Today, Prof. Patrick Y. S. Lam, Adjunct Professor at Drexel University, College of Medicine, coming from Lam Drug Discovery Consulting, LLC, visited our school and gave us a wonderful lecture, named “Discovery of Eliquis®/Apixaban, a novel Factor Xa anticoagulant and Chan-Lam Coupling reaction”.
 
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. Currently the antithrombotic market is the fastest growing one, more than even oncology. 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 innovations, Prof. Patrick Y. S. Lam and his co-workers at Bristol-Myers Squibb had discovered a novel class of potent, selective and orally bioavailable Factor Xa inhibitors culminating in Eliquis®/Apixaban. Eliquis® was recently approved by FDA and named the “Best New Medicine of 2012” by Med Ad News.
 
During the optimization process, Prof. Patrick Y. S. Lam and his co-workers 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 Coupling reaction. In addition, Prof. Patrick Y. S. Lam and his co-workers have pioneered the first rational use of halogen bonding in structure-based drug design.