Predicting the Intravenous Pharmacokinetics of Covalent Drugs in Animals and Humans
Covalent Modifiers
AUGUST 4, 2024
Rowan Stringer and Tobias Kaster Journal of Medicinal Chemistry 2024 DOI: 10.1021/acs.jmedchem.4c00776 30 covalent drugs were used to assess clearance (CL) prediction reliability in animals and humans. In animals, marked CL underprediction was observed using cryopreserved hepatocytes or liver microsomes (LMs) supplemented for cytochrome P450 activity.
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