Patrick Y. S. Lam, Ph.D.

Distinguished Professor, Baruch S. Blumberg Institute, PA, USA

Title: Discovery of Eliquis®/Apixaban, a Novel Factor Xa Anticoagulant and Chan-Lam Coupling Reaction

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Biography

Patrick Lam is currently a medicinal chemistry and drug discovery consultant at Lam Drug Discovery Consulting, LLC, Distinguished Professor of Chemistry at Baruch S. Blumberg Institute and Adjunct Professor at Drexel University College of Medicine. He retired from a chemistry director position of Bristol-Myers Squibb Co. Patrick joined DuPont in 1984 and moved to BMS in 2001.  Patrick has >30 years of drug discovery experience.

Patrick is responsible for a total of eight clinical candidates. He was the group leader/co-inventor responsible for the discovery of Eliquis®/Apixaban, a novel Factor Xa anticoagulant drug. Eliquis® is a transformational “mega block-buster” medicine. It is currently the top-selling small-molecule drug in the world, with $14B annual sales. In 2015, the Eliquis discovery team received the American Chemical Society Heroes of Chemistry Award for a successful commercial product that benefits human welfare

Abstract

Thrombosis is the leading cause of death in developed countries. There is a significant need for novel antithrombotics with an improved safety profile to replace Warfarin which has been in use for ~60 years and has significant bleeding issues. Factor Xa is at the junction of the intrinsic and extrinsic pathways of the coagulation cascade. Preclinical data has demonstrated that blocking FXa is an effective approach for anticoagulation with improved safety profile. Utilizing structure-based drug design tools, focused screening, and ADME-T innovations, we at Bristol-Myers Squibb had discovered a novel class of potent, selective and orally bioavailable Factor Xa inhibitors culminating in Eliquis®/Apixaban. Eliquis® is currently the top-selling small-molecule drug in the world, with annual sales of ~US$14B. In 2015, the Eliquis discovery team received the American Chemical Society Heroes of Chemistry Award for a successful commercial product that benefits human well-being.

During the optimization process, we have also discovered the powerful Chan-Lam Coupling reaction of copper promoted C-X bond cross-coupling via boronic acids, a complementary reaction to the Nobel prize Suzuki-Miyaura C-C bond Coupling reaction.