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| Profile Name | FGFR3 - TACC3 |
| Gene Variant Detail | |
| Relevant Treatment Approaches | FGFR Inhibitor (Pan) FGFR3 Inhibitor U0126 |
| Molecular Profile | Indication/Tumor Type | Response Type | Relevant Treatment Approaches | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|---|
| FGFR3 N540K | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | resistant | FGFR3 Inhibitor | 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 | sensitive | FGFR Inhibitor (Pan) | 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 | sensitive | FGFR Inhibitor (Pan) | 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 | decreased response | FGFR3 Inhibitor | 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 | resistant | FGFR Inhibitor (Pan) | 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 | decreased response | FGFR Inhibitor (Pan) | 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 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 | urinary bladder cancer | resistant | FGFR Inhibitor (Pan) | 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 | FGFR3 Inhibitor | 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 wild-type | myeloid neoplasm | sensitive | FGFR Inhibitor (Pan) | SSR128129E | Preclinical | Actionable | In a preclinical study, SSR128129E 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 | FGFR3 Inhibitor | 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 | FGFR3 Inhibitor | 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 | FGFR3 Inhibitor | 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 - TACC3 | gallbladder cancer | predicted - sensitive | FGFR3 Inhibitor | Debio 1347 | Case Reports/Case Series | Actionable | In a Phase I trial, Debio 1347 treatment resulted in stable disease in a patient with gallbladder cancer harboring FGFR3-TACC3 (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | ODM-203 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ODM-203 inhibited FGFR signaling and proliferation in a bladder cancer cell line harboring FGFR3-TACC3 and inhibited tumor growth in xenograft models (PMID: 30301864). | 30301864 |
| FGFR3 - TACC3 | glioblastoma | sensitive | U0126 | U0126 | Preclinical | Actionable | In a preclinical study, U0126 inhibited downstream signaling and growth of glioblastoma cells expressing the FGFR3-TACC3 fusion in culture (PMID: 23298836). | 23298836 |
| FGFR3 - TACC3 | cervical squamous cell carcinoma | predicted - sensitive | FGFR3 Inhibitor | AZD4547 | Case Reports/Case Series | Actionable | In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with squamous cell carcinoma of the cervix harboring FGFR3-TACC3, with a 40% reduction in target lesion size and a progression-free survival of 4 months (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 - TACC3 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | PRN1371 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PRN1371 inhibited proliferation of bladder transitional cell carcinoma cell lines harboring FGFR3-TACC3 fusion in culture and tumor growth in cell line xenograft models (PMID: 28978721). | 28978721 |
| FGFR3 - TACC3 | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3-TACC3 were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | Pazopanib | Preclinical | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3-TACC3 demonstrated sensitivity to Votrient (pazopanib) in culture (PMID: 23558953). | 23558953 |
| FGFR3 - TACC3 | lung non-small cell carcinoma | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Preclinical - Pdx | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited pERK signaling and tumor growth in a patient-derived xenograft (PDX) model of non-small cell lung cancer harboring FGFR3-TACC3 (PMID: 28341788). | 28341788 |
| FGFR3 - TACC3 | transitional cell carcinoma | sensitive | FGFR3 Inhibitor | AZD4547 + Buparlisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) worked synergistically to induce apoptosis and inhibit growth of a urothelial cell carcinoma cell line harboring FGFR3-TACC3 in culture, and inhibited tumor growth in xenograft models, with increased efficacy over either agent alone (PMID: 28108151). | 28108151 |
| FGFR3 - TACC3 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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-TACC3 v1 and v3 fusions are included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 - TACC3 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in partial response in 2 urothelial cancer patients harboring FGFR3-TACC3 (PMID: 26324363; NCT01703481). | 26324363 |
| FGFR3 - TACC3 | stomach cancer | predicted - sensitive | FGFR Inhibitor (Pan) | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Futibatinib (TAS-120) treatment led to an overall objective response rate of 22% (2/9, 2 partial responses) and a disease control rate of 55.6% (5/9) in patients with gastric cancer harboring an FGFR2 amplification or FGFR3 rearrangement, including a partial response with a progression-free survival of 6.7 months and a duration of response of 5.4 months in a gastric cancer patient harboring FGFR3-TACC3 (PMID: 34551969; NCT02052778). | 34551969 |
| FGFR3 - TACC3 | transitional cell carcinoma | predicted - sensitive | FGFR3 Inhibitor | AZD4547 | Case Reports/Case Series | Actionable | In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with urothelial carcinoma harboring FGFR3-TACC3, with a 70% reduction in target lesions and a progression-free survival of 10.9 months (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ12908010 (AZ8010) induced cell cycle arrest and inhibited proliferation of urothelial cancer cell lines that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 22869148, PMID: 23175443). | 22869148 23175443 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | E7090 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, urinary bladder cancer cells harboring FGFR3-TACC3 demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability, and antitumor activity in xenograft models (PMID: 27535969). | 27535969 |
