Emtricitabine + tenofovir alafenamide for the treatment of HIV.
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.
a Division of HIV Medicine, Department of Internal Medicine , Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center , Torrance CA , USA.
Katya C
KC
Corado
a Division of HIV Medicine, Department of Internal Medicine , Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center , Torrance CA , USA.
Eric S
ES
Daar
D000225:Adenine / Q000031:analogs & derivatives* / Q000627:therapeutic use; D019380:Anti-HIV Agents / Q000627:therapeutic use*; D015519:Bone Density / Q000187:drug effects; D000068679:Emtricitabine / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D007668:Kidney / Q000187:drug effects; D007963:Leukocytes, Mononuclear / Q000378:metabolism; D011355:Prodrugs; D000068698:Tenofovir / Q000627:therapeutic use*
D019380:Anti-HIV Agents; D011355:Prodrugs; C000613801:emtricitabine tenofovir alafenamide; D000068698:Tenofovir; D000068679:Emtricitabine; D000225:Adenine
Bone mineral density; darunavir/cobicistat; elvitegravir/cobicistat; emtricitabine/tenofovir alafenamide; proximal renal tubulopathy; tenofovir; tenofovir alafenamide; tenofovir disoproxil fumarate