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| Gene Symbol | FGFR3 | ||||||||||
| Synonyms | ACH | CD333 | CEK2 | HSFGFR3EX | JTK4 | ||||||||||
| Gene Description | FGFR3, fibroblast growth factor receptor 3, is a receptor tyrosine kinase activated upon binding of the FGF ligand, which activates RAS-MAPK and PI3K-AKT pathways (PMID: 22508544). Altered function of FGFR3 in cancer may lead to increased cell proliferation and decreased apoptosis (PMID: 22508544) and mutations and fusions are commonly observed in bladder cancer (PMID: 30975452, PMID: 23175443), while FGFR3 overexpression only in bladder cancer may have different treatment implications (PMID: 32682615). | ||||||||||
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FGFR3 wild-type | urinary bladder cancer | resistant | Ponatinib | Preclinical | Actionable | In a preclinical study, bladder cancer cells with wild-type FGFR3 were resistant to growth inhibition by Iclusig (ponatinib) in cell culture (PMID: 22238366). | 22238366 |
| FGFR3 wild-type | myeloid neoplasm | sensitive | SSR128129E | Preclinical | Actionable | In a preclinical study, SSR128129E inhibited proliferation of myeloma cells expressing wild-type FGFR3 in culture (PMID: 23597562). | 23597562 |
| FGFR3 wild-type | bladder carcinoma | sensitive | Vofatamab | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Vofatamab (B-701) decreased wild-type FGFR3 activation, thereby inhibited cell proliferation of FGFR3 wild-type human bladder cancer cells in culture and in cell line xenograft models (PMID: 19381019). | 19381019 |
| FGFR3 wild-type | myeloid neoplasm | sensitive | SU5402 | Preclinical - Cell culture | Actionable | In a preclinical study, SU5402 inhibited proliferation of myeloma cells expressing wild-type FGFR3 in culture (PMID: 23597562). | 23597562 |
| FGFR3 dec exp FGFR3 wild-type HRAS G12V | transitional cell carcinoma | resistant | AZD4547 | Preclinical | Actionable | In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZD4547 in culture (PMID: 22869148). | 22869148 |
| FGFR3 dec exp FGFR3 wild-type HRAS G12V | transitional cell carcinoma | resistant | PD173074 | Preclinical | Actionable | In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to PD173074 in culture (PMID: 22869148). | 22869148 |
| FGFR3 dec exp FGFR3 wild-type HRAS G12V | transitional cell carcinoma | decreased response | AZ8010 | Preclinical | Actionable | In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZ8010 in culture (PMID: 22869148). | 22869148 |
| FGFR3 K652E | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cell line expressing FGFR3 K652E in culture (PMID: 32370101). | 32370101 |
| FGFR3 K652E | urinary bladder cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3 K652E in culture (PMID: 27627808). | 27627808 |
| FGFR3 K652E | Advanced Solid Tumor | sensitive | Vofatamab | Preclinical - Cell culture | Actionable | In a preclinical study, Vofatamab (B-701) inhibited ligand-dependent cell proliferation in cells expressing FGFR3 K652E in culture (PMID: 19381019). | 19381019 |
| FGFR3 K652E | urinary bladder cancer | resistant | PD173074 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3 K652E were resistant to PD173074 in culture and in cell line xenograft models (PMID: 23558953). | 23558953 |
| FGFR3 K652E | Advanced Solid Tumor | sensitive | Dasatinib + Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Truseltiq (infigratinib) and Sprycel (dasatinib) treatment inhibited viability of a cell line expressing FGFR3 K652E in culture (PMID: 32370101). | 32370101 |
| FGFR3 K652E PIK3CA P124L | urinary bladder cancer | sensitive | Alpelisib + Nintedanib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Piqray (alpelisib) led to synergistic inhibition of growth in a bladder cancer cell line harboring FGFR3 K652E and PIK3CA P124L in culture (PMID: 36805958). | 36805958 |
| FGFR3 K652E PIK3CA P124L | urinary bladder cancer | sensitive | Nintedanib + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Pictilisib (GDC-0941) inhibited cell proliferation in a bladder cancer cell line harboring FGFR3 K652E PIK3CA P124L in culture (PMID: 36805958). | 36805958 |
| FGFR3 act mut | Advanced Solid Tumor | predicted - sensitive | 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 7 patients with FGFR3 activating mutations (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 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 FGFR3 in culture (PMID: 22238366). | 22238366 |
| FGFR3 act mut | Advanced Solid Tumor | decreased response | Nintedanib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR3 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). | 22238366 |
| FGFR3 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 FGFR3 in culture (PMID: 22238366). | 22238366 |
| FGFR3 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 FGFR3 in culture (PMID: 22238366). | 22238366 |
| FGFR3 act mut | Advanced Solid Tumor | decreased response | Cediranib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR3 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 |
| FGFR3 act mut | Advanced Solid Tumor | sensitive | Debio 1347 | Phase I | Actionable | In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR3 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). | detail... |
| FGFR3 act mut | bladder urothelial carcinoma | sensitive | 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 |
| FGFR3 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 |
| FGFR3 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 |
| FGFR3 act mut | urinary bladder cancer | predicted - sensitive | S-49076 | Preclinical | Actionable | In a preclinical study, S-49076 inhibited autophosphorylation of FGFR3 and downstream signaling in bladder cancer cells over expressing constitutively active FGFR3 in culture (PMID: 23804704). | 23804704 |
| FGFR3 act mut | transitional cell carcinoma | sensitive | Pemigatinib | Phase II | Actionable | In a Phase II trial (FIGHT-201), Pemazyre (pemigatinib) treatment resulted in an objective response rate (ORR) of 17.8%, median duration of response (mDOR) of 6.2 mo, median progression-free survival (mPFS) of 4.0 mo, and median overall survival (mOS) of 6.8 mo with continuous dosing, and an ORR of 23.3%, mDOR of 6.2 mo, mPFS of 4.3 mo, and mOS of 8.9 mo with intermittent dosing in patients with urothelial carcinoma harboring FGFR3 mutations or fusions/rearrangements (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR3 act mut FGFR3 over exp | transitional cell carcinoma | predicted - sensitive | Rogaratinib | Phase II | Actionable | In a Phase II trial (FORT-1), Rogaratinib (BAY 1163877) treatment resulted in a higher objective response rate of 52.4% (11/21) compared to 26.7% (4/15) with chemotherapy in advanced or metastatic urothelial carcinoma patients with FGFR3 overexpression and an FGFR3 alteration (including FGFR3 G370C, FGFR3 R248C, FGFR3 S249C, FGFR3 Y373C, FGFR3-TACC3v1, and FGFR3-TACC3v3) (PMID: 36240478; NCT03410693). | 36240478 |
| FGFR3 mutant | urinary bladder cancer | sensitive | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 mutation in culture (PMID: 27550940). | 27550940 |
| FGFR3 mutant | transitional cell carcinoma | sensitive | Infigratinib | Clinical Study | Actionable | In a clinical study, Truseltiq (infigratinib) treatment in patients with FGFR3 alterations led to 25.4% (17/67) confirmed responses and a disease control rate of 64% (43/67), which included complete responses, partial responses, and stable disease, and resulted in a median progression-free survival of 3.75 months and a median overall survival of 7.75 months (PMID: 29848605). | 29848605 |
| FGFR3 mutant | transitional cell carcinoma | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, Truseltiq (infigratinib) treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517); NCT01004224). | detail... |
| FGFR3 mutant | bladder urothelial carcinoma | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, patients with bladder urothelial carcinoma harboring an FGFR3 mutation demonstrated a disease control rate of 75% (6/8) when treated with Truseltiq (infigratinib), including 3 patients with a partial response and 3 with stable disease (PMID: 27870574; NCT01004224). | 27870574 |
| FGFR3 mutant | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, tumor cell lines with FGFR3 mutations demonstrated sensitivity to Truseltiq (infigratinib) in culture (PMID: 23002168). | 23002168 |
