Lytgobi

Previously treated, unresectable, locally advanced, or metastatic intrahepatic cholangiocarcinoma harboring FGFR2 gene fusions or other rearrangements, as detected by an FDA-approved test.

20 mg orally once daily until disease progression or unacceptable toxicity
Take with or without food at approximately the same time daily
Dose reductions: 16 mg, then 12 mg (permanently D/C if 12 mg not tolerated)
Hyperphosphatemia management: Initiate low-phosphate diet and phosphate binder (sevelamer) when serum phosphate >5.5 mg/dL

Tablets: 4 mg, 12 mg, 20 mg

None listed.

• Ocular Toxicity: Serous retinal detachment (SRD) in 9% (usually Grade 1-2). Central serous retinopathy. Perform baseline ophthalmologic exam; repeat monthly for 4 months then q3 months. Withhold for symptomatic SRD.
• Hyperphosphatemia: Reported in 85% (30% Grade 3-4). Mechanism-based (on-target FGFR inhibition). Initiate phosphate-lowering therapy early. May lead to soft tissue mineralization.
• Palmar-Plantar Erythrodysesthesia (PPE): Hand-foot syndrome in 32%. Manage with moisturizers and dose modification.
• Hepatotoxicity: Monitor LFTs before and during treatment.
• Embryo-Fetal Toxicity

Hyperphosphatemia (85%), alopecia (33%), PPE/hand-foot syndrome (32%), diarrhea (28%), dry mouth (27%), fatigue (25%), stomatitis (25%), nail toxicity (22%), constipation (22%), dry skin (22%), decreased appetite (21%), nausea (21%), dysgeusia (19%), dry eye (18%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Futibatinib is an irreversible, covalent pan-FGFR inhibitor that binds to a conserved cysteine residue (Cys492 in FGFR1) in the P-loop of FGFR1, FGFR2, FGFR3, and FGFR4. By forming a covalent bond, it achieves sustained kinase inhibition even after drug clearance. It inhibits FGFR phosphorylation and downstream FRS2/RAS/MAPK and PI3K/AKT signaling. The irreversible binding mechanism may overcome certain gatekeeper mutations that confer resistance to reversible FGFR inhibitors.

Tmax: 2-3 hours. Half-life: approximately 14 hours (terminal). Protein binding: ~98%. Metabolized by CYP3A4 and CYP2C9. Steady-state by Day 8. Excreted in feces (79%) and urine (6%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• FOENIX-CCA2 — Futibatinib in FGFR2 fusion-positive intrahepatic cholangiocarcinoma. Phase II, n=103.
  🔬 NCT02052778 ↗ 📄 Primary Publication ↗

Lytgobi has FDA-approved indications across the following cancer types covered on PipelineEvidence: