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Gene | FGFR2 |
Variant | over exp |
Impact List | none |
Protein Effect | no effect |
Gene Variant Descriptions | FGFR2 over exp indicates an over expression of the Fgfr2 protein and/or mRNA. However, the mechanism causing the over expression is unspecified. |
Associated Drug Resistance | |
Category Variants Paths |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR2 over exp | breast cancer | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited downstream Erk phosphorylation and proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). | 22869148 |
FGFR2 over exp | breast cancer | sensitive | Fexagratinib | Preclinical | Actionable | In a preclinical study, AZD4547 inhibited downstream Erk phosphorylation and proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). | 22869148 |
FGFR2 over exp | breast cancer | sensitive | PD173074 | Preclinical | Actionable | In a preclinical study, PD173074 inhibited proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). | 22869148 |
FGFR2 over exp | endometrial cancer | resistant | Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, endometrial cells with Fgfr2 overexpression were resistant to the anti-proliferative effects of AZD4547 (PMID: 26294741). | 26294741 |
FGFR2 over exp | colorectal cancer | sensitive | Aprutumab ixadotin | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Aprutumab ixadotin (BAY1187982) inhibited survival of colorectal cancer cells with over expressing Fgfr2 in culture, and suppressed tumor growth in cell line xenograft models (PMID: 27543601). | 27543601 |
FGFR2 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 FGFR2 in culture (PMID: 28978721). | 28978721 |
FGFR2 over exp | Advanced Solid Tumor | sensitive | Derazantinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr2 in culture and in cell line xenograft models (PMID: 27627808). | 27627808 |
FGFR2 over exp | Advanced Solid Tumor | predicted - sensitive | 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 |
FGFR2 over exp | lung squamous cell carcinoma | no benefit | 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 with 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 |
FGFR2 over exp | gastric adenocarcinoma | predicted - sensitive | Bemarituzumab + Fluorouracil + Leucovorin + Oxaliplatin | Phase II | Actionable | In a Phase II trial (FIGHT), the addition of Bemarituzumab (FPA144) to mFOLFOX6 treatment resulted in improved progression-free survival (9.5 months vs 7.4 months, HR=0.68, p=0.073) that did not reach statistical significance, and improved overall survival (not reached vs 12.9 months, HR=0.58, p=0.027) compared to mFOLFOX6 plus placebo in gastric or gastroesophageal junction adenocarcinoma patients with overexpression of FGFR2b (PMID: 36244398; NCT03694522). | 36244398 |
FGFR2 over exp | gastroesophageal adenocarcinoma | predicted - sensitive | Bemarituzumab + Fluorouracil + Leucovorin + Oxaliplatin | Phase II | Actionable | In a Phase II trial (FIGHT), the addition of Bemarituzumab (FPA144) to mFOLFOX6 treatment resulted in improved progression-free survival (9.5 months vs 7.4 months, HR=0.68, p=0.073) that did not reach statistical significance, and improved overall survival (not reached vs 12.9 months, HR=0.58, p=0.027) compared to mFOLFOX6 plus placebo in gastric or gastroesophageal junction adenocarcinoma patients with overexpression of FGFR2b (PMID: 36244398; NCT03694522). | 36244398 |