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The Absolute Bioavailability and Absorption, Metabolism, and Excretion of Ipatasertib, a Potent and Highly Selective Protein Kinase B (Akt) Inhibitor.

Drug Metab Dispos

October 2023

Drug Metabolism and Pharmacokinetics (R.H.T., B.M.L., S.C., Y.D., B.D., S.M.), Clinical Pharmacology (V.M., R.S., S.K., L.M.), BioAnalytical Sciences (J.N.), Small Molecule Pharmaceutics (E.Y.), and Small Molecule Analytical Chemistry (M.A.A.-S.), Genentech Inc., South San Francisco, California.

Article Synopsis
  • Ipatasertib (GDC-0068) is a targeted cancer treatment being developed by Genentech/Roche, focusing on inhibiting the Akt protein kinase, with studies examining its effects both alone and with other therapies.
  • An open-label study with radiolabeled ipatasertib assessed how the drug is absorbed, metabolized, and excreted, showing a bioavailability of 34.0% and similar terminal half-lives for oral and intravenous forms.
  • The majority of the drug recovered was metabolized, primarily through hepatic pathways, with the main metabolic process being -dealkylation facilitated by the CYP3A enzyme.
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