| FGFR3 - TACC3 | high grade glioma | sensitive | FGFR3 Inhibitor | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited Fgfr3 kinase activity in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture (PMID: 22837387). | 22837387 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited growth of bladder cancer cell lines that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 24325461, PMID: 23175443). | 23175443 24325461 |
| FGFR3 - TACC3 | high grade glioma | sensitive | FGFR Inhibitor (Pan) | Infigratinib | Preclinical - Pdx | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment inhibited tumor growth in a patient-derived xenograft (PDX) model of glioma harboring FGFR3-TACC3 (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). | detail... |
| FGFR3 - TACC3 | high grade glioma | sensitive | FGFR Inhibitor (Pan) | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited Fgfr3 kinase activity in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture (PMID: 22837387). | 22837387 |
| FGFR3 - TACC3 | high grade glioma | sensitive | FGFR Inhibitor (Pan) | 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 glioma harboring alterations in FGFR1 or FGFR3, however, resulted in stable disease with PFS of 30.2 months in a patient harboring FGFR3-TACC3 (PMID: 35344029; NCT01975701). | 35344029 |
| FGFR3 - TACC3 | urinary bladder cancer | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in a partial response with 38% shrinkage of tumor in a patient with metastatic bladder cancer harboring FGFR3-TACC3, who stayed on treatment for 10 months (PMID: 28416604; NCT01703481). | 28416604 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | PD173074 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Votrient (pazopanib) inhibited tumor growth in cell line xenograft models of bladder cancer harboring FGFR3-TACC3 (PMID: 23558953). | 23558953 |
| FGFR3 - TACC3 | high grade glioma | sensitive | FGFR3 Inhibitor | PD173074 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PD173074 inhibited Fgfr3 kinase activity and growth in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture and in cell line xenograft models (PMID: 22837387). | 22837387 |
| FGFR3 - TACC3 | transitional cell carcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | Alpelisib + Infigratinib | Phase I | Actionable | In a Phase Ib trial, Truseltiq (infigratinib) and Alpelisib (BYL719) combination treatment resulted in partial response and a complete shrinkage of target lesions lasting 4 months in one urothelial carcinoma patient harboring a FGFR3-TACC3 fusion (J Clin Oncol 34, 2016 (suppl; abstr 2500)). | detail... |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | FIIN-1 | Preclinical | Actionable | In a preclinical study, FIIN-1 inhibited growth of the RT4 bladder cancer cell line, which has been demonstrated to harbor an FGFR3-TACC3 fusion, in culture (PMID: 20338520, PMID: 23175443). | 23175443 20338520 |
| FGFR3 - TACC3 | bladder transitional cell papilloma | no benefit | RO4987655 | Preclinical - Cell culture | Actionable | In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO4987655 in culture (PMID: 26438159). | 26438159 | |
| FGFR3 - TACC3 | lung adenocarcinoma | sensitive | FGFR Inhibitor (Pan) | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatanib) inhibited growth and FGFR3 phosphorylation in cells expressing FGFR3-TACC3 fusion in culture (PMID: 25294908). | 25294908 |
| FGFR3 - TACC3 | lung adenocarcinoma | sensitive | FGFR Inhibitor (Pan) | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth and FGFR3 phosphorylation in cells expressing FGFR3-TACC3 fusion in culture (PMID: 25294908). | 25294908 |
| FGFR3 - TACC3 | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3-TACC3 were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 - TACC3 | central nervous system cancer | predicted - sensitive | FGFR3 Inhibitor | Debio 1347 | Case Reports/Case Series | Actionable | In a clinical case study, Debio 1347 treatment resulted in a prolonged stable disease and stable clinical symptoms at 26 months in a pediatric patient with a right cerebellar hemispheric rosette-forming glioneuronal tumor harboring an FGFR3-TACC3 fusion (PMID: 34250399). | 34250399 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | SU5402 | Preclinical | Actionable | In a preclinical study, SU5402 induced cell-cycle arrest and inhibited proliferation of bladder cancer cells that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 21119661, PMID: 23175443). | 21119661 23175443 |
| FGFR3 - TACC3 | Advanced Solid Tumor | predicted - sensitive | HQP1351 | Preclinical - Cell culture | Actionable | In a preclinical study, GZD824 (HQP1351) inhibited growth of a cell line harboring FGFR3-TACC3 fusion in culture (PMID: 34114373). | 34114373 | |
| FGFR3 - TACC3 | urinary bladder cancer | no benefit | Selumetinib | Preclinical | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3-TACC were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). | 26438159 | |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | LY2874455 | Preclinical | Actionable | In a preclinical study, LY2874455 induced tumor regression in bladder cancer xenograft models that have been demonstrated to harbor an FGFR3-TACC3 fusion (PMID: 21900693, PMID: 23175443). | 21900693 23175443 |