| FGFR3 mutant | bladder urothelial carcinoma | sensitive | Dovitinib | Phase II | Actionable | In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in 33% (1/3) of patients with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 mutations (PMID: 27932416). | 27932416 |
| FGFR3 mutant | Advanced Solid Tumor | predicted - sensitive | Debio 1347 | Phase I | Actionable | In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR3 mutant | transitional cell carcinoma | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in the guidelines for patients with advanced or metastatic urothelial carcinoma harboring Fgfr3 alterations after progression on platinum-based regimens (NCCN.org). | detail... |
| FGFR3 mutant | transitional cell carcinoma | sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in 25% tumor shrinkage at week 8 in an urothelial cancer patient harboring FGFR3 mutations (PMID: 26324363; NCT01703481). | 26324363 |
| FGFR3 mutant | transitional cell carcinoma | sensitive | Erdafitinib | Phase I | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 46% (12/26) in patients with urothelial carcinoma harboring FGFR genomic alterations, including 17 with FGFR3 mutations, and 11 with FGFR2 and/or FGFR3 fusions (PMID: 31088831; NCT01703481). | 31088831 |
| FGFR3 mutant | transitional cell carcinoma | sensitive | Erdafitinib | FDA approved - Has 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 (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 mutant | bladder urothelial carcinoma | sensitive | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in the guidelines for patients with advanced or metastatic urothelial carcinoma harboring Fgfr3 alterations after progression on platinum-based regimens (NCCN.org). | detail... |
| FGFR3 mutant | bladder urothelial carcinoma | sensitive | Erdafitinib | FDA approved - Has 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 (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 mutant | cholangiocarcinoma | predicted - sensitive | Erdafitinib | Phase I | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 27% (3/11) in patients with cholangiocarcinoma harboring FGFR genomic alterations, including 1 with FGFR2 mutation, 2 with FGFR3 mutations, and 8 with FGFR2 fusions (PMID: 31088831; NCT01703481). | 31088831 |
| FGFR3 mutant | transitional cell carcinoma | no benefit | Atezolizumab | Phase II | Actionable | In a Phase II trial (IMVigor 210, CheckMate 275), Tecentriq (atezolizumab) (n=119) treatment resulted in similar response rate (24% vs 21%, p=0.8) in patients with FGFR3 mutant or wild-type metastatic transitional cell carcinoma (PMID: 31272788). | 31272788 |
| FGFR3 mutant | transitional cell carcinoma | no benefit | Nivolumab | Phase II | Actionable | In a Phase II trial (CheckMate 275), Opdivo (nivolumab) (n=270) treatment resulted in similar response rate (20% vs 21%, p=0.2) in patients with FGFR3 mutant or wild-type metastatic transitional cell carcinoma (PMID: 31272788). | 31272788 |
| FGFR3 mutant | Advanced Solid Tumor | sensitive | Pemigatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a variety of cancer cell lines harboring mutations in FGFR1, FGFR2, and/or FGFR3 demonstrated sensitivity to Pemazyre (pemigatinib) in culture and in cell line xenograft models, resulting in inhibition of tumor growth (Cancer Res 2015;75(15 Suppl):Abstract nr 771). | detail... |
| FGFR3 mutant | transitional cell carcinoma | predicted - sensitive | Cetrelimab + Erdafitinib | Phase II | Actionable | In a Phase II trial, the combination of Balversa (erdafitinib) and Cetrelimab (JNJ-63723283) treatment resulted in an overall response rate of 54.5% (6 complete responses), disease control rate of 79.5%, median duration of response of 11.10 months, median progression-free survival of 10.97 months, and a 12-month overall survival of 68% in patients with metastatic urothelial carcinoma harboring FGFR mutations (J Clin Oncol 41, 2023 (suppl 16; abstr 4504); NCT03473743). | detail... |
| FGFR3 mutant | transitional cell carcinoma | predicted - sensitive | Docetaxel + Vofatamab | Phase Ib/II | Actionable | In a Phase I/II trial, Vofatamab (B-701) in combination with Taxotere (docetaxel) demonstrated safety and preliminary efficacy, resulted in enhanced activity in patients with locally advanced or metastatic urothelial carcinoma harboring FGFR3 mutations or fusions comparing to wild-type patients (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 4534-4534; NCT02401542). | detail... |
| FGFR3 mutant | Advanced Solid Tumor | predicted - sensitive | ICP-192 | Phase I | Actionable | In a Phase I trial, ICP-192 (gunagratinib) was well-tolerated, and resulted in an overall response rate or 33.3% (4/12, 1 complete response, 3 partial response) and a disease control rate of 91.7% (11/12) in patients with advanced solid tumors harboring FGF/FGFR gene aberrations (J Clin Oncol 39, 2021 (suppl 15; abstr 4092); NCT03758664). | detail... |
| FGFR3 mut FGFR3 over exp | urinary bladder cancer | sensitive | Dovitinib | Phase II | Actionable | In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 33% (1/3) of non-muscle invasive bladder cancer patients harboring both FGFR3 mutations and FGFR3 over expression (J Clin Oncol 34, 2016 (suppl; abstr 4526)). | detail... |
| FGFR3 fusion FGFR3 mut | multiple myeloma | sensitive | 3D185 | Preclinical - Cell culture | Actionable | In a preclinical study, 3D185 inhibited proliferation of a multiple myeloma cell line harboring an FGFR3 fusion and an FGFR3 mutation in culture (PMID: 31438996). | 31438996 |
| FGFR3 rearrange | myeloid neoplasm | sensitive | AZD4547 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, AZD4547 inhibited survival of myeloma cells harboring FGFR3 translocation in culture and in cell line xenograft models (PMID: 27550940). | 27550940 |
| FGFR3 rearrange | myeloid neoplasm | sensitive | PRN1371 | Preclinical - Cell culture | Actionable | In a preclinical study, PRN1371 inhibited proliferation of myeloma cells harboring FGFR3 rearrangements in culture (AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1249). | detail... |
| FGFR3 rearrange FGFR3 K650E | multiple myeloma | predicted - sensitive | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lytgobi (futibatinib) treatment led to inhibition of cell proliferation in a multiple myeloma cell line harboring an FGFR3 rearrangement and FGFR3 K650E in culture (PMID: 32973082). | 32973082 |
| FGFR3 rearrange FGFR3 Y373C | multiple myeloma | sensitive | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Lytgobi (futibatinib) treatment led to inhibition of cell proliferation in a multiple myeloma cell line harboring an FGFR3 rearrangement and FGFR3 Y373C in culture, and led to tumor regression in a cell line xenograft model (PMID: 32973082). | 32973082 |
| FGFR3 rearrange NRAS act mut | multiple myeloma | no benefit | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, a multiple myeloma cell line harboring an FGFR3 rearrangement and an NRAS activating mutation was not sensitive to treatment with Lytgobi (futibatinib) in culture (PMID: 32973082). | 32973082 |
| FGFR3 rearrange FGFR3 F384L | multiple myeloma | no benefit | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, a multiple myeloma cell line harboring an FGFR3 rearrangement and FGFR3 F384L was not sensitive to treatment with Lytgobi (futibatinib) in culture (PMID: 32973082). | 32973082 |
| FGFR3 S249C | urinary system cancer | sensitive | AZD4547 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, AZD4547 decreased Myc expression and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture and in xenograft models (PMID: 27401245). | 27401245 |
| FGFR3 S249C | renal pelvis transitional cell carcinoma | predicted - sensitive | AZD4547 | Case Reports/Case Series | 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%, including stable disease for greater than 6 months in a patient with transitional cell carcinoma of the renal pelvis harboring FGFR3 S249C (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 S249C | urinary system cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture (PMID: 27401245). | 27401245 |
| FGFR3 S249C | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cell line expressing FGFR3 S249C in culture (PMID: 32370101). | 32370101 |
