR Inhibitor (Pan) 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 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 lung squamous cell carcinoma sensitive FGFR1 Inhibitor 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 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 lung squamous cell carcinoma no benefit FGFR Inhibitor (Pan) 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 predicted - sensitive FGFR Inhibitor (Pan) 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 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 Advanced Solid Tumor predicted - sensitive FGFR1 Inhibitor 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 cancer sensitive FGFR1 Inhibitor 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 large cell carcinoma sensitive FGFR1 Inhibitor 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 breast cancer no benefit FGFR1 Inhibitor 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 breast cancer sensitive FGFR Inhibitor (Pan) 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 FGFR1 Inhibitor 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 GSK3052230 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 lung cancer sensitive GSK3052230 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 non-small cell lung carcinoma sensitive FGFR Inhibitor (Pan) 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 estrogen-receptor positive breast cancer sensitive FGFR1 Inhibitor 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 small cell carcinoma sensitive FGFR1 Inhibitor 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 sensitive FGFR Inhibitor (Pan) 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 lung squamous cell carcinoma sensitive FGFR Inhibitor (Pan) 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 cancer sensitive FGFR1 Inhibitor 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 adrenocortical carcinoma sensitive FGFR1 Inhibitor 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 small cell carcinoma sensitive GSK3052230 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 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 FGFR1 Inhibitor 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 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 synovial sarcoma sensitive FGFR Inhibitor (Pan) 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 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 adenocarcinoma sensitive FGFR Inhibitor (Pan) 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 FGFR1 Inhibitor 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 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 synovial sarcoma sensitive FGFR1 Inhibitor 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 small cell carcinoma sensitive FGFR1 Inhibitor 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 Her2-receptor positive breast cancer sensitive FGFR Inhibitor (Pan) 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 lung squamous cell carcinoma no benefit FGFR1 Inhibitor 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 non-small cell lung carcinoma sensitive FGFR1 Inhibitor 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 squamous cell carcinoma sensitive FGFR Inhibitor (Pan) 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 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 non-small cell lung carcinoma sensitive FGFR Inhibitor (Pan) 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 estrogen-receptor positive breast cancer sensitive FGFR Inhibitor (Pan) 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 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 large cell carcinoma sensitive FGFR Inhibitor (Pan) 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 Her2-receptor negative breast cancer predicted - sensitive FGFR1 Inhibitor 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 FGFR1 Inhibitor 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 sensitive FGFR1 Inhibitor 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 estrogen-receptor positive breast cancer sensitive FGFR Inhibitor (Pan) 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 carcinoma sensitive FGFR1 Inhibitor 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 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 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 lung cancer no benefit FGFR1 Inhibitor 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 synovial sarcoma sensitive FGFR1 Inhibitor 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 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 transitional cell carcinoma sensitive FGFR1 Inhibitor 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 small cell carcinoma sensitive FGFR1 Inhibitor 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 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 Ewing sarcoma predicted - sensitive FGFR Inhibitor (Pan) 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
Clinical Trial Phase Therapies Title Recruitment Status
NCT02608125 Phase I PRN1371 A Dose Escalation and Dose Expansion Study of PRN1371 in Adult Patients With Advanced Solid Tumors Recruiting
NCT02872714 Phase II Pemigatinib A Study to Evaluate the Efficacy and Safety of Pemigatinib (INCB054828) in Subjects With Urothelial Carcinoma - (FIGHT-201) Recruiting
NCT02465060 Phase II Erdafitinib Copanlisib Trametinib Crizotinib Sunitinib Sapanisertib Nivolumab AZD4547 Dasatinib Pertuzumab + Trastuzumab Dabrafenib + Trametinib Binimetinib Adavosertib Osimertinib Palbociclib Afatinib Capivasertib Defactinib GSK2636771 Vismodegib Ado-trastuzumab emtansine Larotrectinib Taselisib Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) Recruiting
NCT02393248 Phase Ib/II Cisplatin + Gemcitabine + Pemigatinib Docetaxel + Pemigatinib INCMGA00012 + Pemigatinib Pemigatinib + Trastuzumab Epacadostat + Pembrolizumab Open-Label, Dose-Escalation Study of Pemigatinib in Subjects With Advanced Malignancies - (FIGHT-101) Recruiting
NCT01948297 Phase I Debio 1347 Debio 1347-101 Phase I Trial in Advanced Solid Tumours With Fibroblast Growth Factor Receptor (FGFR) Alterations Recruiting
NCT01975701 Phase II BGJ398 A Phase 2 Study of BGJ398 in Patients With Recurrent GBM Completed
NCT02160041 Phase II BGJ398 BGJ398 for Patients With Tumors With FGFR Genetic Alterations Completed
NCT02846766 Phase II Lenvatinib Study of Lenvatinib in Patients With Advanced Cancer and Aberrations in FGF/FGFR Signaling Withdrawn
NCT02706691 Phase II BGJ398 Pan FGFR Kinase Inhibitor BGJ398 in Treating Patients With FGFR1-3 Translocated, Mutated, or Amplified Recurrent Head and Neck Cancer Terminated
NCT01868022 Phase I Docetaxel Cisplatin + Pemetrexed GSK3052230 Carboplatin + Paclitaxel Study to Evaluate GSK3052230 in Combination With Paclitaxel and Carboplatin, or Docetaxel or as Single Agent in Subjects With Solid Malignancies and Deregulated Fibroblast Growth Factor (FGF) Pathway Signaling Completed
NCT03344536 Debio 1347 + Fulvestrant A Study of Debio 1347 Plus Fulvestrant in Patients With Metastatic Breast Cancer Recruiting
NCT03238196 Phase I Erdafitinib + Fulvestrant + Palbociclib Fulvestrant, Palbociclib and Erdafitinib in ER+/HER2-/FGFR-amplified Metastatic Breast Cancer Recruiting
NCT01004224 Phase I BGJ398 A Dose Escalation Study in Adult Patients With Advanced Solid Malignancies Completed
NCT02202746 Phase II Lucitanib A Study to Assess the Safety and Efficacy of the VEGFR-FGFR Inhibitor, Lucitanib, Given to Patients With FGF Aberrant Metastatic Breast Cancer Completed
NCT02272998 Phase II Ponatinib Ponatinib for Patients Whose Advanced Solid Tumor Cancer Has Activating Mutations Involving the Following Genes: FGFR1, FGFR2, FGFR3, FGFR4, RET, KIT. Recruiting
NCT02795156 Phase II Cabozantinib Afatinib Regorafenib Study to Assess the Activity of Molecularly Matched Targeted Therapies in Select Tumor Types Based on Genomic Alterations Recruiting
NCT02109016 Phase II Lucitanib A Study to Assess the Efficacy of the VEGFR-FGFR Inhibitor, Lucitanib, Given to Patients With FGFR1-driven Lung Cancer Terminated
NCT02558348 Phase Ib/II Anlotinib Phase 1/2a Evaluation of AL3818 in Subjects With Recurrent or Metastatic Endometrial, Ovarian or Cervical Cancer (AL3818-US-001) Recruiting
NCT02299141 Phase I Nintedanib Nintedanib in Molecularly Selected Patients With Advanced Non-Small Cell Lung Cancer Recruiting