Medicinal Chemistry

The Drug Metabolism/Bioanalytical Chemistry team at the Merck Frosst Centre for Therapeutic Research is part of the Medicinal Chemistry department. This integration into the drug discovery process accelerates the rate at which drug candidates can be tested in human in vitro systems. Using microsomal fractions, hepatocytes and recombinant enzymes from human sources, scientists are able to identify metabolic liabilities and reject unsuitable drug candidates early.

Click here to enlarge

Biotransformations in the intestine, kidney, liver, lung, brain and bloodstream produce metabolites that must be characterized for toxicity and activity. For the SINGULAIR^® (montelukast sodium) programs, human metabolites were identified and tested even before the drug was administered to people. During that program the metabolism team also worked with chemists at Merck Frosst to identify drugs with appropriate rates of metabolism, to ensure favorable dosing regimens.

® Registered Trademark of Merck & Co., Inc. Used under license.