| FGFR3 S249C | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). | 23786770 |
| FGFR3 S249C | Advanced Solid Tumor | resistant | Dasatinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing FGFR3 S249C was resistant to Sprycel (dasatinib) treatment in culture (PMID: 32370101). | 32370101 |
| FGFR3 S249C | bladder urothelial carcinoma | sensitive | Dovitinib | Case Reports/Case Series | Actionable | In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in a patient with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 S249C (PMID: 27932416). | 27932416 |
| FGFR3 S249C | urinary bladder cancer | sensitive | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 S249C mutation in culture (PMID: 22238366). | 22238366 |
| FGFR3 S249C | Advanced Solid Tumor | conflicting | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 S249C were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 S249C | Advanced Solid Tumor | conflicting | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). | 23786770 |
| FGFR3 S249C | urinary bladder cancer | resistant | Nintedanib | Preclinical | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3 S249C were resistant to Ofev (Nintedanib) induced inhibition of cell proliferation in culture (PMID: 22238366). | 22238366 |
| FGFR3 S249C | renal pelvis transitional cell carcinoma | predicted - sensitive | Pazopanib | Clinical Study | Actionable | In a case study, a patient with urothelial carcinoma of the renal pelvis harboring FGFR3 S249C demonstrated a partial response lasting 9 months following treatment with Votrient (pazopanib) (PMID: 27271022). | 27271022 |
| FGFR3 S249C | urinary bladder cancer | sensitive | Ponatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited growth of bladder cancer cells harboring FGFR3 S249C in culture and in cell line xenograft models (PMID: 22238366). | 22238366 |
| FGFR3 S249C | Advanced Solid Tumor | sensitive | Ponatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). | 23786770 |
| FGFR3 S249C | renal pelvis transitional cell carcinoma | no benefit | RO4987655 | Preclinical - Cell culture | Actionable | In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO4987655 in culture (PMID: 26438159). | 26438159 |
| FGFR3 S249C | renal pelvis transitional cell carcinoma | no benefit | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). | 26438159 |
| FGFR3 S249C | urinary bladder cancer | no benefit | Brivanib | Preclinical | Actionable | In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of bladder cancer cells harboring FGFR3 S249C in culture (PMID: 22238366). | 22238366 |
| FGFR3 S249C | urinary bladder cancer | sensitive | Cediranib | Preclinical | Actionable | In a preclinical study, Cediranib (AZD-2171) inhibited growth of bladder cancer cells harboring FGFR3 S249C mutation in culture (PMID: 22238366). | 22238366 |
| FGFR3 S249C | urinary bladder cancer | sensitive | Debio 1347 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of bladder cancer cells harboring FGFR3 S249C in culture and inhibited tumor growth in FGFR3 S249C-positive bladder cancer cell line xenograft models (PMID: 25169980). | 25169980 |
| FGFR3 S249C | ovarian cancer | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (RAGNAR), treatment with Balversa (erdafitinib) resulted in a partial response with a duration of response of 5.55 months in a patient with ovarian cancer harboring FGFR3 S249C (PMID: 37541273; NCT04083976). | 37541273 |
| FGFR3 S249C | 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 S249C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 S249C | lung squamous cell carcinoma | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (RAGNAR), treatment with Balversa (erdafitinib) resulted in a partial response with a duration of response of 9.03 months in a patient with squamous non-small cell lung cancer harboring FGFR3 S249C (PMID: 37541273; NCT04083976). | 37541273 |
| FGFR3 S249C | 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 S249C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 S249C | head and neck squamous cell carcinoma | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (RAGNAR), treatment with Balversa (erdafitinib) resulted in a partial response with a duration of response of 2.89 months in a patient with squamous cell head and neck cancer harboring FGFR3 S249C (PMID: 37541273; NCT04083976). | 37541273 |
| FGFR3 S249C | 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 S249C | transitional cell carcinoma | predicted - sensitive | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Lytgobi (futibatinib) treatment led to an overall objective response rate of 15.8% (3/19, 3 partial responses) and a disease control rate of 47.4% (9/19), with stable disease in 6, in urothelial cancer patients harboring an FGFR3 mutation or FGFR1 mutation, including partial responses in 2 patients with urothelial cancer harboring FGFR3 S249C with a progression-free survival of 2.7 and 4.7 mo, and a duration of response of 1.4 and 3.4 mo, respectively (PMID: 34551969; NCT02052778). | 34551969 |
| FGFR3 S249C | renal pelvis transitional cell carcinoma | no benefit | RO5126766 | Preclinical - Cell culture | Actionable | In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO5126766 in culture (PMID: 26438159). | 26438159 |
| FGFR3 S249C | bladder carcinoma | sensitive | Vofatamab | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Vofatamab (B-701) decreased dimer formation and constitutive activation of FGFR3 S249C, and inhibited growth of bladder cancer cell lines harboring FGFR3 S249C in culture and in xenograft models (PMID: 19381019). | 19381019 |
| FGFR3 S249C | Advanced Solid Tumor | sensitive | Vofatamab | Preclinical - Cell culture | Actionable | In a preclinical study, Vofatamab (B-701) inhibited proliferation of transformed cells expressing FGFR3 S249C in culture (PMID: 19381019). | 19381019 |
| FGFR3 S249C | urinary bladder cancer | resistant | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3 S249C were resistant to PD173074 in culture (PMID: 23558953). | 23558953 |
| FGFR3 S249C | urinary bladder cancer | sensitive | ASP5878 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ASP5878 treatment inhibited proliferation of a bladder cancer cell line harboring FGFR3 S249C in culture, and resulted in tumor regression in xenograft models (Mol Cancer Ther December 2015 14; A170). | detail... |
| FGFR3 S249C | transitional cell 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 8.3 months in a patient with urothelial cancer harboring FGFR3 S249C (PMID: 37377403). | 37377403 |
| FGFR3 S249C | transitional cell carcinoma | predicted - sensitive | Pemigatinib | Case Reports/Case Series | Actionable | In a Phase I trial (FIGHT-101), Pemazyre (pemigatinib) treatment led to a partial response in a urothelial cancer patient harboring FGFR3 S249C (PMID: 35176457; NCT02393248). | 35176457 |
| FGFR3 S249C | transitional cell carcinoma | predicted - sensitive | Pemigatinib | Phase II | Actionable | In a Phase II trial (FIGHT-201), Pemazyre (pemigatinib) treatment resulted in an objective response rate (ORR) of 17.9% with continuous dosing and 24.2% with intermittent dosing in patients with urothelial carcinoma harboring FGFR3 mutations, with an ORR in patients harboring FGFR3 S249C of 23.9% with continuous dosing (n=46) and 24.6% with intermittent dosing (n=61) (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR3 S249C | Advanced Solid Tumor | predicted - resistant | E7090 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 S249C were resistant to treatment with E7090 in culture (PMID: 34272467). | 34272467 |
| FGFR3 S249C | urinary bladder cancer | predicted - sensitive | Cisplatin + Ipatasertib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Ipatasertib (GDC0068) treatment resulted in enhanced sensitivity of bladder cancer cells expressing FGFR3 S249C to treatment with Platinol (cisplatin) in culture, demonstrating a greater reduction in cell proliferation and increased apoptotic activity when compared to Platinol (cisplatin) alone (PMID: 31316618). | 31316618 |
| FGFR3 S249C | urinary bladder cancer | predicted - sensitive | Cisplatin + LY294002 | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of LY294002 treatment resulted in enhanced sensitivity of bladder cancer cells expressing FGFR3 S249C to treatment with Platinol (cisplatin) in culture, demonstrating a greater reduction in cell proliferation and increased apoptotic activity when compared to Platinol (cisplatin) alone (PMID: 31316618). | 31316618 |
