Evaluating the combination of bictegravir and lenacapavir as a single tablet option for HIV

HIV treatment is evolving toward simplified regimens with fewer agents, improved tolerability, and activity against resistant virus. This review evaluates the potential clinical role of lenacapavir (LEN), a capsid inhibitor, combined with bictegravir (BIC), an integrase strand transfer inhibitor, as a single-tablet regimen (STR) for HIV treatment.

This review summarizes the pharmacology, pharmacokinetics, clinical efficacy, safety, resistance profile, and comparative therapeutic landscape of LEN and BIC, and discusses their potential integration into future HIV treatment strategies.

Current HIV therapy is dominated by highly effective and well-tolerated STRs with high barriers to resistance. However, unmet needs remain for individuals with resistant virus, intolerance to injectables, or preference for regimens with fewer agents. The LEN/BIC combination represents a potentially potent and well-tolerated STR with activity against multidrug-resistant HIV. BIC provides a high genetic barrier to resistance, while LEN's prolonged half-life may offer pharmacologic forgiveness. Nevertheless, important challenges remain, with limited data, clinically significant drug-drug interactions related to LEN metabolism and its potential for resistance emergence. Future HIV therapy will evolve toward increasingly personalized treatment integrating daily oral, extended-interval oral, and long-acting injectables. Within this evolving paradigm, LEN/BIC will expand therapeutic options and advance patient-centered HIV care.