| FGFR3 - TACC3 | bladder transitional cell papilloma | no benefit | RO5126766 | Preclinical - Cell culture | Actionable | In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO5126766 in culture (PMID: 26438159). | 26438159 | |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | BO-264 | Preclinical - Cell culture | Actionable | In a preclinical study, BO-264 treatment inhibited Erk1/2 phosphorylation, induced mitotic arrest, and reduced viability of a urinary bladder cancer cell line harboring FGFR3-TACC3 in culture (PMID: 32217742). | 32217742 | |
| FGFR3 - TACC3 | transitional cell carcinoma | predicted - sensitive | FGFR3 Inhibitor | Debio 1347 | Case Reports/Case Series | Actionable | In a Phase I trial, Debio 1347 treatment resulted in partial response in two patients with urothelial cancer harboring FGFR3-TACC3 (PMID: 30745300; NCT01948297). | 30745300 |
| FGFR3 - TACC3 | Advanced Solid Tumor | sensitive | FGFR3 Inhibitor | AZD4547 | Phase II | Actionable | In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in 22% (2/9) and stable disease in 55% (5/9) of patients with advanced solid tumors harboring FGFR fusions, with a 6-month progression-free survival rate of 56%, including partial responses in 2 patients and stable disease for greater than 6 months in 1 of 8 patients harboring FGFR3-TACC3 (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 - TACC3 | Advanced Solid Tumor | sensitive | FGFR3 Inhibitor | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited proliferation of transformed cells expressing FGFR3-TACC3 in culture (PMID: 26992226). | 26992226 |
| FGFR3 - TACC3 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited proliferation of transformed cells FGFR3-TACC3 in culture (PMID: 26992226). | 26992226 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | ASP5878 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, ASP5878 treatment inhibited proliferation of bladder cancer cell lines harboring a FGFR3-TACC3 fusion in culture, and resulted in tumor regression in a FGFR3-TACC3 positive bladder cancer cell line xenograft model (Mol Cancer Ther December 2015 14; A170). | detail... |
| FGFR3 - TACC3 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | 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-TACC3 v1 and v3 fusions are included in the companion diagnostic (PMID: 31340094; NCT02365597). | detail... 31340094 detail... |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cell lines harboring FGFR3-TACC3 fusion in culture (PMID: 27627808). | 27627808 | |
| FGFR3 - TACC3 | glioblastoma | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Case Reports/Case Series | Actionable | In a clinical study, Balversa (erdafitinib) treatment resulted in tumor reduction and stable disease in 2 glioblastoma multiforme patients harboring FGFR3-TACC3 fusion (PMID: 25609060). | 25609060 |
| FGFR3 - TACC3 | glioblastoma | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in partial response in a glioblastoma patient harboring FGFR3-TACC3 fusion (PMID: 26324363; NCT01703481). | 26324363 |
| FGFR3 - TACC3 | urinary bladder cancer | predicted - sensitive | FGFR3 Inhibitor | S-49076 | Preclinical | Actionable | In a preclinical study, S-49076 inhibited autophosphorylation of FGFR3 and downstream signaling in bladder cancer cells that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 23804704, PMID: 23175443). | 23175443 23804704 |
| FGFR3 - TACC3 | high grade glioma | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited proliferation of glioma cells harboring FGFR3-TACC3 fusion in culture and xenograft tumor growth in animal models (PMID: 25609060). | 25609060 |
| FGFR3 - TACC3 | oligodendroglioma | sensitive | FGFR Inhibitor (Pan) | PRN1371 | Preclinical - Pdx | Actionable | In a preclinical study, PRN1371 treatment resulted in tumor regression in patient-derived xenograft models of anaplastic oligodendroglioma harboring FGFR3-TACC3 fusion (PMID: 28978721). | 28978721 |
| FGFR3 - TACC3 | urinary bladder cancer | predicted - sensitive | FGFR Inhibitor (Pan) | Infigratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment inhibited tumor growth and Erk phosphorylation in a cell line xenograft model of bladder cancer harboring FGFR3-TACC3 (Cancer Res 2019;79(13 Suppl):Abstract nr 2206). | detail... |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | Debio 1347 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of bladder cancer cell lines harboring an FGFR3-TACC3 fusion in culture and inhibited tumor growth in FGFR3-TACC3-positive bladder cancer cell line xenograft models (PMID: 25169980). | 25169980 |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | Vofatamab | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Vofatamab (B-701) inhibited FGFR3 signaling and tumor growth in bladder cancer cell line xenograft models harboring FGFR3-TACC3 (PMID: 25326231). | 25326231 | |
| FGFR3 - TACC3 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | PRN1109 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PRN1109 treatment resulted in tumor regression in bladder cancer cell line xenograft models harboring FGFR3-TACC3 fusion (Eu J Cancer 2014 Vol 50, Suppl 6:157). | detail... |
| FGFR2 - CCDC6 FGFR3 - TACC3 | adrenal carcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Case Reports/Case Series | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted tumor shrinkage and no disease progression for 10 months in an adrenal carcinoma patient harboring FGFR3-TACC3 and FGFR2-CCDC6 fusions (PMID: 26324363; NCT01703481). | 26324363 |
| FGFR3 - TACC3 FGFR3 over exp | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in bladder cancer cell lines with FGFR3 overexpression and harboring FGFR3-TACC3 in culture, and led to inhibition of tumor growth in a cell line xenograft model (PMID: 32973082). | 32973082 |
