Lead Discovery & Optimization in Drug Development
Master innovative techniques for identifying and enhancing potential drug compounds, accelerating their development from laboratory to clinical trials.
Master innovative techniques for identifying and enhancing potential drug compounds, accelerating their development from laboratory to clinical trials.
This intermediate-level course focuses on lead selection and optimization in drug development. Students will explore techniques for identifying promising molecules, selecting the best leads, and optimizing their properties for clinical trials. The curriculum covers screening methods, hit validation, pharmacophore determination, and strategies for improving efficacy, pharmacokinetics, and safety profiles. Through a combination of video lectures, readings, and assessments, participants will gain a comprehensive understanding of the drug discovery process, from initial compound screening to lead optimization. The course emphasizes practical applications, including the use of x-ray crystallography, matched pair analysis, and bioisosteres in lead optimization. Designed for those with a background in pharmacology and organic chemistry, this course provides valuable insights into the critical steps between initial drug discovery and clinical trials.
Instructors:
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What you'll learn
Understand general approaches for finding compounds with activity on drug targets
Master methods for confirming target engagement by active compounds
Learn techniques for communicating the pharmacophore of active molecules
Apply criteria to prioritize biologically active compounds as potential leads
Analyze types of information used to guide lead optimization decisions
Identify functional groups used to improve PK properties without affecting on-target activity
Skills you'll gain
This course includes:
PreRecorded video
Graded assignments, exams
Access on Mobile, Tablet, Desktop
Limited Access access
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There are 3 modules in this course
This course provides a comprehensive overview of lead discovery and optimization in drug development. It covers the entire process from initial screening to final lead selection and optimization. Students will learn about various screening methods, hit validation techniques, and criteria for selecting promising leads. The course delves into advanced topics such as pharmacophore determination, structure-activity relationships, and strategies for improving pharmacokinetic properties. A significant focus is placed on lead optimization techniques, including the use of x-ray crystallography, matched pair analysis, and bioisosteres. The curriculum also addresses important considerations in drug development, such as balancing efficacy with safety and the transition from lead-like to drug-like compounds. Through a combination of theoretical knowledge and practical examples, students will gain a deep understanding of the critical steps in advancing a compound towards clinical trials.
Week 1
Module 1
Week 2
Module 2
Week 3
Module 3
Fee Structure
Instructor
7 Courses
Medicinal Chemistry Expert and Educator at Davidson College
Dr. Erland Stevens is a distinguished faculty member in the Chemistry department at Davidson College, bringing a wealth of experience in medicinal chemistry and drug discovery to his role. After earning his Ph.D. from the University of Michigan at Ann Arbor in 1997, specializing in nitrogen heterocycles under Will Pearson, Stevens pursued postdoctoral studies at The Scripps Research Institute with K. Barry Sharpless. Joining Davidson College in 1998, he has since become a cornerstone of the chemistry program, regularly teaching medicinal chemistry to junior and senior undergraduates. Stevens' expertise extends beyond academia, as evidenced by his involvement in the continuing education program at GlaxoSmithKline's Research Triangle Park site in 2006 and 2007. His contributions to the field include authoring the textbook "Medicinal Chemistry: The Modern Drug Discovery Process," published by Pearson Education, which has likely become a valuable resource for students and professionals in the field. Stevens' research focuses on the synthesis and activity of antiviral nucleoside analogues, demonstrating his ongoing commitment to advancing pharmaceutical science. His career exemplifies the integration of academic research, industry relevance, and dedicated teaching in the field of medicinal chemistry.
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