Molecular Profile Detail

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Profile Name FGFR1 over exp
Gene Variant Detail

FGFR1 over exp (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 over exp thyroid gland cancer sensitive FGFR Inhibitor (Pan) 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 head and neck squamous cell carcinoma sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical Actionable In a preclinical study, Truseltiq (infigratinib) inhibited cell growth and induced apoptosis in HNSCC cells over expressing Fgfr1 in culture and in xenograft models (PMID: 26015511). 26015511
FGFR1 over exp uterus leiomyosarcoma sensitive FGFR1 Inhibitor 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 uterus leiomyosarcoma sensitive FGFR1 Inhibitor 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 FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Truseltiq (infigratinib) inhibited survival of FGFR1-overexpressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 over exp Advanced Solid Tumor sensitive FGFR Inhibitor (Pan) 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 Advanced Solid Tumor sensitive FGFR1 Inhibitor 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 over exp Her2-receptor negative breast cancer predicted - sensitive FGFR1 Inhibitor Lucitanib Phase II Actionable In a Phase II (FINESSE) trial, Lucitanib (E-3810) treatment resulted in improved objective response rate (25%, 5/20 vs 8%, 3/39) and median progression-free survival (158 vs 109 days) in patients with metastatic hormone receptor-positive, Erbb2 (Her2)-negative breast cancer with high Fgfr1 expression (H-score>=50) compared to those with low Fgfr1 expression (H-score<50) (PMID: 31619444; NCT02053636). 31619444
FGFR1 over exp Advanced Solid Tumor predicted - sensitive FGFR Inhibitor (Pan) Rogaratinib Phase I Actionable In a Phase I trial, treatment with Rogaratinib (BAY 1163877) was well-tolerated and resulted in objective response rate (ORR) of 15% (15/100) in patients with FGFR1, FGFR2, or FGFR3-overexpressing advanced solid tumors, including urothelial cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer, and led to an ORR of 67% (10/15) in patients with FGFR overexpression, but without an FGFR genetic aberration (PMID: 31405822; NCT01976741). 31405822
FGFR1 over exp colon cancer sensitive FGFR Inhibitor (Pan) Rogaratinib Preclinical Actionable In a preclinical study, syngeneic colon cancer mouse models with FGFR1 over expression demonstrated antitumor activity when treated with Rogaratinib (BAY 1163877), with a partial response observed in 22% (2/9) and stable disease in one (PMID: 30807645). 30807645
FGFR1 over exp lung cancer predicted - sensitive FGFR Inhibitor (Pan) Rogaratinib Preclinical - Pdx Actionable In a preclinical study, a lung cancer patient-derived xenograft (PDX) model with FGFR1 overexpression demonstrated decreased tumor volume when treated with Rogaratinib (BAY 1163877) (PMID: 30807645). 30807645
FGFR1 over exp lung cancer predicted - sensitive FGFR Inhibitor (Pan) Docetaxel + Rogaratinib Preclinical - Pdx Actionable In a preclinical study, the combination of Rogaratinib (BAY 1163877) and Taxotere (docetaxel) resulted in improved inhibition of tumor growth and duration of response, leading to three complete responses and seven partial responses compared to Taxotere (docetaxel) alone, resulting in only six partial responses, in lung cancer patient-derived xenograft models with FGFR1 overexpression (n=10) (PMID: 30807645). 30807645
FGFR1 over exp stomach cancer sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, treatment with Stivarga (regorafenib) in an FGFR1-overexpressing gastric cancer cell line resulted in decreased phosphorylation of Fgfr2 and Erk, and inhibition of cell growth in culture (PMID: 33563752). 33563752
FGFR1 over exp stomach cancer sensitive FGFR Inhibitor (Pan) Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Truseltiq (infigratinib) treatment inhibited growth of FGFR1-overexpressing gastric cancer cells in culture (PMID: 33563752). 33563752
FGFR1 over exp stomach cancer sensitive FGFR Inhibitor (Pan) Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) treatment inhibited growth of FGFR1-overexpressing gastric cancer cells in culture (PMID: 33563752). 33563752
FGFR1 over exp stomach cancer sensitive FGFR Inhibitor (Pan) Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) treatment inhibited growth of gastric cancer cells overexpressing FGFR1 in culture (PMID: 33563752). 33563752
FGFR1 over exp stomach cancer sensitive Regorafenib + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the addition of Mekinist (trametinib) restored sensitivity of gastric cancer cells with FGFR1 overexpression to Stivarga (regorafenib) treatment, demonstrating decreased Erk phosphorylation and reduced cell proliferation in culture (PMID: 33563752). 33563752
FGFR1 over exp stomach cancer sensitive FGFR Inhibitor (Pan) Infigratinib + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the addition of Mekinist (trametinib) restored sensitivity of gastric cancer cells with FGFR1 overexpression to Truseltiq (infigratinib) treatment, demonstrating decreased Erk phosphorylation and reduced cell proliferation in culture (PMID: 33563752). 33563752
FGFR1 over exp lung squamous cell carcinoma no benefit FGFR Inhibitor (Pan) Rogaratinib Phase II Actionable In a Phase II trial (SAKK 19/18), Rogaratinib (BAY 1163877) treatment did not meet its primary endpoint for 6-month progression-free survival (PFS) in patients with advanced lung squamous cell carcinoma harboring overexpression of FGFR1, FGFR2, or FGFR3, and resulted in only 6.7% (1/15) of patients achieving 6-month PFS, with no objective responses, a median PFS of 1.6 months, and a median overall survival of 3.5 months (PMID: 36099710; NCT03762122). 36099710
FGFR1 over exp transitional cell carcinoma no benefit FGFR Inhibitor (Pan) Rogaratinib Phase II Actionable In a Phase II trial (FORT-1), Rogaratinib (BAY 1163877) treatment did not result in improved outcomes compared to chemotherapy in advanced or metastatic urothelial carcinoma patients with FGFR1 or FGFR3 overexpression, with similar median overall survival (8.3 mo vs 9.8 mo), median progression-free survival (2.7 mo vs. 3.2 mo), and objective response rate (20.7% (18/87) vs 19.3% (17/88)), failing to meet the predetermined criteria for continuation to Phase III (PMID: 36240478; NCT03410693). 36240478
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