| FGFR3 Y373C | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | 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 | myeloid neoplasm | sensitive | FGFR3 Inhibitor | 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 | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | 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 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | predicted - resistant | FGFR3 Inhibitor | 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 | 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 | 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 | 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 | multiple myeloma | sensitive | FGFR3 Inhibitor | 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 FGFR3 over exp | multiple myeloma | sensitive | FGFR3 Inhibitor | 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 over exp | multiple myeloma | sensitive | FGFR3 Inhibitor | 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 rearrange FGFR3 Y373C | multiple myeloma | sensitive | FGFR Inhibitor (Pan) | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Futibatinib (TAS-120) 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 V555M | transitional cell carcinoma | resistant | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | FGFR3 Inhibitor | 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 | Advanced Solid Tumor | decreased response | FGFR3 Inhibitor | 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 | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | resistant | FGFR Inhibitor (Pan) | 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 Y375C | urinary bladder cancer | resistant | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | sensitive | FGFR Inhibitor (Pan) | 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 | 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 K650T | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | 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 V555L | Advanced Solid Tumor | decreased response | FGFR Inhibitor (Pan) | 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 V555L | transitional cell carcinoma | resistant | FGFR Inhibitor (Pan) | 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 fusion | transitional cell carcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | 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 | 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 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | 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 | 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 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | Futibatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, TAS-120 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 | Advanced Solid Tumor | predicted - sensitive | FGFR3 Inhibitor | 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 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with advanced or metastatic bladder urothelial carcinoma harboring FGFR alterations (PMID: 34861372; ESMO.org). | detail... 34861372 |
| FGFR3 fusion FGFR3 amp | bladder carcinoma | sensitive | FGFR3 Inhibitor | 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 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 | 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 | renal pelvis transitional cell carcinoma | predicted - sensitive | FGFR3 Inhibitor | 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 | 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 | urinary bladder cancer | resistant | FGFR Inhibitor (Pan) | 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 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | 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 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | 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 | renal pelvis transitional cell carcinoma | predicted - sensitive | FGFR3 Inhibitor | 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 FGFR2 S249C (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 S249C | urinary system cancer | sensitive | FGFR Inhibitor (Pan) | 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 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | 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 | transitional cell carcinoma | predicted - sensitive | FGFR3 Inhibitor | 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 | 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 | 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 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | 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 | transitional cell carcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | Futibatinib | Case Reports/Case Series | Actionable | In a Phase I trial, Futibatinib (TAS-120) 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 | 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 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | conflicting | FGFR Inhibitor (Pan) | 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 | urinary system cancer | sensitive | FGFR3 Inhibitor | 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 | bladder carcinoma | sensitive | FGFR3 Inhibitor | 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 | 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 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | 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 | Advanced Solid Tumor | predicted - resistant | FGFR3 Inhibitor | 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 FGFR3 over exp | transitional cell carcinoma | sensitive | FGFR3 Inhibitor | 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 G384D FGFR3 over exp | multiple myeloma | decreased response | FGFR3 Inhibitor | 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 G384D