Raltegravir
Raltegravir. First-in-class HIV integrase strand-transfer inhibitor (INSTI) — blocks viral DNA integration into host genome. Largely supplanted… Oral half-life 7.8 h.
First-in-class HIV integrase strand-transfer inhibitor (INSTI) — blocks viral DNA integration into host genome. Largely supplanted by dolutegravir + bictegravir for once-daily dosing + better resistance barrier.
PK: zero-content — its citation is an atazanavir interaction study that used an INVESTIGATIONAL formulation and inflated exposure 1.67-fold with a co-administered inhibitor. The stored 9 h probably collides with its "atazanavir q.d. for 9 CONSECUTIVE DAYS". F 0.5 IS UNSOURCEABLE IN PRINCIPLE: searches for an absolute bioavailability or any intravenous raltegravir study return zero records, so F is pinned to 1. ABSORPTION IS THREE SEQUENTIAL TRANSIT COMPARTMENTS, delayed in pregnancy, CIRCADIAN, and formulation-dependent — the 600 mg tablet is 21% more bioavailable than the 400 mg and pregnancy cuts it 49% — so no single rate is admissible. An unusual reversal worth recording: the INTRACELLULAR half-life is 4.5 h, SHORTER than the 7.8 h plasma value, with "no intracellular accumulation or persistence" — the opposite of the other antivirals in this batch.
Pharmacokinetics
- Oral — t½ 7.8 h · F 100%
Sources: PMID:27696440, PMID:21746959, PMID:33369217