Pharmacokinetics and Safety of Ainuovirine/Lamivudine/Tenofovir Combination Tablets in Young and Elderly Patients with Human Immunodeficiency Virus-1 Infection

Abstract

Introduction

Ainuovirine/lamivudine/tenofovir is a novel antiretroviral therapy regimen used to treat human immunodeficiency virus-1 (HIV-1) infection. This study aimed to compare the pharmacokinetics of ainuovirine/lamivudine/tenofovir in HIV-1-infected patients aged ≥ 65 (elderly patients) and ≤ 40 years (young patients).

Methods

This prospective, open-label, parallel controlled clinical study included 15 young and 15 elderly patients. Blood (1 mL) was collected 30 min before dosing and at 0.5, 1, 1.5, 2, 3, 4, 8, 12, 16, and 24 h after dosing, to measure the plasma concentrations of ainuovirine/lamivudine/tenofovir. Safety was assessed by monitoring the adverse events, physical examinations, and clinical laboratory tests.

Results

Plasma concentrations of each ainuovirine/lamivudine/tenofovir component reached peak levels 1–4 h after dosing and gradually decreased during the remaining observation period. Compared with the young group, ainuovirine had significantly higher T _1/2Ke, AUC _0–24, and AUC _0–inf (all P < 0.05) in the elderly group, whereas K _e ( P = 0.002) was significantly lower. However, the C _max and T _max of ainuovirine did not differ significantly. Lamivudine and tenofovir also had a significantly higher C _max ( p = 0.004 and p = 0.008, respectively) and AUC _0–inf ( P = 0.014 and P = 0.006, respectively) in the elderly group, whereas there was no significant difference in T _max, K _e, and T _1/2Ke. Ainuovirine/lamivudine/tenofovir was well tolerated in both the young and elderly groups.

Conclusion

This study suggests that the ainuovirine/lamivudine/tenofovir regimen might be an effective and safe treatment regimen for HIV-1-infected patients aged ≥ 65 years and ≤ 40 years. Further studies are needed to confirm these results and develop optimal dosing regimens for elderly HIV-1-infected patients.