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Gene | FGFR3 |
Variant | Y373C |
Impact List | missense |
Protein Effect | gain of function |
Gene Variant Descriptions | FGFR3 Y373C lies within the extracellular domain of the Fgfr3 protein (UniProt.org). Y373C confers a gain of function to the Fgfr3 protein resulting in increased proliferation relative to wild-type Fgfr3 in a competition assay (PMID: 34272467), constitutive activation, downstream signaling (PMID: 11429702, PMID: 11157491), and transformation of cultured cells (PMID: 11429702, PMID: 11157491, PMID: 34272467). |
Associated Drug Resistance | |
Category Variants Paths |
FGFR3 mutant FGFR3 act mut FGFR3 Y373C |
Transcript | NM_000142.5 |
gDNA | chr4:g.1804372A>G |
cDNA | c.1118A>G |
Protein | p.Y373C |
Source Database | RefSeq |
Genome Build | GRCh38/hg38 |
Transcript | gDNA | cDNA | Protein | Source Database | Genome Build |
---|---|---|---|---|---|
XM_006713872 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
NM_000142 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
NM_001354810.2 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
NM_001354809.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_011513422.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_006713873.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_047449823.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_011513420 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
NM_001354809.2 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_047449824.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
NM_001354810.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
NM_000142.4 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_047449822.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_006713873.2 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_011513422.2 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
NM_000142.5 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_011513420.1 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_006713873 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_011513420.2 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
XM_011513422 | chr4:g.1804372A>G | c.1118A>G | p.Y373C | RefSeq | GRCh38/hg38 |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR3 Y373C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 Y373C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 Y373C | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 Y373C were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
FGFR3 Y373C | myeloid neoplasm | no benefit | RO4987655 | Preclinical - Cell culture | Actionable | In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO4987655 in culture (PMID: 26438159). | 26438159 |
FGFR3 Y373C | myeloid neoplasm | no benefit | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). | 26438159 |
FGFR3 Y373C | myeloid neoplasm | sensitive | Zoligratinib | Preclinical | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 Y373C in culture (PMID: 25169980). | 25169980 |
FGFR3 Y373C | transitional cell carcinoma | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with advanced urothelial carcinoma who have received chemotherapy and an immune checkpoint inhibitor and harboring select FGFR mutations including FGFR3 Y373C (PMID: 38490358; ESMO.org). | detail... 38490358 |
FGFR3 Y373C | transitional cell carcinoma | sensitive | Erdafitinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase II trial (BCL2001) that supported FDA approval, Balversa (erdafitinib) treatment resulted in an objective response rate of 40% (40/99, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations and FGFR3 Y373C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
FGFR3 Y373C | transitional cell carcinoma | sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase III trial (THOR), Balversa (erdafitinib) treatment led to improved median overall survival (25.4 mo vs. 12.4 mo), median progression-free survival (8.4 mo vs. 2.9 mo), objective response rate (57.1% vs. 15.4%), and disease control rate (92.9% vs. 76.9%) compared to chemotherapy in Japanese patients with metastatic urothelial carcinoma with alterations in FGFR2 or FGFR3 (n=14), including FGFR3 Y373C (n=3), S249C (n=4), G370C (n=2), R248C (n=2), and FGFR3-TACC3 (n=3) (PMID: 39017806; NCT03390504). | 39017806 |
FGFR3 Y373C | bladder urothelial carcinoma | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with advanced bladder urothelial carcinoma who have received chemotherapy and an immune checkpoint inhibitor and harboring select FGFR mutations including FGFR3 Y373C (PMID: 38490358; ESMO.org). | 38490358 detail... |
FGFR3 Y373C | bladder urothelial carcinoma | sensitive | Erdafitinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase II trial (BCL2001) that supported FDA approval, Balversa (erdafitinib) treatment resulted in an objective response rate of 40% (40/99, 3 complete response, 37 partial response) and a disease control rate of 80% in patients with metastatic or unresectable urothelial carcinoma harboring FGFR alterations and FGFR3 Y373C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
FGFR3 Y373C | urinary bladder cancer | sensitive | Erdafitinib | Phase II | Actionable | In a Phase II trial (THOR-2), Balversa (erdafitinib) improved median recurrence-free survival (not reached vs 11.6 mo, HR=0.28, p=0.0008) in patients with recurrent high risk non-muscle invasive bladder cancer harboring FGFR3 mutations such as S249C (n=31), R248C (n=4), G370C, (n=3) or Y373C (n=10) or FGFR2-BICC1 (n=1), FGFR3-BAIAP2L1 (n=1), or FGFR3-TACC3 (n=5) compared to intravesical chemotherapy (PMID: 37871701; NCT04172675). | 37871701 |
FGFR3 Y373C | myeloid neoplasm | no benefit | RO5126766 | Preclinical - Cell culture | Actionable | In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO5126766 in culture (PMID: 26438159). | 26438159 |
FGFR3 Y373C | bladder urothelial carcinoma | predicted - sensitive | Pemigatinib | Case Reports/Case Series | Actionable | In a clinical case study, Pemazyre (pemigatinib) treatment resulted in a partial response with a progression-free survival of 8.4 months in a patient with bladder urothelial cancer harboring FGFR3 Y373C (PMID: 37377403). | 37377403 |
FGFR3 Y373C | urinary bladder cancer | predicted - sensitive | Pemigatinib | Case Reports/Case Series | Actionable | In a Phase II trial (FIGHT-207), Pemazyre (pemigatinib) treatment resulted in a partial response with a 50.8% decrease in target lesion and a progression-free survival of 6.2 months, and stable disease with a 30% decrease in target lesion and progression-free survival of 3.9 months in two patients with bladder cancer harboring FGFR3 Y373C (Cancer Res (2023) 83 (8_Supplement): CT016; NCT03822117). | detail... |
FGFR3 Y373C | transitional cell carcinoma | predicted - sensitive | Pembrolizumab + Pemigatinib | Case Reports/Case Series | Actionable | In a Phase I trial (FIGHT-101), treatment with the combination of Pemazyre (pemigatinib) and Keytruda (pembrolizumab) demonstrated safety in patients with advanced solid tumors and resulted in an objective response rate of 26.9% (7/26, all partial responses), including a partial response with a duration of response of 4.2 months in a patient with urothelial cancer harboring FGFR3 Y373C (PMID: 38986210; NCT02393248). | 38986210 |
FGFR3 Y373C | multiple myeloma | sensitive | E7090 | Preclinical - Cell culture | Actionable | In a preclinical study, a multiple myeloma cell line harboring FGFR3 Y373C (PMID: 19901323) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). | 19901323 27535969 |
FGFR3 Y373C | Advanced Solid Tumor | predicted - resistant | E7090 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 Y373C were resistant to treatment with E7090 in culture (PMID: 34272467). | 34272467 |
FGFR3 Y373C | bladder urothelial carcinoma | predicted - sensitive | Anlotinib + Sintilimab | Case Reports/Case Series | Actionable | In a clinical case study, a patient with metastatic bladder urothelial cancer harboring FGFR3 Y373C, PIK3CA E542K and TP53 R213* who had previously progressed on combination treatment with Sintilimab (IBI308) and Abraxane (nab-paclitaxel), achieved a partial response after 3 cycles of combination treatment with Sintilimab (IBI308) and Anlotinib (AL-3818), and stable disease has been observed for over 11 months (PMID: 34109111). | 34109111 |