Name: Lirafugratinib (Lyrfigtu) in Previously treated FGFR2 fusion or rearrangement-positive cholangiocarcinoma: Pharmacokinetics
Published: 2026-09-27T09:44:05-04:00

Dose proportionality, accumulation, and steady state

“Lirafugratinib maximum concentration (Cmax) is 4.7 mcg/mL (30%) and systemic exposure (AUC) is 77 mcg·h/mL (29%).” (opens the prescribing information at this quote)
“increases in a dose proportional manner over the dose range from 20 mg to 100 mg orally once daily (0.3 to 1.4 times the recommended dosage). Lirafugratinib accumulation is approximately 2-fold at the approved recommended dosage. Lirafugratinib steady state is reached in approximately 4 days.” (opens the prescribing information at this quote)

Absorption and food effect

“Lirafugratinib median (min, max) time to maximum plasma concentration (Tmax) is 3.9 (1.9 to 8) hours.” (opens the prescribing information at this quote)
“No clinically significant difference in lirafugratinib pharmacokinetics were observed following administration of a high-fat, high-calorie meal (approximately 800 to 1000 total calories with 500 to 600 calories from fat).” (opens the prescribing information at this quote)

Distribution, metabolism, and elimination

“Lirafugratinib apparent (oral) volume of distribution is 22 (22%) L. Lirafugratinib plasma protein binding is >99% and is not concentration-dependent in vitro.” (opens the prescribing information at this quote)
“Lirafugratinib blood-to-plasma ratio is approximately 0.4.” (opens the prescribing information at this quote)
“Lirafugratinib elimination half-life is 23 (34%) hours with an apparent (oral) clearance of 1 (32%) L/h.” (opens the prescribing information at this quote)
“Lirafugratinib is primarily metabolized by CYP3A4 and CYP2J2 and to a lesser extent by non-CYP enzymes in vitro.” (opens the prescribing information at this quote)

Mass balance and excretion in healthy volunteers

“Lirafugratinib and its metabolites were mainly excreted in feces. Unchanged lirafugratinib represented the predominant circulating component in plasma.” (opens the source at this quote in a new tab)

Recovery of a radiolabeled dose in the prescribing information

“Following a single oral dose of radiolabeled lirafugratinib 70 mg to healthy subjects, approximately 80% of the dose was recovered in feces (23% unchanged), and 8% was recovered in urine (unchanged lirafugratinib not quantified).” (opens the prescribing information at this quote)

Specific populations

“No clinically significant differences in the pharmacokinetics of lirafugratinib were observed based on age (20-87 years), sex, race (White 59%, Asian 16%, or Black 2.7%), body weight (34-147 kg), CLcr 30-89 mL/min (estimated by Cockcroft-Gault), or mild (Child-Pugh Class A) to moderate (Child-Pugh Class B) hepatic impairment.” (opens the prescribing information at this quote)
“The effect of severe renal impairment (CLcr < 30 mL/min) and severe (Child-Pugh Class C) hepatic impairment on lirafugratinib pharmacokinetics is unknown.” (opens the prescribing information at this quote)