The Discovery and Development of Atrasentan, An Endothelin Antagonist

Palestrante:  Dr. Thomas W. Von Geldern – Consultor da MMV e da DNDi

Resumo: Endothelin (ET) is a potent vasoconstrictor peptide, which also induces proliferation of vascular tissues. As such, it has attracted attention from pharma as a target for multiple therapeutic indications. This presentation will summarize the work of Abbott researchers to develop a series of selective ET-receptor antagonists, and their use to explore the role of these receptors in various disease states. As a result of these studies, we eventually selected the ET-A selective antagonist ABT-627 (Atrasentan) as a drug candidate. The talk will focus on medicinal chemistry studies and will highlight key pharmacologic and clinical milestones.

Biografia: Tom von Geldern has been an independent consultant to the pharmaceutical and biotech industries since 2007, specializing in medicinal chemistry and discovery strategy and tactics, and with a particular focus on the development of treatments for neglected tropical diseases. Prior to this, Dr. von Geldern spent over 20 years in the pharmaceutical industry, most recently serving as a Research Fellow and Senior Group Leader at Abbott Laboratories. In this capacity he led medicinal chemistry efforts resulting in the identification of clinical candidates in the areas of oncology, inflammation, cardiovascular and metabolic diseases. He is an author of 85 peer-reviewed articles, an inventor on 70 US patent applications, and has lectured by invitation on ~75 occasions. Dr. von Geldern received S.B. degrees in Chemistry, Mathematics, and Biology from MIT (Undergraduate research with Prof. Rick L. Danheiser), a Ph.D. in Chemistry from the University of California at Berkeley (Prof. Clayton H. Heathcock) and performed post-doctoral research at Stanford University (under Prof. Paul A. Wender).

Responsável: Prof. Luiz Carlos Dias