Pharmacokinetics and Pharmacodynamics: Fundamentals and Role(s) in Drug Discovery and Development

The process of finding new drugs begins with the identification of a target and its validation, then hits are found, leads are generated, and they are optimized. Eventually, a suitable and appealing candidate is chosen, who will then be sent for further development. This chapter's primary goal is to provide an overview of the fundamental concepts behind pharmacokinetics (PK) and pharmacodynamics (PD), as well as how PK works. In the many stages of the drug discovery and development procedures, pharmacodynamics is used. Pharmacokinetic parameters from PK experimental research are used to comprehend and anticipate the drug response, such as clearance, apparent Vd and elimination half-life, and bioavailability. This chapter also discusses the different types of compartmental models with their implications for drug development. Principles from pharmacodynamics are used to enable the safe and effective therapeutic management of patients; hence, various receptor and non-receptor-mediated mechanisms of action are included in this chapter. To assure the accuracy of the PK data generated in the drug development process, it is crucial to establish and validate an appropriate bioanalytical procedure; the application of LC-MS methods in bioanalysis has been discussed in this chapter.