This course is intended for graduate students seeking to gain a comprehensive understanding of the drug discovery process. The course will present an in-depth overview, starting with target selection, where students will learn how to identify and validate potential biological targets for therapeutic intervention. Following this, the course will cover screening methods at the target level, where students will explore various techniques used to identify active compounds known as hits. They will learn about different types of libraries of compounds including virtual libraries. Students will then delve into the process of hit identification, learning how to analyze and interpret screening data to select promising hits for further development. The course will also address the optimization process, guiding students through the steps required to refine hits into lead compounds with improved potency, selectivity, and drug-like properties. This includes an examination of structure-activity relationships (SAR) and the application of medicinal chemistry strategies. A significant component of the course will cover ADME (Absorption, Distribution, Metabolism, and Excretion) studies. Students will gain insights into how these pharmacokinetic properties impact the drug discovery process, including the evaluation of a compound’s bioavailability, distribution in the body, metabolic stability, and permeability. Understanding ADME is crucial for predicting the in vivo behaviour of drug candidates and for optimizing their pharmacokinetic profiles.

Additionally, the course will cover the transition from lead optimization to the identification of preclinical candidates. Students will study the criteria for selecting a candidate suitable for preclinical development, including pharmacokinetics, toxicity, and scalability of synthesis. The preclinical candidate phase involves rigorous testing in vitro and in vivo to ensure the compound's safety and efficacy before moving into clinical trials. The course will also discuss reasons for preclinical and clinical failure of drug candidates.

By the end of the course, students will have a robust understanding of the entire drug discovery process, from initial target selection to the identification of a viable preclinical candidate. They will gain insights into the challenges and strategies involved in each stage, equipping them with the knowledge and skills necessary for careers in the pharmaceutical and biotechnology industries. Successful completion of the course will enable students to comprehend the modern approaches and technological advancements that drive drug discovery today.