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[新型逆转录酶抑制剂的研发]

[Development of new reverse transcriptase inhibitors].

作者信息

Kodama Eiichi

机构信息

Laboratory of Virus Immunology, Research Center for AIDS, Institute for Virus Research, Kyoto University.

出版信息

Nihon Rinsho. 2002 Apr;60(4):775-9.

PMID:11968787
Abstract

Highly active anti-retroviral therapy(HAART) using two or more reverse transcriptase inhibitors(RTIs) and protease inhibitors, has dramatically improves the quality of life and survival of patients infected with human immunodeficiency virus(HIV). RTIs are categorized by their mechanism of action, into two groups, nucleoside(N) and non-nucleoside(NN) RTIs. However, resistant HIV variants against NRTIs and/or NNRTIs including multi-drug resistant, emerge after the prolonged therapy. To suppress the replication of such resistant variants, numerous anti-HIV drugs have been developed. In this review, the mechanisms of action and characters of the major drugs in clinical or under preclinical are described.

摘要

使用两种或更多逆转录酶抑制剂(RTIs)和蛋白酶抑制剂的高效抗逆转录病毒疗法(HAART)显著改善了感染人类免疫缺陷病毒(HIV)患者的生活质量和生存率。RTIs根据其作用机制分为两组,即核苷类(N)RTIs和非核苷类(NN)RTIs。然而,长期治疗后会出现针对核苷类逆转录酶抑制剂和/或非核苷类逆转录酶抑制剂的耐药HIV变异株,包括多药耐药株。为了抑制此类耐药变异株的复制,人们研发了多种抗HIV药物。在本综述中,将描述临床或临床前主要药物的作用机制和特点。

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