Ibrexafungerp citrate

China [CN]

Pharmacokinetics

Absorption: Oral bioavailability is approximately 30%, and absorption is not affected by food. The time to reach peak concentration (Tmax) is approximately 2 hours.

Distribution: Plasma protein binding rate is 99.5%-99.8%. It is widely distributed in tissues, with high concentrations in the kidneys (20-25 times higher than in plasma).

Metabolism: Primarily metabolized by CYP3A4, with a half-life of approximately 15 hours.

Excretion: Approximately 60% is excreted in the feces, and 30% is excreted in the urine.

Safety and Drug Interactions

Common adverse reactions: Diarrhea, nausea, abdominal pain, dizziness, vomiting, etc., are mostly mild to moderate and do not require discontinuation of the drug.

Contraindications: Contraindicated in patients allergic to isavuconazole or its citrate salt.

Special populations: Use with caution in pregnant and breastfeeding women; no dose adjustment is needed for patients with hepatic or renal impairment, but monitoring is required.

Drug Interactions

When used with strong CYP3A4 inhibitors (such as ketoconazole), isavuconazole exposure increases, and dose adjustment is necessary.

When used with strong CYP3A4 inducers (such as rifampicin), exposure decreases, and efficacy may be reduced; co-administration is not recommended.

It inhibits CYP2C8, CYP3A4, P-gp, and OATP1B3; concentration monitoring is required when used with related substrates.