期刊
BIOCHEMICAL PHARMACOLOGY
卷 119, 期 -, 页码 1-7出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2016.04.015
关键词
TAF (tenofovir alafenamide); TDF (tenofovir disoproxil fumarate); TFV (tenofovir); HIV (human immunodeficiency virus); HBV (hepatitis B virus)
Tenofovir alafenamide (TAF) can be considered a new prodrug of tenofovir (TFV), as successor of tenofovir disoproxil fumarate (TDF). It is in vivo as potent against human immunodeficiency virus (HIV) at a 30-fold lower dose (10 mg) than TDF (300 mg). TAF has been approved in November 2015 (in the US and EU), as a single-tablet regimen (STR) containing 150 mg elvitegravir (E), 150 mg cobicistat (C), 200 mg emtricitabine [(-)FTC] (F) and 10 mg TAF, marketed as Genvoya (R), on 01 March 2016 in the US as an STR containing 25 mg rilpivirine (R), 200 mg F and 25 mg TAF, marketed as Odefsey (R), and on 4 April 2016 in the US, as an STR containing 200 mg F and 25 mg TAF, marketed as Descovy (R), for the treatment of HIV infections. STR combinations containing TAF and emtricitabine could be paired with a range of third agents, for example, darunavir and cobicistat. TAF has a much lower risk of kidney toxicity or bone density changes than TDF, and also offers long-term potential in the pre-exposure prophylaxis (PrEP) of HIV infections. TAF is specifically accumulated in lymphatic tissue, and in the liver, and hence also holds great potential for the treatment of hepatitis B virus (HBV) infections. Akin to TDF, TAF is converted intracellularly to TFV. Its active diphosphate metabolite (TFVpp) is targeted at the RNA-dependent DNA polymerase (reverse transcriptase) of either HIV or HBV. (C) 2016 Elsevier Inc. All rights reserved.
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