Role of Metabolites in Safety Testing: A Brief Review Goyal Sarita1,,*, Jindal Pooja1, Gupta MC2 1Assistant Professor, Pharmacology Department, Pt. BD Sharma PGIMS, Rohtak, Haryana, India 2Senior Professor and Head, Pharmacology Department, Pt. BD Sharma PGIMS, Rohtak, Haryana, India *Corresponding author email id: drsaritagoyal@rediffmail.com
Abstract Drug discovery and development is the process of generating compounds and evaluating all their properties to determine the feasibility of selecting one new chemical entity to become a safe and efficacious drug. Metabolism by the host organism is one of the most important determinants of the pharmacokinetic profile of a drug. After administration, a drug is usually converted in the liver by various enzymes to a variety of metabolites. Formation of active or toxic metabolites will have an impact on the pharmacological and toxicological outcomes. There is also potential for drug-drug interactions with co-administered drugs due to inhibition or induction of drug metabolism pathways. Hence, optimisation of the metabolic liability and drug-drug interaction potential of the new chemical entities are some of the most important steps during the drug discovery process. Improved technology has allowed better identification and quantification of metabolites, raising new issues to be addressed during the course of drug development. Recently, a lot of effort has been applied to develop predictive methods to aid the optimisation process during drug discovery and development. This article reviews the role of drug metabolism in drug discovery and development. Top Keywords Metabolites, Pharmacokinetics, Pharmacodynamics, Molecular entities, Good laboratory practices Drug-drug interaction. Top |