Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan.
Article Details
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Sidharta PN, Treiber A, Dingemanse J
Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan.
Clin Pharmacokinet. 2015 May;54(5):457-71. doi: 10.1007/s40262-015-0255-5.
- PubMed ID
- 25860376 [ View in PubMed]
- Abstract
Pulmonary arterial hypertension (PAH) is a progressive disease of the lung vascular system, which leads to right-sided heart failure and ultimately death if untreated. Treatments to regulate the pulmonary vascular pressure target the prostacyclin, nitric oxide, and endothelin (ET) pathways. Macitentan, an oral, once-daily, dual ETA and ETB receptor antagonist with high affinity and sustained receptor binding is the first ET receptor antagonist to show significant reduction of the risk of morbidity and mortality in PAH patients in a large-scale phase III study with a long-term outcome. Here we present a review of the available clinical pharmacokinetic, pharmacodynamic, pharmacokinetic/pharmacodynamic relationship, and drug-drug interaction data of macitentan in healthy subjects, patients with PAH, and in special populations.
DrugBank Data that Cites this Article
- Drugs
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Cyclosporine Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails Macitentan Cytochrome P450 2C19 Protein Humans NoSubstrateDetails Macitentan Cytochrome P450 2C8 Protein Humans NoSubstrateDetails Macitentan Cytochrome P450 2C9 Protein Humans NoSubstrateDetails Macitentan Cytochrome P450 3A4 Protein Humans NoSubstrateDetails - Drug Carriers
Drug Carrier Kind Organism Pharmacological Action Actions Macitentan alpha1-acid glycoprotein (Protein Group) Protein group Humans NoBinderDetails Macitentan Serum albumin Protein Humans NoBinderDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Cyclosporine ATP-binding cassette sub-family G member 2 Protein Humans UnknownInhibitorDetails Cyclosporine Solute carrier family 22 member 6 Protein Humans UnknownSubstrateInhibitorDetails Cyclosporine Solute carrier organic anion transporter family member 1B3 Protein Humans NoInhibitorDetails - Drug Reactions
Reaction Details Details Details Details
