Titre : Discovery of Ertugliflozin: An anti-diabetic agent from the structurally unique dioxa-bicyclo[3.2.1]octane class of SGLT2 inhibitors.
La conférence sera prononcée par le Dr. Vincent Mascitti, chimiste médicinal aux laboratoires Groton de Pfizer Global Research & Development. Elle sera donnée en anglais.
Résumé : Diabetes looms as a threat to human health worldwide. As a result, considerable research efforts are devoted to identify new and efficacious anti-diabetic agents lacking the side effects associated with some of the current drugs (hypoglycemia, weight gain). Inhibition of sodium-dependent glucose cotransporter 2 (SGLT2), a transporter located in the kidney, is a mechanism that promotes glucosuria and therefore, reduction of plasma glucose concentration. Since the mechanism operates in a glucose-dependent and insulin-independent manner, and is associated with weight loss, it has emerged as a very promising approach to the pathophysiologic treatment of type 2 diabetes. In this presentation, we will describe the medicinal and synthetic organic chemistry rationale that led to the rapid identification of Ertugliflozin (PF-04971729), an anti-diabetic agent currently in development and belonging to a new class of SGLT2 inhibitors bearing a dioxa-bicyclo[3.2.1]octane bridged ketal motif.
À propos du conférencier : Vincent Mascitti was born in Reims, France and received his diploma in chemical engineering from the ECPM (Strasbourg, France) in 1999. He completed his Ph.D. in 2003 with Professor Hanessian (University of Montreal, Canada) on the total synthesis of natural products bearing deoxypropionate motifs (e.g., doliculide and borrelidin), and the synthesis of bioactive oligosaccharides. He did his postdoctoral studies in the laboratories of Professor E. J. Corey where he completed the first total synthesis of the ladderane-containing natural product pentacycloanammoxic acid. Vincent joined Pfizer in 2006, where as a medicinal chemist in the CVMED chemistry department, he contributed to various diabetes and obesity related projects. Particularly, Vincent was the driving force behind the design and synthesis of SGLT2 inhibitor PF-04971729, a clinical candidate currently in phase 2 and being evaluated for type 2 diabetes treatment. Vincent is the (co)author of about 30 publications and patent applications. He is currently a Senior Director at Pfizer and Synthesis Head in the CVMED medicinal chemistry department.
