Tenofovir alafenamide fumarate for the treatment of HIV infection.

• Autores: Rangarajan Sampath, J.D Zeuli, Stacey A. Rizza, Zelalem Temesgen
• Localización: Medicamentos de actualidad = Drugs of today, ISSN 1699-3993, Vol. 52, Nº. 11, 2016, págs. 617-626
• Idioma: inglés
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• Resumen

  • Tenofovir alafenamide fumarate is a recently developed prodrug of tenofovir, a nucleotide analogue reverse transcriptase inhibitor with potent inhibitory activity against HIV. The utility of a previously developed tenofovir prodrug, tenofovir disoproxil fumarate, had been hampered by renal and bone mineral adverse events. Tenofovir alafenamide fumarate overcomes the shortcomings of tenofovir disoproxil fumarate by delivering high intracellular concentrations of the parent drug, tenofovir, while substantially reducing systemic exposure. Tenofovir alafenamide fumarate is currently available as a component of three fixed-dose products: i) coformulation with emtricitabine; ii) coformulation with elvitegravir, cobicistat and emtricitabine; and iii) coformulation with rilpivirine and emtricitabine.