Bictegravir CAS# 1611493-60-7 比克替拉韦

Bictegravir (GS-9883) is a potent second-generation HIV-1 integrase strand transfer inhibitor (INSTI) with strong activity in preclinical models. In vitro, it demonstrates low nanomolar inhibitory concentrations against a broad panel of HIV-1 isolates, including strains resistant to first-generation INSTIs such as raltegravir and elvitegravir, with an IC₅₀ typically in the range of 0.2–1 nM. Bictegravir exhibits a high genetic barrier to resistance, requiring multiple integrase mutations to significantly reduce its antiviral activity. Pharmacokinetic studies in animal models show favorable oral bioavailability, extensive tissue penetration, and a long intracellular half-life, supporting once-daily dosing. In humanized mouse models, bictegravir achieves potent viral suppression, with rapid decline in plasma viral RNA comparable to other clinically used INSTIs, and minimal cytotoxicity across relevant human cell lines. Its preclinical profile suggested strong efficacy, safety, and resistance robustness, which translated well into clinical development.