Optimizing the Lead Compound Pharmacokinetic and Pharmaceutical Phases

5 OPTIMIZING THE LEAD COMPOUND PHARMACOKINETIC AND PHARMACEUTICAL PHASES [Pg.146]

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. [Pg.146]

1 Overview of Metabolic Reactions Affecting Drug Molecules [Pg.146]

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. [Pg.147]

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. [Pg.147]

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