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The Role of Biotransformation in Drug Discovery and Development

Selamu Kebamo, Shibiru Tesema and Bekesho Geleta

Biotransformation is a process by which organic compounds are transformed from one form to another, aided by organisms such as bacteria, fungi and enzymes. It plays a major role and determines the fate of the prospective drugs. Biotransformation must take place only after the drugs reach their specific target site and produce the desired effects. In addition, the nature of the metabolites produced from the drug, must be thoroughly studied; otherwise, the drugs would be rejected during the screening process. Hence, drug metabolism is a major criterion in the highthroughput screening of prospective drugs. Biotransformation has an important role in the determination of the pharmacokinetic parameters like oral bioavailability, drug-drug interaction, clearance and the half-life of the entity within the cell. It is very essential in the toxicity studies too. Biotransformation is used as a valuable strategy to build molecules, similar to parent drug in the drug discovery programme. It can play an important role in identifying factors underlying the problems, facilitate the optimal selection of compounds for further development, provide information on metabolites for possible improvement in drug design, and contribute to the identification of the appropriate animal species for subsequent toxicity testing. Hence, so