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Lirafugratinib (Lyrfigtu)

Previously treated FGFR2 fusion or rearrangement-positive cholangiocarcinoma

Also known as RLY-4008
Regulatory submission
NDA submitted January 2026
Last updated
158 sources

Product information and disease descriptionProduct descriptionProduct informationDrug/Drug, drug/disease interactions

Effects of other drugs on Lirafugratinib

3 evidence topics · 1 source

Strong and moderate CYP3A inhibitors

“Avoid concomitant use of LYRFIGTU with strong or moderate CYP3A inhibitors. Reduce LYRFIGTU dosage if concomitant use cannot be avoided [see Dosage and Administration (2.4)].” (opens the prescribing information at this quote)

“increased 1.3-fold and AUC 2-fold following coadministration with itraconazole 200 mg once daily for 8 days.” (opens the prescribing information at this quote)

“is predicted to increase 1.1-fold and AUC 1.7-fold following coadministration with erythromycin (moderate CYP3A inhibitor) 500 mg four times a day for 15 days.” (opens the prescribing information at this quote)

Strong and moderate CYP3A inducers

“Avoid concomitant use of strong or moderate CYP3A inducers.” (opens the prescribing information at this quote)

“Concomitant use of LYRFIGTU with a strong or moderate CYP3A inducer may decrease lirafugratinib exposure [see Clinical Pharmacology (12.3)], which may reduce the effectiveness of LYRFIGTU.” (opens the prescribing information at this quote)

“is predicted to decrease to 65% and AUC to 25% following coadministration of rifampicin (strong CYP3A inducer) 600 mg once daily for 19 days.” (opens the prescribing information at this quote)

“is predicted to decrease to 85% and AUC to 43% following coadministration of efavirenz (moderate CYP3A inducer) 600 mg once daily for 19 days.” (opens the prescribing information at this quote)

Acid-reducing agents, P-gp inhibitors, and transporter substrate status

“No clinically significant differences in lirafugratinib pharmacokinetics are predicted when used concomitantly with quinidine (P-gp inhibitor). No clinically significant differences in lirafugratinib pharmacokinetics were observed when administered concomitantly with esomeprazole (proton pump inhibitor).” (opens the prescribing information at this quote)

“Lirafugratinib is a P-gp and BCRP substrate, but not of OCT1, OATP1B1, OATP1B3, or BSEP.” (opens the prescribing information at this quote)