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Lahore University of Management Sciences Introduction to Drug Discovery & Development Course code: Chem-352/Bio-352 Semester offered: Fall 2012-13 Instructors Room No. Office Hours Email Telephone Secretary/TA TA Office Hours Course URL (if any) Dr. Rahman S. Z. Saleem (lead; SSE-Chemistry) Dr. Kamran Haider (SSE-Biology) Dr. Sohail A. Qureshi (SSE-Biology) 9-513 TBA [email protected] 8215 Course Basics Credit Hours Lecture(s) Recitation (per week) Lab (if any ) per week Tutorial (per week) Course Distribution Core Elective Open for Student Category Closed for Student Category 3 Nbr of Lec(s) Per Week Nbr of Rec (s) Per Week Nbr of Session(s) Per Week Nbr of Tut(s) Per Week 2 0 Duration Duration 0 Duration 0 Duration 75 minutes each X COURSE DESCRIPTION Introduction of Drug Discovery and Development is designed for students majoring in Biology or Chemistry (or outside clinicians or pharmacologists) who are keen to learn about how drugs against a bevy of diseases are developed using modern biological and medicinal chemistry methods. Initial phase of this course is devoted to understanding the underlying causes of disease and the process through which disease causing molecules are identified. Subsequent series of lectures cover how cell-based and in vitro biochemical assays are developed and screened, and how lead compounds are identified, optimized and readied for clinical trials. Due to its wide-spread use and success, particular emphasis is placed on structure-based (or rational) drug design using 3-D in silico modeling of targeted molecule. Drug metabolism, delivery and formulation also receive coverage in separate sessions. Final phase of this course deals with economics of drug development as well as legal and ethical issues that are associated with clinical trials and marketing of drugs. COURSE PREREQUISITE(S) CHEM-101 and BIO-101 COURSE OBJECTIVES Lahore University of Management Sciences The overarching objective of this course is to introduce students to the process of how drugs are developed for use in humans or animals. Learning Outcomes After taking this course students should have a basic understanding of: Molecular basis of disease and how biological molecules are identified and targeted for drug development How biological assays are developed, screened and lead compounds identified Structure based drug design and development using in silico modeling Chemical basis of drug design Process of taking lead compounds into clinical trials and subsequent approval by drug agencies Economic and legal aspects of drug development Drug development in the Pakistani context Grading Breakup and Policy Assignment(s): 20% Midterm exam: 40% Final exam: 40% Examination Detail Midterm Exam Yes/No: Yes Combine/Separate: Combine Duration: 2 hours Preferred Date: During class time Exam Specifications: Closed book; no notes or calculator Final Exam Yes/No: Yes Combine/Separate: Combine Duration: 3 hours Exam Specifications: Closed book; no notes or calculator Lahore University of Management Sciences COURSE CONTENT Lecture Topics 1 2 3 4 5 6 7 8 9 10 11 12 13 14 Introduction Drug Discovery – A Historical Perspective st Drug Development in the 21 Century Identification of Drug Targets Assay Development Drugability of Target Molecules Potential Sources of Drugs Compound Libraries: Synthesis, Storage and Use Lead Compound Identification by HTS Stereochemistry in Drug Development Use of Proteins, Nucleic Acids and Antibodies as Drugs Structure-Based Drug Design Introduction to Molecular Visualization and Modeling HANDS-ON SESSION-1 Virtual Screening and High-Throughput Molecular Docking Enhancing Lead Compound Efficiency via StructureActivity Relationship (SAR) Advanced Computational Methods for Ligand Optimization HANDS-ON SESSION-2 Pharmacodynamics, - kinetics and -genomics Drug Delivery and Routes of Administration; Formulation of Drugs Nanoparticles in Drug Delivery Animal Models and Clinical Trials New Drug Approval & Large-Scale Manufacturing Drugonomics Legal Issues, Biosimilars and Generics Ethics of Drug Discovery & Marketing Low Hanging Fruits No More! st 21 Century R&D in Pharmaceutical Industry Pharmaceutical Industry in Pakistan 15 16 17 18 19 20 21 22 23 25 26 27 28 29 Recommended Readings Objectives/ Application Textbook(s)/Supplementary Readings The course covers a wide spectrum of topics that are not available in a single book. However, following books can be consulted: th 1. Wilson & Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry; John Block, John M. Beale, 12 edition, Lippincott Williams & Wilkins, A Wolters Kluwer Business 2011. nd 2. The organic chemistry of drug design and drug action, Richard B. Silverman, 2 edition, Elsevier Academic Press, 2004 th 3. Text book of drug design and discovery, Povl Krogsgaard-Larsen, Ulf Madsen, Kristian Stromgaard, 4 edition, CRC Press 2009 4. Computational drug design: A Guide for Computational and Medicinal Chemists; David C. Young, John Wiley & Sons, Inc. 2009 5. Structural Bioinformatics; Philip E. Bourne and Helge Weissig; John Wiley & Sons, Inc. 2009.