Optimizing the Lead Compound Pharmacokinetic and Pharmaceutical Phases

5 OPTIMIZING THE LEAD COMPOUND PHARMACOKINETIC AND PHARMACEUTICAL PHASES 

Once the lead dmg molecule has been optimized for the pharmacodynamic phase, it must next be optimized for the pharmacokinetic and pharmaceutical phases. If a dmg molecule cannot withstand the trip from the gut to the receptor microenvironment, it makes no difference whether the drug actually binds to the receptor. 

1 Overview of Metabolic Reactions Affecting Drug Molecules 

The previous section listed the various reactions that the body can inflict upon a drug molecule. This section presents brief examples of a number of these reactions. 

Oxidation Aliphatic Carbon Atoms. Oxidation at the terminal carbon atom of an alkyl substituent is co-oxidation oxidation of the carbon atom located second from the end is co-1 oxidation. Unless specifically catalyzed by an enzyme, co-1 oxidation tends to occur more frequently. The anticonvulsant drug ethosuximide is metabolized at both the CO and co-1 position. 

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