| FGFR3 S249C | bladder carcinoma | sensitive | CPL304110 | Preclinical - Cell culture | Actionable | In a preclinical study, CPL304110 treatment inhibited proliferation of a bladder carcinoma cell line harboring FGFR3 S249C in culture (PMID: 33199155). | 33199155 |
| FGFR3 S249C | urinary bladder cancer | sensitive | CPL304110 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, CPL304110 inhibited Erk phosphorylation in a bladder cancer cell line harboring FGFR3 S249C in culture and inhibited tumor growth in a cell line xenograft model (PMID: 38282676). | 38282676 |
| FGFR3 S249C | transitional cell carcinoma | sensitive | Erdafitinib + Gefitinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, combination treatment with Balversa (erdafitinib) and Iressa (gefitinib) inhibited cell growth of patient-derived urothelial cancer cells harboring FGFR3 S249C and PIK3CA E545A in culture, and led to synergistic inhibition of tumor growth in a patient-derived xenograft (PDX) model (PMID: 37377403). | 37377403 |
| FGFR3 S249C | urinary bladder cancer | sensitive | 3D185 | Preclinical - Cell culture | Actionable | In a preclinical study, 3D185 inhibited downstream signaling and proliferation in a bladder cancer cell line harboring FGFR3 S249C in culture (PMID: 31438996). | 31438996 |
| FGFR3 S249C | urinary bladder cancer | sensitive | Erdafitinib + Quisinostat | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Balversa (erdafitinib) and Quisinostat (JNJ-26481585) synergistically inhibited viability in a bladder cancer cell line harboring FGFR3 S249C in culture (PMID: 37479885). | 37479885 |
| FGFR3 S249C | urinary bladder cancer | predicted - sensitive | TYRA-300 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, TYRA-300 induced tumor regression a cell line xenograft model of bladder cancer harboring FGFR3 S249C (Annals of Oncology 33 (2022): S751). | detail... |
| FGFR3 S249C | adult spinal cord glioblastoma multiforme | predicted - sensitive | Anlotinib + Irinotecan | Case Reports/Case Series | Actionable | In a clinical case study, Anlotinib (AL-3818) and Camptosar (irinotecan) combination treatment resulted in symptom improvement and a partial response maintained for at least 10 months in a patient with IDH wild-type primary spinal cord glioblastoma harboring FGFR3 S249C (PMID: 35847381). | 35847381 |
| FGFR3 S249C | Advanced Solid Tumor | sensitive | Dasatinib + Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Truseltiq (infigratinib) and Sprycel (dasatinib) treatment inhibited viability of a cell line expressing FGFR3 S249C in culture (PMID: 32370101). | 32370101 |
| FGFR3 S249C FGFR3 over exp | transitional cell carcinoma | sensitive | PD173074 | Preclinical | Actionable | In a preclinical study, PD173074 inhibited growth of urothelial carcinoma (UC) cells expressing high levels of FGFR3 S249C, but had reduced efficacy against UC cells with low levels of FGFR3 S249C expression (PMID: 22869148). | 22869148 |
| FGFR3 S249C PIK3CA E545K | bladder urothelial carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, PIK3CA E545K was identified in the post-progression biopsy of a patient with bladder urothelial cancer harboring FGFR3 S249C who progressed on treatment with Balversa (erdafitinib) (PMID: 37377403). | 37377403 |
| FGFR3 S249C PIK3CA E545K | bladder urothelial carcinoma | predicted - resistant | Futibatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with bladder urothelial cancer harboring FGFR3 S249C and an acquired PIK3CA E545K experienced primary resistance to treatment with Lytgobi (futibatinib) (PMID: 37377403). | 37377403 |
| FGFR3 S249C PIK3CA E545K | transitional cell carcinoma | sensitive | Erdafitinib + Pictilisib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, combination treatment with Balversa (erdafitinib) and Pictilisib (GDC-0941) resulted in synergistic inhibition of tumor growth in a patient-derived xenograft (PDX) model of urothelial cancer harboring FGFR3 S249C and PIK3CA E545K (PMID: 37377403). | 37377403 |
| FGFR3 S249C PIK3CA E545A | transitional cell carcinoma | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, Balversa (erdafitinib) treatment resulted in a partial response with a progression-free survival of 5.8 months in a patient with upper tract urothelial carcinoma harboring FGFR3 S249C and PIK3CA E545A (PMID: 37377403). | 37377403 |
| FGFR3 S249C FGFR3 N540K PIK3CA E545K | transitional cell carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 N540K was identified in the post-progression biopsy of a patient with upper tract urothelial carcinoma harboring FGFR3 S249C and PIK3CA E545K who previously responded to Balversa (erdafitinib) treatment (PMID: 37377403). | 37377403 |
| FGFR3 S249C FGFR3 V553L | transitional cell carcinoma | not predictive | Pemigatinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 V553L was identified in the post-progression biopsy of a patient with upper tract urothelial carcinoma harboring FGFR3 S249C who previously responded to Pemazyre (pemigatinib) treatment (PMID: 37377403). | 37377403 |
| FGFR3 S249C FGFR3 V555L | transitional cell carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 V555L was identified in the post-progression circulating tumor DNA of a patient with urothelial cancer harboring FGFR3 S249C who previously responded to Balversa (erdafitinib) treatment (PMID: 37377403). | 37377403 |
| FGFR3 S249C FGFR3 V555L | transitional cell carcinoma | predicted - resistant | Pemigatinib | Case Reports/Case Series | Actionable | In a Phase II trial (FIGHT-201), FGFR3 V555L was identified in post-progression biopsy in a patient with urothelial carcinoma harboring FGFR3 S249C who previously achieved stable disease on Pemazyre (pemigatinib) treatment (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR3 S249C FGFR3 V553M | bladder urothelial carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 V553M was identified in the post-progression circulating tumor DNA of a patient with bladder urothelial cancer harboring FGFR3 S249C who previously responded to Balversa (erdafitinib) treatment (PMID: 37377403). | 37377403 |
| FGFR3 S249C FGFR3 amp PTEN C136fs | transitional cell carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, PTEN C136fs and FGFR3 amplification (6 copies) were identified in the tissue biopsy of a patient with bladder urothelial cancer harboring FGFR3 S249C who progressed on Balversa (erdafitinib) after 1.4 months of treatment (PMID: 37377403). | 37377403 |
| FGFR3 S249C FGFR3 V553M FGFR3 V555L | transitional cell carcinoma | predicted - resistant | Pemigatinib | Case Reports/Case Series | Actionable | In a Phase II trial (FIGHT-201), FGFR3 V553M and V555L were identified in post-progression biopsy in a patient with urothelial carcinoma harboring FGFR3 S249C who previously achieved a partial response on Pemazyre (pemigatinib) treatment (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR3 S249C FGFR3 M528I FGFR3 V553M | transitional cell carcinoma | predicted - resistant | Pemigatinib | Case Reports/Case Series | Actionable | In a Phase II trial (FIGHT-201), FGFR3 V553M and M528I were identified in post-progression biopsy in a patient with urothelial carcinoma harboring FGFR3 S249C who previously achieved a partial response on Pemazyre (pemigatinib) treatment (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR3 S249C FGFR3 N540S | transitional cell carcinoma | predicted - resistant | Pemigatinib | Case Reports/Case Series | Actionable | In a Phase II trial (FIGHT-201), FGFR3 N540S was identified in post-progression biopsy in a patient with urothelial carcinoma harboring FGFR3 S249C who previously achieved stable disease on Pemazyre (pemigatinib) treatment (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR2 R255W FGFR3 S249C FGFR3 V553M FGFR3 K650M | transitional cell carcinoma | predicted - resistant | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 V553M, FGFR3 K650M, and FGFR2 R255W, along with AKT1 E17K, was identified on post-progression biopsy in a patient with urothelial carcinoma harboring FGFR3 S249C who previously responded to Balversa (erdafitinib) (PMID: 37682528). | 37682528 |
| FGFR3 Y375C | urinary bladder cancer | sensitive | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). | 22238366 |
