Darunavir:一个全面的简介。

Q1 Pharmacology, Toxicology and Pharmaceutics Profiles of drug substances, excipients, and related methodology Pub Date : 2021-01-01 Epub Date: 2020-08-21 DOI:10.1016/bs.podrm.2020.07.001
Ibrahim A Darwish, Abdulrahman A Al-Majed, Nawaf A Alsaif, Ahmed H Bakheit, Rashed N Herqash, Abdullah Alzaid
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引用次数: 4

摘要

Darunavir: (3R,3aS,6aR)-六氢呋喃[2,3-b]呋喃-3-基[(2S,3R)-4-{[(4-氨基苯基)磺酰](异丁基)氨基}-3-羟基-1-苯基-2-丁基]氨基甲酸酯是一种合成的非肽蛋白酶抑制剂。2006年6月,它首次被美国食品和药物管理局(FDA)批准用于治疗耐药1型人类免疫缺陷病毒(HIV)。2016年7月,FDA扩大了darunavir在感染HIV的孕妇中使用的批准。Darunavir通过抑制HIV-1蛋白酶的催化活性来阻止HIV病毒的复制,并选择性地抑制病毒感染细胞中HIV编码的Gag-Pol多蛋白的裂解,从而阻止成熟感染性病毒颗粒的形成。Darunavir在目前可用的蛋白酶抑制剂中是独一无二的,因为它对多种多重耐药的HIV毒株保持抗逆转录病毒活性。本文通过对文献的批判性广泛回顾,讨论了darunavir在其名称、配方、元素组成、外观和在治疗hiv感染患者中的使用方面的描述。本文还讨论了达那韦的制备方法、理化性质、测定方法、药理学性质和给药情况。
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Darunavir: A comprehensive profile.

Darunavir: (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl] (isobutyl)amino}-3-hydroxy-1-phenyl-2-butanyl]carbamate is a synthetic non-peptide protease inhibitor. On June 2006, it was first approved by the Food and Drug administration (FDA) for treatment of resistant type-1 of the human immunodeficiency virus (HIV). In July 2016, the FDA expanded the approval for use of darunavir in pregnant women with HIV infection. Darunavir prevents the replication of HIV virus by inhibiting the catalytic activity of the HIV-1 protease enzyme, and selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in virus-infected cells, which prevents the formation of mature infectious virus particles. Darunavir is unique among currently available protease inhibitors because it maintains antiretroviral activity against a variety of multidrug-resistant HIV strains. This article discusses, by a critical extensive review of the literature, the description of darunavir in terms of its names, formulae, elemental composition, appearance, and use in the treatment of HIV-infected patients. The article also discusses the methods for preparation of darunavir, its physical-chemical properties, analytical methods for its determination, pharmacological properties, and dosing information.

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来源期刊
Profiles of drug substances, excipients, and related methodology
Profiles of drug substances, excipients, and related methodology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
13.10
自引率
0.00%
发文量
4
期刊最新文献
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