FGFR3 over exp | multiple myeloma | decreased response | FGFR3 Inhibitor | 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 | FGFR3 Inhibitor | 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 A391E | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | bladder urothelial carcinoma | predicted - sensitive | FGFR3 Inhibitor | 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 | FGFR3 Inhibitor | 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 A391E | Advanced Solid Tumor | predicted - sensitive | FGFR3 Inhibitor | 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 | FGFR Inhibitor (Pan) | 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 rearrange | myeloid neoplasm | sensitive | FGFR Inhibitor (Pan) | 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 | myeloid neoplasm | sensitive | FGFR3 Inhibitor | 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 FGFR3 K650E | multiple myeloma | predicted - sensitive | FGFR Inhibitor (Pan) | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Futibatinib (TAS-120) 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 NRAS act mut | multiple myeloma | no benefit | FGFR Inhibitor (Pan) | 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 Futibatinib (TAS-120) in culture (PMID: 32973082). | 32973082 |
| FGFR3 rearrange FGFR3 F384L | multiple myeloma | no benefit | FGFR Inhibitor (Pan) | 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 Futibatinib (TAS-120) in culture (PMID: 32973082). | 32973082 |
| FGFR3 G380R | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | 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 | FGFR3 Inhibitor | 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 G380R | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 P573S | lung non-small cell carcinoma | no benefit | FGFR3 Inhibitor | 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 D788N | head and neck squamous cell carcinoma | no benefit | FGFR Inhibitor (Pan) | 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 over exp | urinary bladder cancer | sensitive | FGFR3 Inhibitor | 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 | head and neck squamous cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 | transitional cell carcinoma | sensitive | FGFR3 Inhibitor | 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 | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | Rogaratinib | Phase I | Actionable | In a Phase I trial, treatment with Rogaratinib (BAY 1163877) was well-tolerated and resulted in objective response rate (ORR) of 15% (15/100) in patients with FGFR1, FGFR2, or FGFR3-overexpressing advanced solid tumors, including urothelial cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer, and led to an ORR of 67% (10/15) in patients with FGFR overexpression, but without an FGFR genetic aberration (PMID: 31405822). | 31405822 |
| 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 | sensitive | FGFR3 Inhibitor | 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 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 | lung squamous cell carcinoma | no benefit | FGFR Inhibitor (Pan) | Rogaratinib | Phase II | Actionable | In a Phase II trial, Rogaratinib (BAY 1163877) treatment did not result in improved progression-free survival (PFS) of metastatic lung squamous cell carcinoma patients with overexpression of FGFR1, FGFR2, or FGFR3, as only 10% (1/10) of patients achieved 6-month PFS, further clinical development of this agent was halted (J Clin Oncol 39, no. 15_suppl (May 20, 2021) e2119; NCT03762122). | detail... |
| FGFR3 over exp | glioblastoma | sensitive | U0126 | 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 K650E FGFR3 over exp HRAS K117E | myeloid neoplasm | sensitive | FGFR3 Inhibitor | 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 K650E FGFR3 over exp HRAS K117E | multiple myeloma | sensitive | FGFR3 Inhibitor | PD173074 | Preclinical | Actionable | In a preclinical study, PD173074 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells harboring HRAS H117E and over expression of FGFR3 K650E in culture (PMID: 22869148). | 22869148 |
| FGFR3 mut FGFR3 over exp | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | 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 D764H | head and neck squamous cell carcinoma | no benefit | FGFR Inhibitor (Pan) | 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 G380E | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G380E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G380E | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G380E were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 G380E | Advanced Solid Tumor | predicted - sensitive | FGFR3 Inhibitor | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G380E were sensitive to treatment with Pemazyre (pemigatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 G380E | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G380E were sensitive to treatment with Balversa (erdafitinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 K650E | Advanced Solid Tumor | conflicting | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | high grade glioma | predicted - sensitive | FGFR Inhibitor (Pan) | 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 | myeloid neoplasm | sensitive | FGFR3 Inhibitor | 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 | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | decreased response | FGFR3 Inhibitor | 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 | myeloid neoplasm | no benefit | FGFR Inhibitor (Pan) | 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 | myeloid neoplasm | sensitive | FGFR3 Inhibitor | 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 | decreased response | FGFR Inhibitor (Pan) | 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 | sensitive | FGFR3 Inhibitor | 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 | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 | 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited proliferation of transformed cells expressing FGFR3 K560E in culture (PMID: 26992226). | 26992226 |
