Course

Unit 1

Introduction, Definition of drug, Composition of drug, Properties of drug, Druggable genome, Biologics, Properties of Biologics, Similarities and differences with respect to Chemical Entities, Target identification and validation: Different types of targets, Methods of target identification, Phenotypic screening, Chemoproteomics, Gene association studies, Transgenics, Compound Libraries, Combi-chem, Computer Aided Drug Discovery (CADD), Fragment Based Drug Discovery (FBDD).

Unit 2

Assay development: Introduction and Importance, Primary screening, Outcomes: Hit identification and re-confirmation Secondary screening, IC₅₀ determination, Lead discovery and optimization, Pharmacophore, SAR studies, Rational drug design, Toxicity studies – Different types: acute, sub-acute chronic, Safety evaluation, Clinical studies, Features, Different types: Phase 1, 2, 3 and 4, Biologics steps in drug development, Biological drug development process, Cloning in biologics development, Hybridoma technology, Bioreactors, Batch, Fed-batch and Continuous cultures, Techniques for purification, Formulation development, Types of antibodies.

Unit 3

Cancer and Chemotherapy, Alkylating agents, Antimetabolites, Folic acid antagonists, Purine antagonists, Pyrimidine antagonists, Antibiotics, Estrogen therapy, Androgen therapy, Aromatase inhibitors, Drugs derived from natural products, Tyrosine kinase inhibitors.

Unit 4

Metabolism, Mechanism of action, Detoxification reactions, Phase I – functionalization reactions, Phase II – conjugation reactions, Structure toxicity relationships, Reactive metabolites, Factors influencing drug metabolism, Metabolic enzyme induction, Biological factors, Prodrugs, Prodrugs to improve membrane permeability, Drugs recognized by transport proteins, Prodrugs to prolong drug activity, Prodrugs masking drug toxicity and side effects, Prodrugs to improve water solubility, Prodrugs to increase chemical stability, Prodrugs activated by external influence.

LEARNING OBJECTIVE:

The course aims to familiarize students with the fundamental concepts of drugs, including their properties, and biologics. It seeks to introduce various methods for target identification and validation, such as phenotypic screening and chemoproteomics. Students will learn about the processes involved in assay development, lead discovery, and optimization, including techniques like computer-aided drug discovery and SAR studies, chemotherapeutic agents and their properties. Additionally, the course covers the processes involved in drug metabolism, mechanisms of action, toxicity evaluation, and the role of prodrugs in enhancing drug efficacy and safety

COURSE OUTCOMES:

CO1: Acquire a comprehensive understanding of the fundamental concepts of drug discovery and development, including the definition and properties of drugs, biologics, the druggable genome, target identification and validation techniques, and methods such as computer-aided and fragment-based drug discovery.

CO2: Develop the ability to design drug screening assays, SAR studies, and rational drug design, along with understanding toxicity evaluation, pharmacophore modeling, and processes involved in biologics development, and formulation.

CO3: Gain comprehensive knowledge of cancer biology and chemotherapy, including the mechanisms of action, classes of anticancer agents and to understand their application in cancer treatment

CO4: Comprehend drug metabolism pathways, the rationale behind prodrug design, and factors influencing drug efficacy and safety

REFERENCES

1. Pharmaceutical Biotechnology

Daan J. A. Crommelin, Robert D. Sindelar, Bernd Meibohm

Springer Nature, Switzerland, Sixth Edition, 2024.

2. Principles of Pharmacology
3. Golan, A. Tashjian, E. Armstrong, J. Galanter, A.W. Armstrong, R. Arnaout, H. Rose

Lippincott Williams and Wilkins/Wolters Kluwer, Baltimore, Seventh Edition, 2011.

3. Goodman and Gilman’s The Pharmacological Basis of Therapeutics

Laurence L. Brunton, John S. Lazlo, Keith L. Parker

McGraw Hill, Singapore, Eleventh Edition, 2006.

4. Foye’s Principles of Medicinal Chemistry

Thomas L. Lemke, David A. Williams, Victoria F. Roche, S. William Zito

Lippincott Williams and Wilkins/Wolters Kluwer, Baltimore, Seventh Edition, 2013.