Comparison of pharmacokinetics and safety of albuvirtide in healthy subjects after intravenous drip and bolus injection

Purpose: Albuvirtide (ABT) is the first long-acting HIV fusion inhibitor originally developed in China, blocking the invasion of HIV-1 virus into target cells. This study aimed to compare the pharmacokinetics, tolerability, and safety of ABT following a single intravenous (IV) bolus injection or intravenous drip in healthy Chinese subjects. Methods: . A single-center, randomized, open-label, single-period, parallel phase I clinical trial was conducted. 30 subjects were randomly divided into 3 groups in a ratio of 1:1:1. After an overnight fast, all subjects received a single dose administration of 320 mg ABT by intravenous drip for 45 min (Group A) or bolus injection for 0.5 min (Group B) or bolus injection for 3 min (Group C). ABT plasma concentrations were analyzed using validated enzyme-linked immunosorbent assay. Noncompartmental analysis was used to evaluate PK parameters. Results: . The median value of time to reach maximum concentration was 0.75 h in group A and 0.16 h in both group B and C, elimination half-life, mean residence time, apparent clearance and apparent volume of distribution was similar among three groups. The 90% confidence intervals of geometric mean ratios of PK parameters for group B and C relative to group C are mainly within 85–120%. All AEs in this study were mild, according to the CTCAE guidelines and the study investigator’s judgement. Conclusion: ABT bolus injection for 0.5 min and 3 min are expected well tolerated and to have similar pharmacokinetic characteristics as IV drip for 45 min, thus offering potential clinical benefits.