A highly potent and safe pyrrolopyridine-based allosteric HIV-1 integrase inhibitor targeting host LEDGF/p75-integrase interaction site
Fig 5
In vivo pharmacokinetics and histology of STP0404 treated subjects.
A. SD rats were administrated with STP0404 by IV (1 and 5 mg/kg) and PO (2 and 10 mg/kg). B. Beagle dogs were administrated IV and PO (2 mg/kg). Plasma concentrations were determined by LC-MS for 24 h post administration (see Methods). For A and B, data are presented as means of three independent experiments and error bars indicate the standard deviations from the means. C. Half-lives (T1/2), area under the curve (AUC), maximum concentration (Cmax), and bioavailability (Ft) from the administrated animals (A and B) were calculated. D. Histology of beagle dogs orally administrated with STP0404 (90 mg/kg) or vehicle for bladder, ureter, and kidney in 4-week GLP toxicology study. The entire GLP toxicology study’s results were summarized in S3 Table.