Preface

Drug metabolism and pharmacokinetics (DMPK) is an important discipline in drug discovery and development programs, which deal with biotransformation and other pharmacokinetic parameters to assess a drug's safety. DMPK basically evaluates a drug's absorption, distribution, metabolism, and excretion (ADME) properties, enabling the discovery and development of a safe and efficacious drug molecule. An understanding of the DMPK process and associated properties is an essential requirement for a candidate drug to become a successful therapeutic agent. Preclinical studies with satisfactory pharmacokinetic, metabolic, and toxicological data reduce failure rates of drug candidates in the clinical phase of drug discovery. Besides adequate potency against the therapeutic target and an acceptable safety profile, a balance of optimized PK properties and minimized drug–drug interactions (DDIs) maximizes the chance of a candidate drug becoming a successful therapeutic agent. In recent times, there has been increased attention on evaluating the pharmacokinetic and safety profile of drug candidates, which includes various pharmacokinetic parameters (aqueous solubility, lipophilicity, cell permeability, bioavailability, protein binding, and metabolism and elimination half-life), DDIs, and toxicokinetics. Various in silico tools and in vitro/in vivo experimental techniques are applied to predict/ evaluate such parameters as a rational strategy for the design, optimization, and selection of successful drug candidates. Such studies can help researchers and drug developers predict potential risks of failure early in drug development, as well as provide pre-clinical evidence to conduct clinical trials.

#### **Mithun Rudrapal**

Department of Pharmaceutical Sciences, School of Biotechnology and Pharmaceutical Sciences, Vignan's Foundation for Science, Technology and Research (Deemed to be University), Guntur, India
