Advancing Macrocycles in Drug Discovery
Flash Talk with Kat Leftheris, Ph.D.
Hosted by Drug Hunter's Director of Industry Research & Relations Dennis Koester, Ph.D.
November 21 2024 at 8 AM PDT / 11 AM EDT / 5 PM CEST
Macrocycles have re-emerged as a promising modality in drug discovery, offering unique advantages in the chemical space between small molecules and biologics. Historically, the development of macrocycles faced obstacles due to a variety of constraints including synthetic complexities and unfavorable pharmacokinetic properties. However, recent approvals and investments in the space show that the industry has re-engaged in the discovery of macrocyclic molecules.
In this Flash Talk, Kat Leftheris will highlight how advances in our understanding of ADME requirements, screening technologies, synthetic chemistry, formulations development and computational modeling helped macrocycles back on the center stage of the industry. Kat will highlight applications for macrocycles in drug discovery and illustrate how the recent developments in technologies have contributed to the discovery of breakthrough compounds such as Merck's PCSK9 inhibitor enlicitide chloride, Chugai's pan-RAS inhibitor LUNA18, and even RevMed’s RAS inhibitor platform.
Dr. Katerina Leftheris has over 25 years of experience in the small molecule/macrocycle drug discovery and early development space.
Most recently, Kat served as CSO at Vilya Inc. Before that, she was SVP of Drug Discovery at Rheos Medicines, focusing on targeting altered cellular metabolism in autoimmune diseases. Prior to Rheos, she was VP of Discovery Chemistry at Pliant Therapeutics, a biotech company developing novel treatments for fibrotic diseases. Earlier in her career, Kat led Discovery Chemistry as the site head for Celgene in San Diego, and she previously held leadership roles at Vitae Pharmaceuticals. She began her career at Bristol-Myers Squibb, where she held positions of increasing responsibility in Discovery Oncology and Immunology Chemistry.
Throughout her career, she and her teams have put 15 compounds into the Clinic spanning many molecular targets including (but not limited to) kinases, GPCRs, NHRs, protease inhibitors, E3 ligase modulators/ligand directed degraders, and integrins. These targets cover debilitating diseases in several therapeutic areas including oncology, I/O, immunology, neuroscience, metabolic diseases and fibrosis. To date, Katerina has over 140 publications and issued patents.
Don't miss this opportunity to learn about more about macrocycles as a modality from an expert in the field. Kat will also be available for a Q&A session. So be sure to bring your questions about drug discovery with macrocycles.