Entecavir

pharmacological · renal · immune-hematologic · Oral

Entecavir. Guanosine nucleoside analog — selective HBV polymerase inhibitor. First-line oral therapy for chronic HBV with high barrier to… Oral half-life 24 h.

Guanosine nucleoside analog — selective HBV polymerase inhibitor. First-line oral therapy for chronic HBV with high barrier to resistance + minimal HIV cross-activity. Renal excretion; food reduces F.

PK: half-life corrected 130 -> 24 h, and the correction is a change of PARAMETER, not just of number. Yan 2006 (PMID:17050790), 24 healthy subjects on 14 days of dosing, states verbatim a "terminal half-life ranging from 128 to 149 hours and an effective half-life of approximately 24 hours". The 128-149 h terminal phase reflects intracellular triphosphate persistence and is the wrong quantity for a plasma model on daily dosing; the effective half-life governs accumulation. The stored 130 h sat inside that terminal range but is written in no paper. ka 0.7 /h, V 42 L and F 0.95 dropped: the previous citation is a food-effect study whose only numbers are relative changes.

Pharmacokinetics

Sources: PMID:21125816, PMID:17050790