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Dapivirine

英文名称: 4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile

CAS号:244767-67-7 分子式:C20H19N5 分子量:329.39800

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简介

Dapivirine (TMC120) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) developed at Janssen Therapeutics (formerly Tibotec Therapeutics). The International Partnership for Microbicides (IPM) has held exclusive worldwide rights to dapivirine since 2014, building upon a 2004 royalty-free license to develop dapivirine-based microbicides for women in resource-poor countries.
A monthly intravaginal ring containing dapivirine has been developed as a form of HIV prevention for women. Two Phase 3 clinical trials of intravaginal dapivirine rings for HIV prevention were completed in 2015 and results were announced at the 2016 Conference on Retrovirology and Opportunistic Infections (CROI). The ASPIRE Study (MTN-020) reported a 27% reduction in HIV-1 acquisition (95% CI 12-57%, p=0.007), with a trend toward greater protection in women over age 21 and no significant protection for women under age 21. The Ring Study (IPM-027) reported a 31% reduction in HIV acquisition (95% CI 0.9-51.5%, p=0.040) also with a trend toward greater efficacy in women over age 21. In both trials, more than 80% of returned rings showed signs of drug depletion indicating at least some use, and more than 80% of blood samples from participants in the active arm had levels of dapivirine consistent at least 8 hours of continuous use preceding the blood test. Neither trial could evaluate whether the product was used consistently between study visits.

基本信息

中文名称 Dapivirine 英文名称 4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile
中文别名

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英文别名

4-({4-[(2,4,6-trimethylphenyl)amino]pyrimidin-2-yl}amino)benzenecarbonitrile; Dapivirine (TMC120); TMC120; 4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile; Dapivirine; UNII-TCN4MG2VXS; dapivirinum;

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CAS号 244767-67-7 分子式 C20H19N5
分子量 329.39800 精确质量 329.16400
PSA 73.63000 LOGP 4.90668

编号系统

MDL号 MFCD09833899

物化性质

密度:
1.23g/cm3
沸点:
557.9ºC at 760mmHg
闪点:
291.2ºC
折射率:
1.648
蒸汽压:
1.76E-12mmHg at 25°C
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上游原料
4-(4-chloro-6-(mesitylamino)pyrimidin-2-ylamino)benzonitrile 对氨基苯腈 4-N[2(4,6-二氯吡啶基)]-氨基苯腈

Dapivirine

CAS号:244767-67-7 分子式:C20H19N5 分子量:329.39800

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