Nature Communications (Sep 2021)

Transformation of tenofovir into stable ProTide nanocrystals with long-acting pharmacokinetic profiles

  • Denise A. Cobb,
  • Nathan Smith,
  • Suyash Deodhar,
  • Aditya N. Bade,
  • Nagsen Gautam,
  • Bhagya Laxmi Dyavar Shetty,
  • JoEllyn McMillan,
  • Yazen Alnouti,
  • Samuel M. Cohen,
  • Howard E. Gendelman,
  • Benson Edagwa

DOI
https://doi.org/10.1038/s41467-021-25690-5
Journal volume & issue
Vol. 12, no. 1
pp. 1 – 16

Abstract

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Antiretroviral therapy (ART) for the treatment of HIV-1 requires life-long daily adherence to supress viral replication, and nucleoside reverse transcriptase inhibitors that are commonly used in ART have not been converted into long-acting agents. Here, the authors report two lipophilic tenofovir (TVF) ProTide nanoformulations, NM1TFV and NM2TFV, which sustain drug levels above therapeutic concentrations for two months after a single intramuscular dose in rats.