| FGFR3 Y375C | urinary bladder cancer | resistant | Nintedanib | Preclinical | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3 Y375C were resistant to growth inhibition by Ofev (Nintedanib) in culture (PMID: 22238366). | 22238366 |
| FGFR3 Y375C | urinary bladder cancer | sensitive | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited Fgfr phosphorylation and cell proliferation in bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). | 22238366 |
| FGFR3 Y375C | urinary bladder cancer | no benefit | Brivanib | Preclinical | Actionable | In a preclinical study, Brivanib (BMS-540215) did not inhibit growth of bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). | 22238366 |
| FGFR3 Y375C | urinary bladder cancer | resistant | Cediranib | Preclinical | Actionable | In a preclinical study, bladder cancer cells harboring an FGFR3 Y375C mutation were resistant to growth inhibition by Cediranib (AZD-2171) in culture (PMID: 22238366). | 22238366 |
| FGFR3 Y375C | Advanced Solid Tumor | sensitive | Vofatamab | Preclinical - Cell culture | Actionable | In a preclinical study, Vofatamab (B-701) inhibited ligand-dependent proliferation of cells expressing FGFR3 Y375C in culture (PMID: 19381019). | 19381019 |
| FGFR3 R248C | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). | 23786770 |
| FGFR3 R248C | Advanced Solid Tumor | conflicting | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 R248C were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 R248C | Advanced Solid Tumor | conflicting | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). | 23786770 |
| FGFR3 R248C | Advanced Solid Tumor | sensitive | Pazopanib | Preclinical - Cell culture | Actionable | In a preclinical study, Votrient (pazopanib) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). | 23786770 |
| FGFR3 R248C | breast cancer | predicted - sensitive | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (RAGNAR), treatment with Balversa (erdafitinib) resulted in a partial response with a duration of response of 12.75 months in a patient with breast cancer harboring FGFR3 R248C (PMID: 37541273; NCT04083976). | 37541273 |
| FGFR3 R248C | 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 R248C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | 31340094 detail... detail... |
| FGFR3 R248C | 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 R248C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 R248C | urinary bladder cancer | predicted - sensitive | Erdafitinib | Case Reports/Case Series | 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 R248C | Advanced Solid Tumor | sensitive | Vofatamab | Preclinical - Cell culture | Actionable | In a preclinical study, Vofatamab (B-701) inhibited ligand-independent proliferation induced by FGFR3 R248C in cultured cells (PMID: 19381019). | 19381019 |
| FGFR3 R248C | transitional cell carcinoma | sensitive | Dasatinib + Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Sprycel (dasatinib) to treatment with Truseltiq (infigratinib) enhanced inhibition of colony formation and synergistically decreased viability in a urothelial cancer cell line harboring FGFR3 R248C in culture (PMID: 32370101). | 32370101 |
| FGFR3 R248C | transitional cell carcinoma | sensitive | Dasatinib + PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Sprycel (dasatinib) to treatment with PD173074 enhanced inhibition of colony formation of a urothelial cancer cell line harboring FGFR3 R248C in culture (PMID: 32370101). | 32370101 |
| FGFR3 R248C PIK3CA A1066V | urinary bladder cancer | sensitive | Nintedanib + Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Ofev (nintedanib) and Pictilisib (GDC-0941) inhibited cell proliferation in a bladder cancer cell line harboring FGFR3 R248C and PIK3CA A1066V in culture (PMID: 36805958). | 36805958 |
| FGFR3 K650E | Advanced Solid Tumor | decreased response | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to growth inhibition by AZD4547 in culture (PMID: 26992226). | 26992226 |
| FGFR3 K650E | high grade glioma | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase II trial, Truseltiq (infigratinib) treatment resulted in limited efficacy with a 6-month progression-free survival (PFS) rate of 16.0%, a median PFS of 1.7 months, an objective response rate of 4.8% (1/21), and median overall survival of 6.7 months in patients with recurrent gliomas harboring alterations in FGFR1 or FGFR3, however, resulted in stable disease with PFS of 12.9 months in a patient harboring FGFR3 K650E (PMID: 35344029; NCT01975701). | 35344029 |
| FGFR3 K650E | Advanced Solid Tumor | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
| FGFR3 K650E | Advanced Solid Tumor | conflicting | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650E were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 K650E | Advanced Solid Tumor | conflicting | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). | 28034880 |
| FGFR3 K650E | Advanced Solid Tumor | sensitive | Ponatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). | 28034880 |
| FGFR3 K650E | myeloid neoplasm | sensitive | Debio 1347 | Preclinical | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 K650E in culture (PMID: 25169980). | 25169980 |
| FGFR3 K650E | Advanced Solid Tumor | sensitive | Debio 1347 | Preclinical - Cell culture | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). | 28034880 |
| FGFR3 K650E | Advanced Solid Tumor | sensitive | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited proliferation of transformed cells expressing FGFR3 K650E in culture (PMID: 26992226). | 26992226 |
| FGFR3 K650E | Advanced Solid Tumor | sensitive | LY2874455 | Preclinical - Cell culture | Actionable | In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). | 28034880 |
| FGFR3 K650E | myeloid neoplasm | no benefit | SSR128129E | Preclinical | Actionable | In a preclinical study, SSR128129E did not inhibit proliferation of myeloma cells expressing FGFR3 K650E in culture (PMID: 23597562). | 23597562 |
| FGFR3 K650E | Advanced Solid Tumor | sensitive | PD98059 | Preclinical | Actionable | In a preclinical study, PD98059 inhibited FGFR3 K650E-induced transformation of cells in culture (PMID: 14534538). | 14534538 |
| FGFR3 K650E | myeloid neoplasm | sensitive | SU5402 | Preclinical - Cell culture | Actionable | In a preclinical study, SU5402 inhibited proliferation of myeloma cells expressing FGFR3 K650E in culture (PMID: 23597562). | 23597562 |
| FGFR3 K650E | Advanced Solid Tumor | sensitive | FIIN-2 | Preclinical - Cell culture | Actionable | In a preclinical study, FIIN-2 inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). | 28034880 |
| FGFR3 K650E FGFR3 over exp HRAS K117E | multiple myeloma | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 inhibited Fgfr3 signaling, induced cell cycle arrest, and decreased proliferation of multiple myeloma cells harboring HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). | 22869148 |
| FGFR3 K650E FGFR3 over exp HRAS K117E | myeloid neoplasm | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited Fgfr3 signaling and decreased proliferation of myeloma cells with HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). | 22869148 |
| FGFR3 K650M | Advanced Solid Tumor | resistant | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650M were resistant to treatment with AZD4547 in culture (PMID: 34272467). | 34272467 |
| FGFR3 K650M | Advanced Solid Tumor | resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650M were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 K650M | Advanced Solid Tumor | sensitive | PRN1371 | Preclinical - Cell culture | Actionable | In a preclinical study, PRN1371 inhibited proliferation of transformed cells over expressing FGFR3 K650M in culture (PMID: 28978721). | 28978721 |
| FGFR3 K650N | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 K650N | Advanced Solid Tumor | sensitive | Erdafitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with Balversa (erdafitinib) in culture, demonstrating reduced cell viability, and Balversa (erdafitinib) treatment led to inhibition of tumor growth in a cell line xenograft model (PMID: 34272467). | 34272467 |
