Molecular Profile Detail

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Profile Name FGFR2 over exp
Gene Variant Detail

FGFR2 over exp (no effect)

Relevant Treatment Approaches FGFR Inhibitor (Pan) FGFR2 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
FGFR2 over exp breast cancer sensitive FGFR2 Inhibitor 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 FGFR2 Inhibitor 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 FGFR2 Inhibitor 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 FGFR Inhibitor (Pan) 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 FGFR2 Inhibitor 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 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
FGFR2 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 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