- Guide to PHARMACOLOGY
Synonyms: example 74 [US8962630]  | Kisqali® | LEE-011 | LEE011
ribociclib is an approved drug (FDA & EMA (2017))
Compound class: Synthetic organic
Comment: Ribociclib is a selective, orally available inhibitor of the cyclin-dependent kinases CDK4 and CDK6 [1,3].
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|Ribociclib is FDA approved as initial therapy for treatment of postmenopausal women with HR+ve, HER2-ve advanced or metastatic breast cancer, in combination with the aromatase inhibitor letrozole. It was approved under the FDA Breakthrough Therapy designation and Priority Review programs. Phase 3 trial NCT01958021 results are reported in . Early phase trials in other cancers are underway. To view the current list of ribociclib trials link to ClinicalTrials.gov.
In July 2018, the FDA expanded ribociclib's approval to include the treatment of pre/perimenopausal women with HR+ve, HER2-ve advanced/metastatic breast cancer, in combination with an aromatase inhibitor. This expanded approval was based on results from clinical trial NCT02278120 .
|Mechanism Of Action and Pharmacodynamic Effects|
|The cyclin D-CDK4/6 (CDK-4/6:INK4:Rb) pathway is key to regulating cell growth in many types of human cancer [2,7,9], such as genetic subtypes of non-small cell lung cancer (NSCLC, [4,7,11], melanoma, Mantle cell lymphoma (MCL), and ovarian and breast cancers [4-5]. Inhibiting this pathway prevents cell cycle transition from G1 to S phase, induces cell senescence and in some cases results in apoptosis .|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)