Drug Discovery and Development of Galeterone and The Next Generation Galeterone Analogs (NGGAs) for Prostate Cancer Therapy
Tuesday, October 18, 2022
12:00 pm - 1:00 pm
About the Event
In Njar’s effort to discover potent and specific inhibitors of 17α-hydroxylase/17,20-lyase (CYP17), the key enzyme which catalyzes the biosynthesis of androgens from progestins, VN/124-1 (now called GALETERONE) was identified as a selective development candidate which modulates multiple targets in the androgen receptor (AR) signaling pathway. GALETERONE and its analogs were later shown to inhibit Mnk1/2-eIF4E signaling via induction of ubiquitin-proteasome degradation of Mnk1/2 proteins.
About the Speaker
Vincent C.O. Njar, Ph.D., is the Inaugural Distinguished University Professor of Medicinal Chemistry and Pharmacology and head of the Medicinal Chemistry Section of Center for Biomolecular Therapeutics at the University of Maryland School of Medicine. Njar is a leading medicinal chemist and oncopharmacologist who has made significant discoveries in the design, synthesis, discovery and development of novel small molecules with potential for the treatment of a variety of cancers, especially breast, prostate, and pancreatic cancers.
He invented a novel CYP17 inhibitor/AR antagonist/androgen receptor degrader (ARD), VN/124-1 (now named GALETERONE) that was licensed to Tokai Pharmaceuticals, Inc. and advanced to pivotal phase III clinical trials in AR-V7 positive metastatic castration-resistant prostate cancer patients (ARMOR3-SV). Additionally, GALETERONE is in a Phase II clinical trial in patients with metastatic pancreatic cancer. The next generation GALETERONE analogs (NGGAs) that are an order of magnitude more potent than GALETERONE are in development.