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Review
. 2016 Nov 1:119:1-7.
doi: 10.1016/j.bcp.2016.04.015. Epub 2016 Apr 29.

Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF)

Erik De Clercq  1
Affiliations
Review

Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF)

Erik De Clercq. Biochem Pharmacol. .

Abstract

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 (10mg) than TDF (300mg). TAF has been approved in November 2015 (in the US and EU), as a single-tablet regimen (STR) containing 150mg elvitegravir (E), 150mg cobicistat (C), 200mg emtricitabine [(-)FTC] (F) and 10mg TAF, marketed as Genvoya®, on 01 March 2016 in the US as an STR containing 25mg rilpivirine (R), 200mg F and 25mg TAF, marketed as Odefsey®, and on 4 April 2016 in the US, as an STR containing 200mg F and 25mg TAF, marketed as Descovy®, 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.

Keywords: Cobicistat (PubChem CID: 25151504); Darunavir, Prezista® (PubChem CID: 213039); Efavirenz, Sustiva® (PubChem CID: 64139); Elvitegravir (PubChem CID: 5277135); Emtricitabine [(−)FTC], Emtriva® (PubChem CID: 60877); HBV (hepatitis B virus); HIV (human immunodeficiency virus); Rilpivirine, Edurant® (PubChem CID: 6451164); TAF (tenofovir alafenamide); TDF (tenofovir disoproxil fumarate); TFV (tenofovir); Tenofovir [(R)-PMPA] (PubChem CID: 464205); Tenofovir alafenamide (TAF), GS-7340 (PubChem CID: 9574768); Tenofovir disoproxil fumarate (TDF), Viread® (PubChem CID: 6398764).

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