【摘要】：目前多種抗逆轉(zhuǎn)錄病毒準(zhǔn)新藥正在2、3期臨床評價(jià)中。新的核苷逆轉(zhuǎn)錄酶抑制劑tenofoviralafenamidefumarate(TAF)比替諾福韋(tenofovir,TDF)抗病毒活性強(qiáng)且毒性較低;非核苷逆轉(zhuǎn)錄酶抑制劑doravirine對該酶耐受病毒株有效,而新的整合酶抑制劑GSK744具有長效的特點(diǎn)。此外,幾個具有新的作用機(jī)制的化合物也受到關(guān)注,如BMS-663 068小分子化合物是CD4結(jié)合的抑制劑,而cenicriviroc是新穎的CCR5/CCR2受體拮抗劑,具有抗HIV和抗炎的雙重作用。幾類針對潛伏病毒感染的藥物也正在研發(fā)中,其中組蛋白去乙�；敢种苿┌l(fā)展較快,其余大多處于體外篩選階段,如蛋白激酶C激活劑、DNA甲基轉(zhuǎn)移酶抑制劑、陽性轉(zhuǎn)錄延長因子激活劑和組蛋白甲基轉(zhuǎn)移酶抑制劑等。本文對有望近期進(jìn)入臨床使用的新藥和可能逆轉(zhuǎn)HIV潛伏感染的化合物進(jìn)行重點(diǎn)介紹。
[Abstract]:At present, a variety of anti-retroviral quasi-new drugs are in phase 2 3 clinical evaluation. The new nucleoside reverse transcriptase inhibitor (tenofoviralafenamidefumarate (TAF) has stronger antiviral activity and lower toxicity than that of tenofovir (tenofovir,TDF), and the non-nucleoside reverse transcriptase inhibitor (doravirine) is effective against the strain, while the new integrase inhibitor GSK744 has a long effect. In addition, several compounds with new mechanism of action are also concerned, such as BMS-663 068 small molecule compound is an inhibitor of CD4 binding, while cenicriviroc is a novel CCR5/CCR2 receptor antagonist with both anti-HIV and anti-inflammatory effects. Several kinds of drugs for latent virus infection are also under development, among which histone deacetylase inhibitors develop rapidly, and the rest are mostly in the screening stage in vitro, such as protein kinase C activator, DNA methyltransferase inhibitor, Positive activator of transcription extension factor and histone methyltransferase inhibitor. This article focuses on new drugs and compounds that could reverse latent infection of HIV in the near future.
【作者單位】： 加州大學(xué)圣地亞哥醫(yī)學(xué)院傳染病系;
【分類號】：R978.7
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本文編號：2209215