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目的重点介绍正在进行临床研究的小分子趋化因子受体5(CCR5)拮抗剂的相关进展。方法通过查阅并归纳总结近期国内外报道的已经进入临床研究的小分子趋化因子受体5拮抗剂的相关文献进行介绍。结果与结论小分子趋化因子受体5拮抗剂的设计与研究已经成为当前抗HIV-1药物研发的热点。该类药物maraviroc早在2007年就获得FDA批准成功上市,目前仍有6个小分子趋化因子受体5拮抗剂被选作候选药物正处在不同的临床试验阶段。这些拮抗剂结构呈现多样,成药性好,它们的临床研究结果对于开发更多新型有效的抗HIV-1药物具有重要意义。
Objective To highlight the progress of small molecule Chemokine Receptor 5 (CCR5) antagonists undergoing clinical studies. Methods By reviewing and summarizing the recent reports of small molecule chemokine receptor 5 antagonists that have been reported in clinical trials in and out of China. Results and Conclusions The design and study of small molecule chemokine receptor 5 antagonists has become a hot spot in the current research and development of anti-HIV-1 drugs. The drug, maraviroc, was approved by the FDA as early as 2007 and is on the market. There are still six small-molecule chemokine receptor 5 antagonists currently being selected as candidates for the drug at different clinical trials. These antagonists have diverse structures and good druggability, and their clinical findings are of great importance for the development of more new and effective anti-HIV-1 drugs.