Ribociclib

Definition

An orally available inhibitor of the cyclin-dependent kinases (CDKs) 4 and 6, with antineoplastic activity. Upon oral administration, ribociclib specifically targets, binds to and inhibits CDK4 and CDK6. This inhibits the cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, which inhibits phosphorylation of the retinoblastoma (Rb) protein. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle dysregulation.

Also known as 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide, LEE 011, LEE-011, LEE011, RIBOCICLIB — per NCIT

Also identified as

• ATC L01EF02 per RXNORM
• NCIT NCIT:C95701 per NCIT
• SCTID 732257004 per RXNORM
• SCTID 763537002 per RXNORM
• UNII TK8ERE8P56 per RXNORM

Indications