Bictegravir
Bictegravir. Second-generation HIV INSTI — higher barrier to resistance than dolutegravir. Co-formulated with TAF + emtricitabine as Biktarvy, a… Oral half-life 17 h.
Second-generation HIV INSTI — higher barrier to resistance than dolutegravir. Co-formulated with TAF + emtricitabine as Biktarvy, a single-tablet once-daily HIV regimen.
PK: THE RECORD OWN DATA-INTEGRITY FLAG IS MISPLACED AND IS CLOSED HERE. Its note claimed the stored volume is a central-compartment value, but the cited paper is a physiologically-based interaction study whose abstract reports only fold-changes and CONTAINS NO COMPARTMENT VOLUMES AT ALL, so that claim was unsupported in either direction. THE VOLUME AND BIOAVAILABILITY ARE ACQUITTED ON ARITHMETIC: they imply a clearance of 0.63 L/h against about 0.49 derived from a published exposure — 1.28x, the tightest agreement in that group — and an independent source states "Its systemic plasma clearance is low, and the volume of distribution is approximately the volume of extracellular water in nonclinical species", which is around fourteen litres and consistent with what is stored. Bictegravir is the one drug in its group where a low clearance and a small volume make the central and terminal volumes converge, so the usual class-12 hazard does not bite. The absorption rate is removed rather than replaced: it implied a 4.33 h peak against a verbatim "Median Tmax ranged from 1.0 to 1.8 hours (day 1, postdose) and 1.3-2.7 hours (day 10)", ABOVE THE UPPER BOUND OF THE ENTIRE PUBLISHED RANGE, and the only source reports ranges across four dose cohorts rather than a value for the dose this record models. The half-life is unsupported but sits inside that paper verbatim 15.9 to 20.9 hours.
Pharmacokinetics
- Oral — t½ 17.3 h · F 99% · Vd 15.56 L
Sources: PMID:37701391, PMID:28196003