Penetration of enfuvirtide, tenofovir, efavirenz, and protease inhibitors in the genital tract of HIV-1-infected men
Penetration of enfuvirtide, tenofovir, efavirenz, and protease inhibitors in the genital tract of HIV-1-infected men
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DOI：
10.1097/00002030-200409240-00014
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发表时间：
2004-09-24
期刊：
影响因子：
3.8
通讯作者：
Rouzioux, C
中科院分区：
文献类型：
--
作者：
Ghosn, J;Chaix, ML;Rouzioux, C
病毒学失败的一个可能机制是抗逆转录病毒能力差。药物在生殖道等病毒复制部位的扩散。我们测量了13名未能接受治疗的艾滋病毒感染者的血液和精液中的抗逆转录病毒药物浓度。恩福韦肽没有通过血-睾丸屏障，而替诺福韦则在精液中蓄积。与依地那韦不同的是，洛匹那韦、氨丙那韦、沙奎那韦和依法韦仑的精液浓度无效。这些都是令人担忧的发现，因为不理想的精液药物浓度可能会增加性传播耐药艾滋病毒变种的风险。
One likely mechanism of virological failure is poor antiretroviral. drug diffusion in sites of viral replication such as the genital tract. We measured antiretroviral drug concentrations in blood and semen in 13 HIV-infected men failing treatment. Enfuvirtide did not cross the blood-testis barrier, whereas tenofovir accumulated in semen. Unlike indinavir, semen concentrations of lopinavir, amprenavir, saquinavir and efavirenz were ineffective. These are worrying findings, because suboptimal semen drug concentrations may enhance the risk of sexually transmitted drug-resistant HIV variants.