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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
futibatinib
L01EN04
Forms & Strengths
- Tablets: 14 mg, 16 mg, 20 mg
Adult Dosing
- Recommended dose: 20 mg orally once daily until disease progression or unacceptable toxicity
- Taken with or without food
- Swallow tablets whole; do not crush, chew, split, or dissolve
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of adult patients with previously treated, unresectable, locally advanced or metastatic cholangiocarcinoma containing a fibroblast growth factor receptor 2 (FGFR2) gene fusion or other rearrangement
Mechanism of Action
- Irreversible, covalent inhibitor of fibroblast growth factor receptors (FGFR1-4)
- Suppresses FGFR signaling pathways, leading to decreased cell proliferation and increased apoptosis in tumor cells harboring FGFR2 gene fusions/rearrangements
Adverse Reactions
- Hyperphosphatemia
- Nail toxicity (onycholysis, nail bed disorder)
- Musculoskeletal pain
- Fatigue
- Diarrhea
- Constipation
- Stomatitis
- Dry eye and other ocular toxicities (retinal pigment epithelial detachment)
- Decreased appetite
- Vomiting
- Abdominal pain
- Alopecia
Drug Interactions
- Strong or moderate CYP3A inhibitors: Avoid concurrent use if possible; if unavoidable, monitor closely for adverse reactions
- Strong or moderate CYP3A inducers: Avoid concurrent use as they may decrease futibatinib efficacy
- Substrates of P-gp: Concomitant use may increase concentrations of P-gp substrates
Curated Content: Needs Vetting Before Put to Clinical Use