Mechanistic Basis of Cabotegravir–Glucuronide Disposition in Humans

  title={Mechanistic Basis of Cabotegravir–Glucuronide Disposition in Humans},
  author={Mitesh G. Patel and H. Christian Eberl and Andrea Wolf and Esaie Pierre and Joseph W. Polli and Maciej J. Zamek-Gliszczynski},
  journal={The Journal of Pharmacology and Experimental Therapeutics},
  pages={269 - 277}
Cabotegravir, a novel integrase inhibitor under development for treatment and prevention of HIV, is primarily metabolized by UGT1A1 and UGT1A9 to a direct ether glucuronide metabolite. The aim of these studies was to elucidate the mechanistic basis of cabotegravir–glucuronide disposition in humans. Cabotegravir glucuronidation was predominantly hepatic (>95%) with minimal intestinal and renal contribution. Rat liver perfusions demonstrated that cabotegravir–glucuronide formed in the liver… 

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