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Tenofovir alafenamide for HIV: time to switch?

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Cited by (6)

  • Pharmacokinetics of a weekly transdermal delivery system of tenofovir alafenamide in hairless rats

    2020, International Journal of Pharmaceutics
    Citation Excerpt :

    Tenofovir alafenamide (TAF, also known as GS-7340) is a potent tenofovir (TFV) prodrug against human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections (Brahmania et al., 2016; Liu et al., 2017; Ray et al., 2016; Wyatt and Baeten, 2015). In comparison with the last generation TFV prodrug, tenofovir disoproxil fumarate (TDF), TAF shows improved stability in the systemic circulation, a reduced systemic TFV exposure, as well as an enhanced lymphoid cell and tissue loading, and thus having more favorable oral pharmacokinetic (PK) properties, better renal and bone safety profiles, and a higher resistance barrier (Babusis et al., 2013; De Clercq, 2016; Dhanireddy and Baeten, 2016; Margot et al., 2016; Ruane et al., 2013; Sax et al., 2015). TAF has been in the replacement for TDF for the treatment of HIV-1 infections (De Clercq, 2018).

  • Role of tenofovir alafenamide (TAF) in the treatment and prophylaxis of HIV and HBV infections

    2018, Biochemical Pharmacology
    Citation Excerpt :

    Resistance selection experiments using HIV isolates harboring pre-existing TFV resistance (K65R, M41L, L210W, T25Y, Q151M) were carried out with TAF and TFV to investigate the potential for the induction of additional resistance-associated mutations (RAMs), but, after 6 months in culture, no new mutations were detected, except for L429I and T69I, that were further characterized and found to have very limited or no role in resistance to TAF or TFV [57]. Now that TDF has been replaced by TAF for the treatment of HIV-1 infections, the question could be raised whether TAF may also be advocated for the pre-exposure prophylaxis (PrEP) of HIV infections [58,59]. The combination of TDF with emtricitabine (Truvada®) has been approved by the US Food and Drug Administration for the prophylaxis of HIV infections on 16 July 2012.

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

    2016, Biochemical Pharmacology
    Citation Excerpt :

    In fact, switching from E/C/F/TDF to E/C/F/TAF in HIV-positive patients with mild or moderate renal impairment, can be perfectly well rationalized, as it significantly improved proteinuria (albuminuria) and bone mineral density [32]. Patients and providers have long been averse to changing HIV treatment regimens [33], essentially based on the principle of “not changing a winning team”. However, the risk of long-term toxicity [34] and the cost-effectiveness of long-acting antiretroviral therapy [35] justify switching from TDF to TAF, as part of the newer ART combination of E/C/F/TAF.

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