The road to the discovery of Ribociclib a selective CDK4/6 inhibitor for the treatment of breast cancer<br/>Ying Hou, Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Cambridge, Massachusetts<br/><br/>CDK4/6 is a genetically validated target for the treatment of many types of cancer and has been in the sights of drug-hunters for many years.. Ribociclib (LEE011) is a potent, selective and orally bioavailable CDK4/6 inhibitor which is approved by FDA as a first-line therapy for HER2- / ER+ advanced breast cancers. It was discovered by optimization of a non-selective compound from another kinase program in Novartis. The multi-faceted drug discovery approach, utilization of cross-project data analysis, and strong structure-based design were key contributors leading to the discovery of this molecule. The presentation herein describes the backstories of the early lead identification, the medicinal chemistry efforts that ultimately led to LEE011, as well as other selective CDK4/6 inhibitors.

Road to the discovery of ribociclib a selective CDK4/6 inhibitor for the treatment of breast cancer

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.