Futibatinib
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-FUTIBATINIB |
|---|---|
| Type | Drug |
| Aliases | LytgobiФутибатиніб |
| Status | reviewed 2026-04-29 | pending_clinical_signoff |
| Diseases | DIS-CHOLANGIOCARCINOMA |
| Sources | SRC-ESMO-BTC-2023 SRC-FOENIX-CCA2 SRC-NCCN-HEPATOBILIARY |
Drug Facts
| Class | Selective irreversible (covalent) FGFR1/2/3/4 tyrosine kinase inhibitor |
|---|---|
| Mechanism | Oral, highly selective irreversible covalent inhibitor of FGFR1, FGFR2, FGFR3, and FGFR4. Forms a covalent bond with a conserved cysteine in the FGFR P-loop, conferring sustained target inhibition with reduced off-target activity vs ATP-competitive reversible FGFR TKIs. Designed to retain potency against gatekeeper (e.g. FGFR2 V564F) and molecular-brake resistance mutations that drive acquired resistance to reversible FGFR inhibitors (pemigatinib, infigratinib). Pivotal FOENIX-CCA2 Phase II (n=103, FGFR2 fusion / rearrangement cholangiocarcinoma post ≥1 prior line including gem-cis) showed ORR 41.7%, mDOR 9.7 months, mPFS 9.0 months, mOS 21.7 months → FDA accelerated approval Sep 2022. |
| Typical dosing | 20 mg PO once daily continuously, until disease progression or unacceptable toxicity. Take with or without food at the same time each day. Hold + reduce for grade ≥3 hyperphosphatemia despite phosphate binders + diet (target serum phosphate <7.0 mg/dL); hold for any retinal pigment epithelial detachment (RPED) until resolution. Dose reductions: 16 mg → 12 mg → permanent discontinuation. |
| Ukraine registered | False |
| NSZU reimbursed | False |
| Ukraine last verified | 2026-04-29 |
Notes
Futibatinib is the second FGFR-targeted therapy approved for FGFR2 fusion / rearrangement cholangiocarcinoma (after pemigatinib). Its irreversible covalent mechanism is the key differentiator: retains activity against several gatekeeper (V564F) + molecular-brake resistance mutations that drive acquired resistance to pemigatinib / infigratinib (Goyal NEJM 2019). FOENIX-CCA2 (Goyal NEJM 2023) is the pivotal Phase II — 103 patients, FGFR2 fusion / rearrangement iCCA post ≥1 prior line including gem-cis, ORR 41.7%, DCR 82.5%, mDOR 9.7 mo, mPFS 9.0 mo, mOS 21.7 mo, all CTCAE-v5 hyperphosphatemia grade ≥3 manageable with binders + diet, RPED rate ~9%. NCCN-Hepatobiliary + ESMO-BTC-2023 list both pemigatinib and futibatinib as preferred 2L+ options for FGFR2-altered iCCA. FOENIX-CCA3 (1L vs gem+cis) is the post-marketing confirmatory required for accelerated → traditional approval conversion. Class toxicity dominated by hyperphosphatemia (target <7.0 mg/dL) and serous retinopathy (monthly ophtho + OCT for first 4 mo, then per protocol). Missing source IDs to flag: SRC-FDA-LYTGOBI not yet authored; FOENIX-CCA3 trial source pending.
Used By
Drug
DRUG-INFIGRATINIB- Infigratinib
Regimens
REG-FUTIBATINIB-CHOLANGIO-2L- Futibatinib monotherapy (FOENIX-CCA2) — 2L+ FGFR2-fusion cholangiocarcinoma