| FGFR3 K650N | Advanced Solid Tumor | sensitive | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with Lytgobi (futibatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 K650N | Advanced Solid Tumor | sensitive | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with Pemazyre (pemigatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 K650N | Advanced Solid Tumor | sensitive | E7090 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with E7090 in culture, demonstrating reduced cell viability, and E7090 treatment led to inhibition of tumor growth in a cell line xenograft model (PMID: 34272467). | 34272467 |
| FGFR3 K650T | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650T were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 G370C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G370C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G370C | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G370C were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 G370C | 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 G370C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 G370C | 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 G370C is included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 G370C | urinary bladder cancer | predicted - sensitive | Erdafitinib | Case Reports/Case Series | 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 G370C | Advanced Solid Tumor | predicted - resistant | E7090 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G370C were resistant to treatment with E7090 in culture (PMID: 34272467). | 34272467 |
| FGFR3 amp | urinary system cancer | sensitive | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). | 27401245 |
| FGFR3 amp | urinary system cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). | 27401245 |
| FGFR3 amp | Advanced Solid Tumor | predicted - sensitive | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited growth of several tumor cell lines with FGFR alterations in culture (Cancer Res April 15, 2011 71:3560). | detail... |
| FGFR3 amp | Advanced Solid Tumor | predicted - sensitive | Debio 1347 | Phase I | Actionable | In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR3 amp | Advanced Solid Tumor | no benefit | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase II trial (MATCH), Balversa (erdafitinib) treatment resulted in an objective response rate of 0% (0/18), median progression-free survival of 1.7 months, and median overall survival of 4.2 months in patients with advanced solid tumors with FGFR1 (n=12), FGFR2 (n=3), FGFR3 (n=2), or FGFR4 (n=1) amplification (PMID: 38603651; NCT02465060). | 38603651 |
| FGFR3 amp | lung non-small cell carcinoma | sensitive | PRN1371 | Preclinical - Pdx | Actionable | In a preclinical study, PRN1371 treatment resulted in 28.2% tumor growth inhibition in patient-derived xenograft models of FGFR3-amplified non-small cell lung cancer (PMID: 28978721). | 28978721 |
| FGFR3 amp | urinary bladder cancer | sensitive | 3D185 | Preclinical - Cell culture | Actionable | In a preclinical study, 3D185 inhibited proliferation of a bladder cancer cell line harboring FGFR3 amplification in culture (PMID: 31438996). | 31438996 |
| FGFR3 fusion FGFR3 amp | bladder carcinoma | sensitive | CPL304110 | Preclinical - Cell culture | Actionable | In a preclinical study, CPL304110 treatment inhibited proliferation of a bladder carcinoma cell line harboring FGFR3 amplification and an FGFR3 fusion in culture (PMID: 33199155). | 33199155 |
| 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 | Debio 1347 | 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 | 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 | 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 | 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 |
| FGFR3 Y373C FGFR3 over exp | multiple myeloma | sensitive | PD173074 | Preclinical | Actionable | In a preclinical study, PD173074 inhibited Fgfr3 signaling and decreased proliferation and survival of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). | 22869148 |
| FGFR3 Y373C FGFR3 over exp | multiple myeloma | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). | 22869148 |
| FGFR3 Y373C FGFR3 N540K FGFR3 V555L FGFR3 L608V | bladder urothelial carcinoma | predicted - resistant | Futibatinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR3 N540K, FGFR3 V555L, and FGFR3 L608V were identified in the post-progression circulating tumor DNA of a patient with bladder urothelial carcinoma harboring FGFR3 Y373C who previously responded to Lytgobi (futibatinib) treatment (PMID: 37377403). | 37377403 |
| FGFR3 Y373C FGFR3 N540K | transitional cell carcinoma | predicted - resistant | Pemigatinib | Case Reports/Case Series | Actionable | In a Phase II trial (FIGHT-201), FGFR3 N540K was identified in post-progression biopsy in a patient with urothelial carcinoma harboring FGFR3 Y373C who previously achieved stable disease on Pemazyre (pemigatinib) treatment (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR3 S371C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 S371C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 S371C | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 S371C were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 A391E | bladder urothelial carcinoma | predicted - sensitive | AZD4547 | Case Reports/Case Series | 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 single nucleotide variants and a 6-month progression-free survival (PFS) rate of 6%, with stable disease in 2 of 7 patients with FGFR3 activating mutations, and a partial response in a patient with urinary bladder transitional cell carcinoma harboring FGFR3 A391E (reported as A393E) (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 A391E | Advanced Solid Tumor | predicted - sensitive | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 A391E were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 A391E | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 A391E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 A391E | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 A391E were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 A391E | Advanced Solid Tumor | predicted - sensitive | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 A391E were sensitive to treatment with Balversa (erdafitinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 A391E | Advanced Solid Tumor | predicted - sensitive | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 A391E were sensitive to treatment with Pemazyre (pemigatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G380R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G380R | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380R were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 G380R | Advanced Solid Tumor | predicted - sensitive | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380R were sensitive to treatment with Balversa (erdafitinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G380R | Advanced Solid Tumor | predicted - sensitive | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380R were sensitive to treatment with Pemazyre (pemigatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 F386L | myeloid neoplasm | sensitive | Debio 1347 | Preclinical | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of myeloma cell lines harboring FGFR3 F386L in culture (PMID: 25169980). | 25169980 |
| FGFR3 over exp | transitional cell carcinoma | sensitive | AZD4547 | Preclinical | Actionable | In a preclinical study, AZD4547 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). | 22869148 |
| FGFR3 over exp | urinary bladder cancer | sensitive | Infigratinib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with Truseltiq (infigratinib) led to improved progression-free survival in a patient-derived xenograft (PDX) model of bladder cancer with FGFR3 over expression (PMID: 26270481). | 26270481 |
| FGFR3 over exp | urinary bladder cancer | sensitive | Dovitinib | Phase II | Actionable | In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 8% (1/13) of non-muscle invasive bladder cancer patients over expressing FGFR3 (J Clin Oncol 34, 2016 (suppl; abstr 4526)). | detail... |
| FGFR3 over exp | urinary bladder cancer | sensitive | Dactolisib + Sorafenib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of BEZ235 and Nexavar (sorafenib) resulted in improved progression-free survival in an FGFR3-over expressing patient-derived xenograft (PDX) model of bladder cancer with secondary resistance to BGJ398 due to reactivation of downstream signaling, as evidenced by increased activation of Akt and Erk (PMID: 26270481). | 26270481 |