| FGFR3 K650N | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Futibatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
| FGFR3 K650N | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR3 Inhibitor | 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 | FGFR Inhibitor (Pan) | 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 | FGFR3 Inhibitor | 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 S131L | head and neck squamous cell carcinoma | decreased response | FGFR Inhibitor (Pan) | 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 H284fs | Advanced Solid Tumor | predicted - resistant | FGFR3 Inhibitor | 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 H284fs | Advanced Solid Tumor | predicted - resistant | FGFR3 Inhibitor | Pemigatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 H284fs (FGFR3 H284fs*10) were resistant to treatment with Futibatinib (TAS-120) in culture (PMID: 34272467). | 34272467 |
| FGFR3 H284fs | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 S756P | lung non-small cell carcinoma | no benefit | FGFR3 Inhibitor | 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 R248_S249insC | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | 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 | FGFR3 Inhibitor | 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 S371C | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | 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 S371C | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | 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 G370C | Advanced Solid Tumor | predicted - resistant | FGFR3 Inhibitor | 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 G370C | Advanced Solid Tumor | predicted - resistant | FGFR Inhibitor (Pan) | 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 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | 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 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 mutant | urinary bladder cancer | sensitive | FGFR3 Inhibitor | 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 | FGFR Inhibitor (Pan) | 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 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | predicted - sensitive | FGFR3 Inhibitor | 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 | cholangiocarcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | 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 | 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 | FGFR Inhibitor (Pan) | 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 mutant | Advanced Solid Tumor | sensitive | FGFR3 Inhibitor | 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 | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 - BAIAP2L1 | urinary bladder cancer | sensitive | Cediranib | Preclinical - Cell culture | Actionable | In a preclinical study, Cediranib (AZD-2171) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). | 25589496 | |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | PD173074 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Votrient (pazopanib) inhibited growth of bladder cancer cells harboring FGFR3-BAIAP2L1 in culture, and inhibited tumor growth and ERK phosphorylation in cell line xenograft models (PMID: 23558953). | 23558953 |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). | 25589496 |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3-BAIAP2L1 fusion in culture (PMID: 27627808). | 27627808 | |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | AZD4547 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD4547 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). | 25589496 |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | ASP5878 | Preclinical - Cell culture | Actionable | In a preclinical study, ASP5878 treatment inhibited proliferation of a bladder cancer cell line harboring an FGFR3-BAIAP2L1 fusion in culture (Mol Cancer Ther December 2015 14; A170). | detail... |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | Pazopanib | Preclinical - Cell culture | Actionable | In a preclinical study, bladder cancer cells harboring FGFR3-BAIAP2L1 demonstrated sensitivity to Votrient (pazopanib) in culture (PMID: 23558953). | 23558953 |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). | 25589496 |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR Inhibitor (Pan) | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). | 25589496 |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | Debio 1347 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Debio 1347 decreased phosphorylation of ERK and FRS and inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture, and inhibited tumor growth in bladder cancer cell line xenograft models with FGFR3-BAIAP2L1 (PMID: 25589496) | 25589496 |
| FGFR3 - BAIAP2L1 | urinary bladder cancer | sensitive | FGFR3 Inhibitor | Debio 1347 | Preclinical - Cell culture | Actionable | In a preclinical study, Debio 1347 inhibited proliferation of a bladder cancer cell line harboring an FGFR3-BAIAP2L1 fusion in culture (PMID: 25169980). | 25169980 |
| FGFR3 - BAIAP2L1 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Balversa (erdafitinib) inhibited Fgfr phosphorylation and downstream signaling, resulted in growth inhibition of transformed cells expressing FGFR3-BAIA2PL1 in culture (PMID: 28416604). | 28416604 |
