Macitentan
Macitentan. Dual endothelin receptor antagonist — successor to bosentan with sustained tissue binding and once-daily dosing. PAH; hepatotoxicity… Oral half-life 14 h.
Dual endothelin receptor antagonist — successor to bosentan with sustained tissue binding and once-daily dosing. PAH; hepatotoxicity is less than bosentan. Anemia + nasopharyngitis are the more common adverse effects.
PK: the stored 16 h was the MIDPOINT of a stated 14.3 to 18.5 h range and is replaced by the stated lower endpoint. V 34 L comes from a population fit of 452 patients (PMID:34159557) and is APPARENT, so F is pinned to 1 and the stored 0.74 is dropped rather than paired with it. ka 0.1 /h dropped as unsourced. The active metabolite aprocitentan has a half-life near 48 hours and is not modelled by this record, so the curve understates the duration of endothelin blockade.
Pharmacokinetics
- Oral — t½ 14.3 h · F 100% · Vd 34 L
Sources: PMID:23900878, PMID:34159557