| FGFR3 over exp | transitional cell carcinoma | no benefit | Rogaratinib | Phase II | Actionable | In a Phase II trial (FORT-1), Rogaratinib (BAY 1163877) treatment did not result in improved outcomes compared to chemotherapy in advanced or metastatic urothelial carcinoma patients with FGFR1 or FGFR3 overexpression, with similar median overall survival (8.3 mo vs 9.8 mo), median progression-free survival (2.7 mo vs. 3.2 mo), and objective response rate (20.7% (18/87) vs 19.3% (17/88)), failing to meet the predetermined criteria for continuation to Phase III (PMID: 36240478; NCT03410693). | 36240478 |
| FGFR3 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 |
| FGFR3 over exp | head and neck squamous cell carcinoma | sensitive | Rogaratinib | Preclinical | Actionable | In a preclinical study, Rogaratinib (BAY 1163877) inhibited tumor growth in a head and neck squamous cell carcinoma xenograft model with FGFR3 overexpression (Cancer Res August 1, 2015 75:772). | detail... |
| FGFR3 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 |
| FGFR3 over exp | Advanced Solid Tumor | sensitive | LY2874455 | Preclinical | Actionable | In a preclinical study, LY2874455 induced tumor regression in FGFR3-over expressing bladder and multiple myeloma xenograft models (PMID: 21900693). | 21900693 |
| FGFR3 over exp | glioblastoma | sensitive | U0126 | Preclinical | Actionable | In a preclinical study, U0126 inhibited downstream signaling and growth of glioblastoma cells over-expressing Fgfr3 in culture (PMID: 23298836). | 23298836 |
| FGFR3 over exp | multiple myeloma | sensitive | Vofatamab | Phase I | Actionable | In a Phase I trial, Vofatamab (B-701) demonstrated safety and resulted in stable disease in 42% (6/14) of multiple myeloma patients overexpressing FGFR3 (Blood (ASH Annual Meeting Abstracts) 2012 120: Abstract 4029). | detail... |
| FGFR3 over exp | transitional cell carcinoma | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). | 22869148 |
| FGFR3 over exp | urinary bladder cancer | sensitive | SU5402 | Preclinical | Actionable | In a preclinical study, SU5402 inhibited growth of bladder cancer cells over expressing wild-type FGFR3 in culture (PMID: 21119661). | 21119661 |
| FGFR3 over exp | Advanced Solid Tumor | sensitive | PRN1371 | Preclinical - Cell culture | Actionable | In a preclinical study, PRN1371 inhibited proliferation in transformed cells overexpressing wild-type FGFR3 in culture (PMID: 28978721). | 28978721 |
| FGFR3 G384D FGFR3 over exp | multiple myeloma | decreased response | AZD4547 | Preclinical | Actionable | In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZD4547 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). | 22869148 |
| FGFR3 G384D FGFR3 over exp | multiple myeloma | decreased response | PD173074 | Preclinical | Actionable | In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to PD173074 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). | 22869148 |
| FGFR3 G384D FGFR3 over exp | multiple myeloma | decreased response | AZ8010 | Preclinical | Actionable | In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZ8010 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). | 22869148 |
| FGFR3 positive | lung squamous cell carcinoma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR3-positive lung squamous cell carcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR3 positive | lung adenocarcinoma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR3-positive lung adenocarcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR3 positive | head and neck squamous cell carcinoma | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including a partial response in a patient with FGFR3-positive head and neck squamous cell carcinoma (PMID: 31405822; NCT01976741). | 31405822 |
| FGFR3 positive | stomach cancer | predicted - sensitive | Rogaratinib | Case Reports/Case Series | Actionable | In a Phase I trial, sensitivity to treatment with Rogaratinib (BAY 1163877) was demonstrated in patients with a variety of FGFR-expressing solid tumor types, including long lasting stable disease in a patient with FGFR3-positive gastric cancer (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR2 pos FGFR3 pos | breast carcinoma | sensitive | E7090 | Preclinical | Actionable | In a preclinical study, a mouse breast carcinoma cell line xenograft model demonstrated inhibition of tumor growth when treated with E7090, a result of decreased FGFR2 and FGFR3 activity (PMID: 27535969). | 27535969 |
| FGFR3 fusion | urinary bladder cancer | sensitive | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 fusion in culture (PMID: 27550940). | 27550940 |
| FGFR3 fusion | transitional cell carcinoma | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, Truseltiq (infigratinib) treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517)). | detail... |
| FGFR3 fusion | urinary bladder cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, bladder cancer cell lines harboring an FGFR3 fusion were sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth (PMID: 33563752). | 33563752 |
| FGFR3 fusion | Advanced Solid Tumor | predicted - sensitive | Debio 1347 | Phase I | Actionable | In a Phase I trial, Debio 1347 treatment resulted in partial response in 10.5% (6/57) and stable disease in 28.1% (16/57) of patients with advanced solid tumors harboring genomic alterations of FGFR1/2/3, including amplifications, fusions, and mutations (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR3 fusion | transitional cell carcinoma | predicted - sensitive | Erdafitinib | Phase I | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in an objective response rate of 46% (12/26) in patients with urothelial carcinoma harboring FGFR genomic alterations, including 17 with FGFR3 mutations, and 11 with FGFR2 and/or FGFR3 fusions (PMID: 31088831; NCT01703481). | 31088831 |
| FGFR3 fusion | bladder urothelial carcinoma | sensitive | 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 |
| FGFR3 fusion | 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 |
| FGFR3 fusion | Advanced Solid Tumor | predicted - sensitive | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Lytgobi (futibatinib) demonstrated growth inhibition and reduced FGFR phosphorylation in human cancer cell lines and xenograft models harboring FGFR mutations (Mol Cancer Ther 2013;12(11 Suppl):A270). | detail... |
| FGFR3 fusion | transitional cell carcinoma | sensitive | Pemigatinib | Phase II | Actionable | In a Phase II trial (FIGHT-201), Pemazyre (pemigatinib) treatment resulted in an objective response rate (ORR) of 17.8%, median duration of response (mDOR) of 6.2 mo, median progression-free survival (mPFS) of 4.0 mo, and median overall survival (mOS) of 6.8 mo with continuous dosing, and an ORR of 23.3%, mDOR of 6.2 mo, mPFS of 4.3 mo, and mOS of 8.9 mo with intermittent dosing in patients with urothelial carcinoma harboring FGFR3 mutations or fusions/rearrangements (PMID: 37956738; NCT02872714). | 37956738 |
| FGFR3 fusion | transitional cell carcinoma | predicted - sensitive | Docetaxel + Vofatamab | Phase Ib/II | Actionable | In a Phase I/II trial, Vofatamab (B-701) in combination with Taxotere (docetaxel) demonstrated safety and preliminary efficacy, resulted in enhanced activity in patients with locally advanced or metastatic urothelial carcinoma harboring FGFR3 mutations or fusions comparing to wild-type patients (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 4534-4534; NCT02401542). | detail... |
| FGFR3 fusion | transitional cell carcinoma | predicted - sensitive | ABSK061 | Phase I | Actionable | In a Phase I trial, ABSK061 treatment resulted in a partial response in a patient with urothelial carcinoma harboring an FGFR3 fusion (ESMO Open 9 (2024): 102274); NCT05244551). | detail... |
| FGFR3 V555M | Advanced Solid Tumor | resistant | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to AZD4547 in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555M | transitional cell carcinoma | resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with Truseltiq (infigratinib) and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) (PMID: 29848605). | 29848605 |
