GSK744 (S/GSK1265744)

GSK744 (S/GSK1265744)是一种有效的HIV整合酶抑制剂，IC50值为3 nM[1]。

HIV整合酶是由HIV病毒产生的一种酶，能够使其遗传物质整合到感染细胞的DNA上。据报道，HIV整合酶在抑制HIV的发展中起重要作用[2]。

GSK744 (S/GSK1265744)是一种有效的HIV整合酶抑制剂。在用HIV-1抑制剂及整合酶链转移抑制剂抗性的定点分子（SDM）HIV克隆进行的阻力通道实验、整合酶实验和细胞实验中，GSK1265744通过抑制HIV整合酶，有效抑制HIV的复制[1]。

在阴道内接种猿猴/人类免疫缺陷病毒（一周2次，11周）的雌性猪尾猕猴模型中，GSK744注射可防止猕猴被病毒感染，而对照组在4个中位数的SHIV阴道挑战后被感染，表明GSK744可能是一种潜在的暴露前预防药物，通过抑制HIV整合酶，预防HIV感染[2][3]。

许多已进行的临床试验表明，GSK744可以有效地保护健康受试者免受HIV感染[4-6]。

参考文献：
[1].  Yoshinaga, T., et al., Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother, 2015. 59(1): p. 397-406.
[2].  Andrews, C.D., et al., Long-acting integrase inhibitor protects macaques from intrarectal simian/human immunodeficiency virus. Science, 2014. 343(6175): p. 1151-4.
[3].  Radzio, J., et al., The long-acting integrase inhibitor GSK744 protects macaques from repeated intravaginal SHIV challenge. Sci Transl Med, 2015. 7(270): p. 270ra5.
[4].  Ford, S.L., et al., Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744. Antimicrob Agents Chemother, 2013. 57(11): p. 5472-7.
[5].  Spreen, W., et al., Pharmacokinetics, safety, and tolerability with repeat doses of GSK1265744 and rilpivirine (TMC278) long-acting nanosuspensions in healthy adults. J Acquir Immune Defic Syndr, 2014. 67(5): p. 487-92.
[6].  Spreen, W.R., D.A. Margolis, and J.C. Pottage, Jr., Long-acting injectable antiretrovirals for HIV treatment and prevention. Curr Opin HIV AIDS, 2013. 8(6): p. 565-71.