| FGFR3 - BAIAP2L1 | Advanced Solid Tumor | sensitive | Derazantinib | Preclinical - Cell culture | Actionable | In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR3-BAIAP2L1 in culture (PMID: 27627808). | 27627808 | |
| FGFR3 L608V | Advanced Solid Tumor | decreased response | FGFR3 Inhibitor | 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 | sensitive | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | decreased response | FGFR3 Inhibitor | 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 | decreased response | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 | sensitive | FGFR Inhibitor (Pan) | 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 R248C | Advanced Solid Tumor | sensitive | FGFR3 Inhibitor | 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 | Advanced Solid Tumor | conflicting | FGFR Inhibitor (Pan) | 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 | conflicting | FGFR Inhibitor (Pan) | Dovitinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 R348C were resistant to treatment with Dovitinib (TKI258) in culture (PMID: 34272467). | 34272467 |
| FGFR3 R248C | transitional cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | 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 | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | 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 K650M | Advanced Solid Tumor | resistant | FGFR3 Inhibitor | 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 | FGFR Inhibitor (Pan) | 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 | FGFR Inhibitor (Pan) | 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 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 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 | decreased response | FGFR Inhibitor (Pan) | 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 | predicted - sensitive | FGFR3 Inhibitor | AZD4547 | Phase II | Actionable | In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, with a partial response in 1 and stable disease in 2 of 7 patients with FGFR3 activating mutations (PMID: 32463741; NCT02465060). | 32463741 |
| FGFR3 act mut | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR3 in culture (PMID: 22238366). | 22238366 |
| FGFR3 act mut | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active 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 | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Phase I | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in stable disease in 70% (16/23) and partial response in 22% (5/23) of patients with advanced solid tumors harboring FGFR 1-4 activating mutations (including amplifications, mutations and translocations), while no antitumor activity was observed in patients with unknown or no known changes in FGFR (PMID: 26324363; NCT01703481). | 26324363 |
| FGFR3 act mut | bladder urothelial carcinoma | sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Guideline | Actionable | Balversa (erdafitinib) is included in guidelines for patients with advanced or metastatic bladder urothelial carcinoma harboring FGFR alterations (PMID: 34861372; ESMO.org). | detail... 34861372 |
| FGFR3 act mut | Advanced Solid Tumor | sensitive | FGFR3 Inhibitor | Debio 1347 | Phase I | Actionable | In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR3 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). | detail... |
| FGFR3 act mut | urinary bladder cancer | predicted - sensitive | FGFR3 Inhibitor | 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 amp | urinary system cancer | sensitive | FGFR3 Inhibitor | 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 | Advanced Solid Tumor | predicted - sensitive | FGFR3 Inhibitor | 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 | predicted - sensitive | FGFR Inhibitor (Pan) | 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 | urinary system cancer | sensitive | FGFR Inhibitor (Pan) | 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 | lung non-small cell carcinoma | sensitive | FGFR Inhibitor (Pan) | 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 F386L | myeloid neoplasm | sensitive | FGFR3 Inhibitor | 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 positive | lung squamous cell carcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | Rogaratinib | Phase I | 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 | head and neck squamous cell carcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | Rogaratinib | Phase I | 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 remission in a patient with FGFR3-positive head and neck squamous cell carcinoma (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #379P; NCT01976741). | detail... |
| FGFR3 positive | lung adenocarcinoma | predicted - sensitive | FGFR Inhibitor (Pan) | Rogaratinib | Phase I | 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 | stomach cancer | predicted - sensitive | FGFR Inhibitor (Pan) | Rogaratinib | Phase I | 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 | FGFR3 Inhibitor | 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 - PHGDH | childhood oligodendroglioma | predicted - sensitive | FGFR Inhibitor (Pan) | Ponatinib | Case Reports/Case Series | Actionable | In a clinical case study, a pediatric thalamic oligodendroglioma patient who achieved a partial response when treated with radiation therapy, was found to harbor an FGFR3-PHGDH fusion, and subsequent Iclusig (ponatinib) treatment led to a tumor reduction of 15% (compared to post-radiation scans), and an ongoing partial response lasting seven moths post-treatment initiation (PMID: 29872711). | 29872711 |
| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04424966 | Phase 0 | Infigratinib | Infigratinib in Recurrent High-Grade Glioma Patients | Recruiting | USA | 0 |