| FGFR3 V555M | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555M | Advanced Solid Tumor | sensitive | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555M | Advanced Solid Tumor | sensitive | Ponatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555M | Advanced Solid Tumor | decreased response | Debio 1347 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 V555M demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555M | Advanced Solid Tumor | sensitive | LY2874455 | Preclinical - Cell culture | Actionable | In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555M | Advanced Solid Tumor | resistant | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing FGFR3 V555M was resistant to Pemazyre (pemigatinib) in a kinase assay and in culture (PMID: 36698015). | 36698015 |
| FGFR3 V555M | Advanced Solid Tumor | decreased response | FIIN-2 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 V555M demonstrated reduced sensitivity to FIIN-2 in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555M FGFR3 L608V | transitional cell carcinoma | predicted - resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with Truseltiq (infigratinib) and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) and FGFR3 L608V (also corresponds to L496V) (PMID: 29848605). | 29848605 |
| FGFR3 N540K | Advanced Solid Tumor | resistant | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 N540K were reistant to growth inhibition by AZD4547 in culture (PMID: 26992226). | 26992226 |
| FGFR3 N540K | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 N540K were resistant to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
| FGFR3 N540K | Advanced Solid Tumor | sensitive | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 N540K in culture (PMID: 28034880). | 28034880 |
| FGFR3 N540K | Advanced Solid Tumor | sensitive | Ponatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 N540K in culture (PMID: 28034880). | 28034880 |
| FGFR3 N540K | Advanced Solid Tumor | decreased response | Debio 1347 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). | 28034880 |
| FGFR3 N540K | Advanced Solid Tumor | sensitive | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinicl study, Balversa (erdafitinib) inhibited proliferation of transformed cells expressing FGFR3 N540K in culture (PMID: 26992226). | 26992226 |
| FGFR3 N540K | Advanced Solid Tumor | decreased response | LY2874455 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to LY2874455 in culture (PMID: 28034880). | 28034880 |
| FGFR3 N540K | Advanced Solid Tumor | decreased response | FIIN-2 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 N540K demonstrated reduced sensitivity to FIIN-2 in culture (PMID: 28034880). | 28034880 |
| FGFR3 D788N | head and neck squamous cell carcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D788N in culture, however, cells expressing FGFR3 D788N did not demonstrate increased sensitivity to Truseltiq (infigratinib) compared to cells expressing wild-type FGFR3 (PMID: 27053219). | 27053219 |
| FGFR3 S131L | head and neck squamous cell carcinoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line expressing FGFR3 S131L demonstrated decreased sensitivity to Truseltiq (infigratinib) compared to cells expressing wild-type FGFR3 in culture (PMID: 27053219). | 27053219 |
| FGFR3 L608V | Advanced Solid Tumor | decreased response | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to AZD4547 in culture (PMID: 28034880). | 28034880 |
| FGFR3 L608V | Advanced Solid Tumor | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
| FGFR3 L608V | Advanced Solid Tumor | sensitive | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). | 28034880 |
| FGFR3 L608V | Advanced Solid Tumor | sensitive | Ponatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). | 28034880 |
| FGFR3 L608V | Advanced Solid Tumor | decreased response | Debio 1347 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to Debio 1347 in culture (PMID: 28034880). | 28034880 |
| FGFR3 L608V | Advanced Solid Tumor | sensitive | LY2874455 | Preclinical - Cell culture | Actionable | In a preclinical study, LY2874455 inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). | 28034880 |
| FGFR3 L608V | Advanced Solid Tumor | sensitive | FIIN-2 | Preclinical - Cell culture | Actionable | In a preclinical study, FIIN-2 inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). | 28034880 |
| FGFR3 V555L | transitional cell carcinoma | resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical study, two patients with metastatic urothelial carcinoma progressed while being treated with Truseltiq (infigratinib) and subsequent cell-free DNA testing revealed FGFR3 V555L (also corresponds to V443L) (PMID: 29848605). | 29848605 |
| FGFR3 V555L | Advanced Solid Tumor | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 V555L demonstrated reduced sensitivity to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
| FGFR3 G372C | Advanced Solid Tumor | sensitive | Vofatamab | Preclinical - Cell culture | Actionable | In a preclinical study, Vofatamab (B-701) inhibited ligand-dependent proliferation in cells expressing FGFR3 G372C (PMID: 19381019). | 19381019 |
| FGFR3 D764H | head and neck squamous cell carcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D764H in culture, however, cells expressing FGFR3 D764H did not demonstrate increased sensitivity to Truseltiq (infigratinib) compared to cells expressing wild-type FGFR3 (PMID: 27053219). | 27053219 |
| FGFR3 P573S | lung non-small cell carcinoma | no benefit | AZD4547 | Case Reports/Case Series | Actionable | In a Phase II trial (NLMT), AZD4547 treatment did not result in a confirmed response or durable clinical benefit in a patient with non-small cell lung cancer harboring FGFR3 P575S (corresponds to P573S in the canonical isoform (PMID: 32669708, NCT02664935). | 32669708 |
| FGFR3 S756P | lung non-small cell carcinoma | no benefit | AZD4547 | Case Reports/Case Series | Actionable | In a Phase II trial (NLMT), AZD4547 treatment did not result in a confirmed response or durable clinical benefit in a patient with non-small cell lung cancer harboring FGFR3 S758P (corresponds to S756P in the canonical isoform (PMID: 32669708, NCT02664935). | 32669708 |
| FGFR3 G380E | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G380E | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380E were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 G380E | Advanced Solid Tumor | predicted - sensitive | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380E were sensitive to treatment with Balversa (erdafitinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G380E | Advanced Solid Tumor | predicted - sensitive | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380E were sensitive to treatment with Pemazyre (pemigatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 R248_S249insC | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 R248_S249insC were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 R248_S249insC | Advanced Solid Tumor | predicted - resistant | E7090 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 R248_S249insC were resistant to treatment with E7090 in culture (PMID: 34272467). | 34272467 |
| FGFR3 H284fs | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 H284fs (FGFR3 H284fs*10) were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 H284fs | Advanced Solid Tumor | predicted - resistant | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 H284fs (FGFR3 H284fs*10) were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 H284fs | Advanced Solid Tumor | predicted - resistant | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 H284fs (FGFR3 H284fs*10) were resistant to treatment with Pemazyre (pemigatinib) in culture (PMID: 34272467). | 34272467 |
| FGFR3 H284fs | Advanced Solid Tumor | predicted - resistant | E7090 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 H284fs (FGFR3 H284fs*10) were resistant to treatment with E7090 in culture (PMID: 34272467). | 34272467 |
| FGFR3 N542K | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cell line expressing FGFR3 N542K in culture (PMID: 32370101). | 32370101 |
| FGFR3 N542K | Advanced Solid Tumor | sensitive | Dasatinib + Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Truseltiq (infigratinib) and Sprycel (dasatinib) treatment inhibited viability of a cell line expressing FGFR3 N542K in culture (PMID: 32370101). | 32370101 |
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