Table 2 Overview of clinical trials involving FGFR fusions
From: Fibroblast growth factor receptor fusions in cancer: opportunities and challenges
Inhibitor | IC50 | Clinical trial ID | Genetic alterations | Cancer type | Phase | Status |
|---|---|---|---|---|---|---|
First-generation inhibitors | ||||||
 Derazantinib (ARQ-087) | FGFR1 (4.5 nM) FGFR2 (1.8 nM) FGFR3 (4.5 nM) FGFR4 (34 nM) | NCT01752920 | FGFR genetic alterations including FGFR2 gene fusion | Advanced solid tumors | I/II | Completed |
NCT03230318 | FGFR2 gene fusion, mutation or amplification | Cholangiocarcinoma | II | Recruiting | ||
NCT04045613 | FGFR genetic aberrations | Urothelial cancer | I/II | Recruiting | ||
 Ponatinib | FGFR1 (2.2 nM) FGFR2 (1.6 nM) FGFR3 (18.2 nM) FGFR4 (7.7 nM) | NCT02265341 | FGFR2 fusions | Biliary cancer | II | Completed |
NCT02272998 | FGFR alterations including fusions | Advanced solid tumor | II | Recruiting | ||
Second-generation inhibitors | ||||||
 Pemigatinib (INCB054828) | FGFR1 (0.4 nM) FGFR2 (0.5 nM) FGFR3 (1.2 nM) FGFR4 (30 nM) | NCT03656536 | FGFR2 rearrangement. | Cholangiocarcinoma | III | Recruiting |
NCT04003610 | FGFR3 mutation or rearrangement | Urothelial carcinoma | II | Active | ||
NCT04258527 | FGF/FGFR alterations | Advanced malignancies | I | Active | ||
NCT04096417 | FGFR alterations | Colorectal cancer | II | Recruiting | ||
NCT02872714 | FGF/FGFR alterations | Urothelial carcinoma | II | Active | ||
NCT03822117 | FGFR mutations or fusions | Solid tumor | II | Recruiting | ||
NCT04003623 | FGFR mutations or translocations | Solid tumors | II | Recruiting | ||
NCT03011372 | FGFR1 rearrangement | Myeloid/lymphoid neoplasms | II | Recruiting | ||
 Erdafitinib (JNJ-42756493) | FGFR1 (2.0 nM) FGFR2 (2.0 nM) FGFR3 (4.0 nM) FGFR4 (6.3 nM) | NCT02365597 | FGFR genomic alterations. | Urothelial cancer | II | Recruiting |
NCT02465060 | FGFR amplification mutation or fusion | Solid tumors, lymphomas, or multiple myeloma | II | Recruiting | ||
NCT03827850 | FGFR genetic alterations | Non small cell lung carcinoma | II | Recruiting | ||
NCT03390504 | FGFR gene aberrations | Urothelial cancer | II | Recruiting | ||
NCT04083976 | FGFR mutations and gene fusions. | Advanced solid tumors | II | Recruiting | ||
 Infigratinib (BGJ398) | FGFR1 (0.9 nM) FGFR2 (1.4 nM) FGFR3 (1.0 nM) FGFR4 (60 nM) | NCT03773302 | FGFR2 gene fusions/translocations | Cholangiocarcinoma | III | Recruiting |
NCT04424966 | FGFR3-TACC3 translocation | High-grade glioma | I | Recruiting | ||
NCT02150967 | FGFR genetic alterations | Cholangiocarcinoma | II | Recruiting | ||
NCT04197986 | FGFR3 genetic alterations including fusion | Urothelial carcinoma | III | Recruiting | ||
NCT04233567 | FGFR1–3 gene fusions or other genetic alterations | Solid tumors | II | Recruiting | ||
 Debio1347 (CH5183284) | FGFR1 (9.3 nM) FGFR2 (7.6 nM) FGFR3 (22 nM) FGFR4 (290 nM) | NCT03834220 | FGFR1–3 fusions | Solid Tumors | II | Active |
 AZD4547 | FGFR1 (0.2 nM) FGFR2 (1.8 nM) FGFR3 (2.5 nM) FGFR4 (165 nM) | NCT02824133 | FGFR-TACC gene fusion | Malignant glioma | I/II | Completed |
Third-generation inhibitors | ||||||
 Futibatinib (TAS-120) | FGFR1 (3.9 nM), FGFR2 (1.3 nM), FGFR3 (1.6 nM) FGFR4 (8.3 nM) | NCT04093362 | FGFR2 gene rearrangements | Advanced cholangiocarcinoma | III | Not yet recruiting |
NCT04189445 | FGFR1–4 rearrangements | Solid tumors/ myeloid or lymphoid neoplasms | II | Recruiting | ||
NCT02052778 | FGFR fusion or activating mutation or amplification | Advanced solid tumors | I/II | Active, | ||