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Profile Name | FGFR2 act mut |
Gene Variant Detail | |
Relevant Treatment Approaches | FGFR Inhibitor (Pan) FGFR2 Inhibitor |
Molecular Profile | Indication/Tumor Type | Response Type | Relevant Treatment Approaches | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|---|
FGFR2 act mut | endometrial cancer | sensitive | FGFR Inhibitor (Pan) | Dovitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, both cell lines and cell line xenograft models of endometrial cancer with FGFR2 activating mutations showed greater sensitivity to Dovitinib (TKI258) as compared to FGFR2 wild-type (PMID: 23443805). | 23443805 |
FGFR2 act mut | Advanced Solid Tumor | sensitive | FGFR2 Inhibitor | Debio 1347 | Phase I | Actionable | In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR2 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). | detail... |
FGFR2 act mut | stomach carcinoma | sensitive | FGFR2 Inhibitor | S-49076 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, S-49076 inhibited Met activation, resulting in growth inhibition of gastric carcinoma cells harboring FGFR2 activating mutations in culture and in cell line xenograft models (PMID: 23804704). | 23804704 |
FGFR2 act mut | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR2 in culture (PMID: 22238366). | 22238366 |
FGFR2 act mut | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR2 in culture (PMID: 22238366). | 22238366 |
FGFR2 act mut | Advanced Solid Tumor | decreased response | Cediranib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Cediranib (AZD-2171) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). | 22238366 | |
FGFR2 act mut | Advanced Solid Tumor | decreased response | FGFR Inhibitor (Pan) | Nintedanib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). | 22238366 |
FGFR2 act mut | Advanced Solid Tumor | decreased response | Brivanib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR2 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Brivanib (BMS-540215) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). | 22238366 | |
FGFR2 act mut | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Phase I | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in stable disease in 70% (16/23) and partial response in 22% (5/23) of patients with advanced solid tumors harboring FGFR 1-4 activating mutations (including amplifications, mutations and translocations), while no antitumor activity was observed in patients with unknown or no known changes in FGFR (PMID: 26324363; NCT01703481). | 26324363 |
FGFR2 act mut | Advanced Solid Tumor | predicted - sensitive | FGFR2 Inhibitor | AZD4547 | Phase II | Actionable | In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, with a partial response in 1 and stable disease in 2 of 12 patients with FGFR2 activating mutations (PMID: 32463741; NCT02465060). | 32463741 |
FGFR2 act mut | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with advanced or metastatic bladder urothelial carcinoma harboring FGFR alterations (PMID: 34861372; ESMO.org). | detail... 34861372 |