长效抗 HIV 药物的设计策略。
Design strategies for long-acting anti-HIV pharmaceuticals.
机构信息
School of Science, Harbin Institute of Technology (Shenzhen), Shenzhen 518055, China; Green Pharmaceutical Engineering Research Center, Harbin Institute of Technology (Shenzhen), Shenzhen 518055, China.
Engineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433, China.
出版信息
Curr Opin Pharmacol. 2020 Oct;54:158-165. doi: 10.1016/j.coph.2020.10.005. Epub 2020 Nov 8.
Current combination antiretroviral therapy (cART) for human immunodeficiency virus (HIV) is limited by the frequent dosing and unfavorable adherence, and the rapid appearance of resistant mutants. Thus, there is a continuous need to improve and optimize the present therapies. The clinical phase III trials of FLAIR and ATLAS, showed two-drug injectable cabotegravir (CAB) and rilpivirine (RPV) formulation is potent, safe, and tolerable in HIV-infected patients. The recent approval of cabenuva (CAB+RPV) by Health Canada is a milestone in the development of long-term therapies for HIV infection. Broadly neutralizing antibodies (bNAbs) with excellent breath and efficiency against HIV have been investigated as LA antiviral weapons. Several modern modalities capable of sustained drug release for long-term treatment and prevention of HIV infection are also in development, such as implants, vaginal rings, and nanotherapies.
目前，针对人类免疫缺陷病毒（HIV）的联合抗逆转录病毒疗法（cART）受到频繁给药和不良依从性以及耐药突变体快速出现的限制。因此，不断需要改进和优化现有疗法。FLAIR 和 ATLAS 的临床 III 期试验表明，双药注射用卡博特韦（CAB）和利匹韦林（RPV）制剂在 HIV 感染患者中具有强大、安全和耐受的特性。加拿大卫生部最近批准卡布韦（CAB+RPV）是 HIV 长期治疗发展的一个里程碑。具有广谱中和抗体（bNAbs）的高效抗 HIV 药物已被研究作为长效抗病毒武器。还有几种能够持续释放药物用于长期治疗和预防 HIV 感染的现代方式也在开发中，如植入物、阴道环和纳米疗法。
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