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Gene | FGFR1 |
Variant | act mut |
Impact List | unknown |
Protein Effect | gain of function |
Gene Variant Descriptions | FGFR1 act mut indicates that this variant results in a gain of function in the Fgfr1 protein. However, the specific amino acid change has not been identified. |
Associated Drug Resistance | |
Category Variants Paths |
FGFR1 mutant FGFR1 act mut |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR1 act mut | Advanced Solid Tumor | sensitive | Zoligratinib | Phase I | Actionable | In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR1 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). | detail... |
FGFR1 act mut | Advanced Solid Tumor | sensitive | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | sensitive | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | decreased response | Cediranib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR1 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 |
FGFR1 act mut | Advanced Solid Tumor | decreased response | Nintedanib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR1 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | no benefit | Brivanib | Preclinical | Actionable | In a preclinical study, Brivanib (BMS-540215) did not inhibit receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | predicted - sensitive | 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 |
FGFR1 act mut | Advanced Solid Tumor | predicted - sensitive | Erdafitinib | Phase II | Actionable | In a Phase II trial (RAGNAR), Balversa (erdafitinib) treatment resulted in an objective response rate of 29.5% (64/217, 6 complete and 58 partial responses), a disease control rate of 74%, clinical benefit rate of 46%, a median duration of response of 6.9 months, median progression-free survival of 4.2 months, and median overall survival of 10.7 months in patients with advanced solid tumors harboring FGFR1, FGFR2, or FGFR3 mutations or fusions (PMID: 37541273; NCT04083976). | 37541273 |
FGFR1 act mut | breast cancer | sensitive | FIIN-1 | Preclinical | Actionable | In a preclinical study, FIIN-1 inhibited Fgfr1 activation-induced proliferation and transformation of human breast epithelial cell lines in culture (PMID: 20338520). | 20338520 |
FGFR1 act mut | low grade glioma | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (MATCH), Balversa (erdafitinib) was tolerated and resulted in a partial response (PR) in 10% (2/20) and stable disease (SD) in 30% (6/20) of heavily pre-treated pediatric patients with low-grade gliomas or glioneuronal tumors harboring activating mutations in FGFR1 (n=16), FGFR2 (n=1), FGFR4 (n=1), or FGFR1 fusions (n=2), with a 6-mo overall survival rate of 89.7%, 2 PR and 4 SD were observed in patients with FGFR1 mutations ( (J Clin Oncol 41, 2023 (suppl 16; abstr 10007); NCT03210714). | detail... |
FGFR1 act mut | central nervous system benign neoplasm | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (MATCH), Balversa (erdafitinib) was tolerated and resulted in a partial response (PR) in 10% (2/20) and stable disease (SD) in 30% (6/20) of heavily pre-treated pediatric patients with low-grade gliomas or glioneuronal tumors harboring activating mutations in FGFR1 (n=16), FGFR2 (n=1), FGFR4 (n=1), or FGFR1 fusions (n=2), with a 6-mo overall survival rate of 89.7%, 2 PR and 4 SD were observed in patients with FGFR1 mutations (J Clin Oncol 41, 2023 (suppl 16; abstr 10007); NCT03210714). | detail... |
FGFR1 act mut | transitional cell carcinoma | no benefit | Derazantinib | Phase Ib/II | Actionable | In a Phase I/II trial (FIDES-02), Derazantinib (ARQ 087) treatment was well tolerated but demonstrated limited efficacy in patients with urothelial carcinoma harboring FGFR1 (n=4), FGFR2 (n=7), or FGFR3 (n=35) mutations or FGFR3 fusions (n=6), with an objective response rate of 8.2% (4/49, all partial responses) and disease control rate of 30.6% (15/49) by independent central review (PMID: 38627238; NCT04045613). | 38627238 |
FGFR1 act mut | lung non-small cell carcinoma | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with metastatic non-small cell lung cancer harboring oncogenic or likely oncogenic FGFR alterations (NCCN.org). | detail... |
FGFR1 act mut | breast cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with stage IV (M1) breast cancer harboring FGFR fusion or mutations (NCCN.org). | detail... |
FGFR1 act mut | salivary gland cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with unresectable locally advanced, recurrent, or metastatic salivary gland tumors harboring FGFR mutations or fusions (category 2B) who received prior systemic therapy and have no alternative systemic therapy available (NCCN.org). | detail... |
FGFR1 act mut | oral cavity cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with oral cavity cancer harboring FGFR mutations or fusions and with no alternative options (NCCN.org). | detail... |
FGFR1 act mut | oropharynx cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with oropharynx cancer harboring FGFR mutations or fusions and with no alternative options (NCCN.org). | detail... |
FGFR1 act mut | hypopharynx cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with hypopharynx cancer harboring FGFR mutations or fusions and with no alternative options (NCCN.org). | detail... |
FGFR1 act mut | supraglottis cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with supraglottic larynx cancer harboring FGFR mutations or fusions and with no alternative options (NCCN.org). | detail... |
FGFR1 act mut | glottis cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with glottic larynx cancer harboring FGFR mutations or fusions and with no alternative options (NCCN.org). | detail... |
FGFR1 act mut | ethmoid sinus cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with ethmoid sinus cancer harboring FGFR mutations or fusions and with no alternative options (NCCN.org). | detail... |
FGFR1 act mut | maxillary sinus cancer | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with maxillary sinus cancer harboring FGFR mutations or fusions and with no alternative options (NCCN.org). | detail... |