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ABSTRACT
Introduction: Tenofovir alafenamide is a new oral prodrug of tenofovir resulting in relatively low plasma levels and rapid uptake into peripheral blood mononuclear cells in its active form. The United States Food and Drug Administration has now approved this drug coformulated with elvitegravir/cobicistat/emtricitabine, rilpivirine/emtricitabine and emtricitabine. United States guidelines now list this formulation as one of the preferred components of a variety of antiretroviral regimens, and is included as an alternative in other international guidelines, with the notable exception of the World Health Organization, mostly due to limited availability.
Areas covered: This review covers pre-clinical and clinical data searched through PubMed up to August 2016.
Expert opinion: Tenofovir alafenamide is effective as part of an antiretroviral regimen. There is also compelling data that it has less adverse effects on bone mineral density and possibly kidneys than tenofovir disoproxil fumarate. Although approved for use in those with estimated glomerular filtration rates as low as 30 mL/min, data is somewhat limited in this group. While there are few reasons to not use tenofovir alafenamide as a substitute for tenofovir disoproxil fumarate, the former should not be used with rifamycins, is not yet recommended in pregnancy and needs to be studied further before it can be considered as part of a pre-exposure prophylaxis regimen.
Declaration of interest
K Corado has received research support from Gilead Sciences Inc. and ViiV Healthcare. E S Daar has received research support from Gilead Sciences Inc., Merck, and ViiV Healthcare, he is also a consultant for Bristol-Myers Squibb, Gilead Sciences Inc., Janssen, Merck, Teva, and ViiV Healthcare. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.