Doravirine
Doravirine. Newer NNRTI with cleaner DDI profile (CYP3A4 substrate but minimal induction). Lower psychiatric side effect signal than efavirenz.… Oral half-life 15 h.
Newer NNRTI with cleaner DDI profile (CYP3A4 substrate but minimal induction). Lower psychiatric side effect signal than efavirenz. Used in DOR/3TC/TDF (Delstrigo) once-daily regimen.
PK: real-PMID zero-content on all four. The one supported number in that paper is one the record does not store, an apparent clearance of 5.9 L/h, and the stored V 60 L is contradicted by the record own arithmetic — that clearance with a 15 h half-life implies about 128 L. ABSOLUTE BIOAVAILABILITY HAS NEVER BEEN DETERMINED: there is no intravenous doravirine and no published intravenous arm, and the 64% in circulation traces to sponsor label data rather than to any abstract. F is therefore pinned to 1 and every doravirine volume is necessarily apparent. The half-life of 15 h is retained but is REVIEW-GRADE (PMID:31388941); the primary gives a range of 12 to 21 h (PMID:25470746), of which 15 is not even the midpoint. V dropped rather than derived across two papers, which leaves the resolver default understating the apparent volume by roughly three-fold. ka 0.5 /h dropped against a stated time to peak of 1 to 4 h.
Pharmacokinetics
- Oral — t½ 15 h · F 100%
Sources: PMID:29723418, PMID:31388941, PMID:25470746