AAC Accepts, published online ahead of print on 26 October 2009
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Antimicrob. Agents Chemother. doi:10.1128/AAC.00976-09
Copyright (c) 2009, American Society for Microbiology and/or the Listed Authors/Institutions. All Rights Reserved.

An Albumin-conjugated Peptide Exhibits Potent Anti-HIV Activity and Long In Vivo Half-Life

Dong Xie*, Cheng Yao, Li Wang, Wenjie Min, Jiahong Xu, Jiahai Xiao, Mingxian Huang, Bo Chen, Bin Liu, Xiaolin Li, and He Jiang

Chongqing Frontier Biotechnologies Co., Chongqing 400041, China; Chengdu WestChina Frontier Pharmatech Co., Chengdu 610041, China; National Chengdu Center for Safety Evaluation of Drugs, West China Hospital, Sichuan University, Chengdu 610041, China

* To whom correspondence should be addressed. Email: dxie{at}frontierbiotech.com.


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Abstract

Clinical application of conventional peptide drugs is often limited by their short in vivo half-life and potential immunogenicity. Frequent injection presents challenges to treatment of chronic diseases, such as HIV infection. We chemically modified a peptide HIV fusion inhibitor with a single 3-maleimidopropionic acid (MPA), which allows rapid and irreversible conjugation with serum albumin at 1:1 molar ratio. FB006M, with a MPA modification at the 13th amino acid, rapidly formed conjugate with albumin upon intravenous injection, and exhibited a remarkably extended in vivo half-life. The albumin conjugate of FB006M displayed potent inhibitory activity against a number of laboratory and clinical isolates of HIV-1 in vitro and in vivo. No immunogenicity or antibody formation was detected after repeated dosing. Clinical application of FB006M may potentially decrease the cost of treatment and improve treatment compliance and patient quality of life.






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