.Pharmacolibrary.Drugs.C_CardiovascularSystem.C02K_OtherAntihypertensives.C02KX04_Macitentan.Macitentan

Information

Macitentan is an orally administered dual endothelin receptor antagonist approved for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression. It is currently used in clinical practice for this indication.

Pharmacokinetics

Pharmacokinetic model parameters in healthy adults following a single oral dose of 10 mg macitentan.

References

1. Bartolucci, R, et al., & Poggesi, I (2021). A Population Pharmacokinetic Model of Macitentan and Its Active Metabolite Aprocitentan in Healthy Volunteers and Patients with Pulmonary Arterial Hypertension. Clinical pharmacokinetics 60(12) 1605–1619. DOI:10.1007/s40262-021-01049-3 PUBMED:https://pubmed.ncbi.nlm.nih.gov/34159557

2. Sidharta, PN, et al., & Dingemanse, J (2015). Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. Clinical pharmacokinetics 54(5) 457–471. DOI:10.1007/s40262-015-0255-5 PUBMED:https://pubmed.ncbi.nlm.nih.gov/25860376

3. Bruderer, S, et al., & Dingemanse, J (2013). Pharmacokinetics of macitentan in caucasian and Japanese subjects: the influence of ethnicity and sex. Pharmacology 91(5-6) 331–338. DOI:10.1159/000351704 PUBMED:https://pubmed.ncbi.nlm.nih.gov/23817130

Revisions

• 06/2025 initial generated model