title: Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF).
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.
authors.affiliation: KU Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Minderbroedersstraat 10, B-3000 Leuven, Belgium. Electronic address: erik.declercq@kuleuven.be.
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
mesh_terms: D000225:Adenine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000191:economics / Q000627:therapeutic use; D000409:Alanine; D000998:Antiviral Agents / Q000008:administration & dosage / Q000191:economics / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy* / Q000517:prevention & control; D006801:Humans; D000068698:Tenofovir / Q000008:administration & dosage / Q000191:economics / Q000627:therapeutic use* / Q000031:analogs & derivatives
chemical_list: D000998:Antiviral Agents; D000068698:Tenofovir; C442442:tenofovir alafenamide; D000225:Adenine; D000409:Alanine
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)