Patrick Y. S. Lam talks about Small-Molecule Drug
On October 23, 2023, Prof. Patrick Y. S. Lam from the Baruch S. Blumberg Institute was invited to the 131st Science Lecture in the College of Science. He gave a lecture themed “From World's Best-Selling Small-Molecule Drug (Eliquis) to a Powerful Chinese Name Reaction (Chan-Lam-Coupling)”, which was chaired by Assistant Professor Tiezheng JIA of the Department of Chemistry, SUSTech.
In the lecture, Prof. LAM introduced that thrombosis is one of the most common causes of death in developed countries. There is an urgent need for a new, safer antithrombotic drug to replace Warfarin, which has been used for about 60 years and has other symptoms that will appear during use. 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 an improved safety profile. Utilizing structure-based drug design tools, focused screening, and ADME-T innovations, Prof. LAM 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.
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 synthetic process of Eliquis, Prof. LAM along with Dominic M. T. Chan and David A. Evans, discovered the powerful Chan-Evans-Lam coupling reaction of copper promoted C-X bond cross-coupling via boronic acids and heterocyclic, an effective complementary reaction to Suzuki-Miyaura C-C bond coupling reaction, which won the Nobel Prize in chemistry. Prof. LAM also has made a series of discussions about the mechanism and new discoveries about Chan-Lam coupling in recent years.
During the Q&A interactive session, the on-site teachers and students enthusiastically asked questions about the discovery of Chan-Lam coupling, the mechanism of copper catalysis, and the process of drug development. Prof. LAM provided detailed answers one by one.
In conclusion, Prof. Minghua XU handed an honorary certificate to Prof. LAM.