Pharmacokinetics of Bictegravir in Older Japanese People Living with HIV-1

Abstract

BIC is a potent integrase strand transfer inhibitor (INSTI), widely used for the treatment of HIV-1 as part of a once-daily single-tablet regimen that includes emtricitabine and tenofovir alafenamide (BIC+FTC+TAF). Although the safety and efficacy of BIC+FTC+TAF have been confirmed in older patients with HIV-1, PK data in this patient population remain limited.

Treatment outcomes amongst older people with HIV infection receiving antiretroviral therapy

“…Although ART [41][42][43][44][45][46]. Furthermore, novel therapeutic modalities and treatment strategies, including the 'shock and kill' approach for the elimination of latent HIV reservoirs, immunotherapies (such as neutralizing antibodies, cytokine adjuvant therapy, and immune checkpoint inhibitors), stem cell transplantation, and gene editing [47], have shown promising results in achieving a functional cure for HIV.…”

“…These findings collectively emphasize the efficacy, safety, and tolerability of INSTIs in the older patient population. Despite the limited guidance on the use of INSTIs in older participants and cautionary advice in product labeling, available data suggest that INSTIs may be considered for use in geriatric participants [41–46]. Furthermore, novel therapeutic modalities and treatment strategies, including the ‘shock and kill’ approach for the elimination of latent HIV reservoirs, immunotherapies (such as neutralizing antibodies, cytokine adjuvant therapy, and immune checkpoint inhibitors), stem cell transplantation, and gene editing [47], have shown promising results in achieving a functional cure for HIV.…”

“…The investigation by Foca et al [ 43 ] revealed no virological failures among individuals aged 65 years and above who received an INSTI regimen, indicating strong and lasting effectiveness. The study by Kawashima et al [ 44 ] demonstrated the safe use of the BIC+FTC+TAF regimen in men over 50 years, with no reported renal or hepatic failure and no significant correlation found between age and pharmacokinetic parameters. Importantly, no instances of virological failure and no observed changes in various health markers further support the well tolerated use of the regimen in older participants.…”

“…The study by Kawashima et al[44] demonstrated the safe use of the BICþFTCþTAF regimen in men over 50 years, with no reported renal or hepatic failure and no significant correlation found between age and pharmacokinetic parameters. Importantly, no instances of virological failure and no observed changes in various health markers further support the well tolerated use of the regimen in older participants.…”

Steady-state pharmacokinetics of plasma tenofovir alafenamide (TAF), tenofovir (TFV) and emtricitabine (FTC), and intracellular TFV-diphosphate and FTC-triphosphate in HIV-1 infected old Japanese patients treated with bictegravir/FTC/TAF

“…However, the pharmacokinetic (PK) data for the elderly Japanese population are currently limited. Here, we conducted a prospective steady-state PK study of BIC/FTC/TAF in elderly Japanese patients using previously published BIC data (3). In this study, we examined the remaining PK data for plasma FTC, TAF, and tenofovir (TFV), an intermediate metabolite of TAF.…”