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

• Published in: Naunyn-Schmiedeberg's archives of pharmacology Vol. 397; no. 2; pp. 913 - 922
• Main Authors: Qin, Huiling, Yao, Cheng, Zhang, Wei, Hu, Wei, Liu, Yuantao, Yu, Shuchang, Xie, Dong, Hu, Min, Ye, Jun
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer Berlin Heidelberg 01.02.2024; Springer Nature B.V
• Subjects: Biomedical and Life Sciences; Biomedicine; Enzyme-linked immunosorbent assay; Healthy Volunteers; HIV; Human immunodeficiency virus; Humans; Infusions, Intravenous; Injection; Injections, Intravenous; Intravenous administration; Maleimides; Neurosciences; Peptides; Pharmacokinetics; Pharmacology/Toxicology; Bolus injection; Bioequivalence; Pharmacokinetics; Albuvirtide
• ISSN: 0028-1298; 1432-1912; 1432-1912
• DOI: 10.1007/s00210-023-02614-2

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