Lead Selection & Optimization

О курсе

This course covers the stages of drug discovery in which promising compounds (leads) are identified, their optimal and suboptimal characteristics determined, and the suboptimal characteristics optimized to create a candidate suitable for the clinic.  The course is built around a case study on the discovery of an antimalarial therapy.  Assays useful for screening new compounds are outlined, examples of selection criteria for leads are discussed - such as potency, efficacy, and pharmacokinetics - and the structure activity relationships that contribute to the optimization of a lead series are considered.  The phenotypic approach used by the antimalarial program will be briefly contrasted with a target-based program on a different target. Target audience: This course is suitable for life scientists, clinicians, and individuals from fields that support drug discovery (e.g., patents, finance, licensing, etc.) interested in learning more about the pharmaceutical/biotechnology sector. Advanced undergraduate coursework or practical familiarity/working knowledge in biological sciences and organic chemistry is recommended.

Навыки, которые вы освоите

Учитесь у экспертов

Erland Stevens, PhD

James G. Martin Professor of Chemistry, Davidson College

W. Ross Tracey, PhD

Associate Director, Biomedical Research Learning, Novartis

Douglas S. Auld, PhD

Associate Director, Discovery Sciences, Biomedical Research, Novartis

Alan P. Brown, PhD, DABT

Director, Preclinical Safety, Biomedical Research, Novartis

Sujal Deshmukh, PhD

Director, Pharmacokinetic Sciences, Biomedical Research, Novartis

Stephanie Dodd, MSc.

Associate Director, Chemical & Pharmaceutical Profiling, Development, Novartis

Sabine Guth, PhD

Director, Diseases Of Aging and Regenerative Medicine, Biomedical Research, Novartis

Thomas M. Smith, PhD

Associate Director, Early Strategic Partnerships Biomedical Research, Novartis