ribociclib

Ligand id: 7383

Name: ribociclib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 9
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 91.21
Molecular weight 434.25
XLogP 1.76
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Ribociclib is FDA approved as initial endocrine-based therapy for treatment of postmenopausal women with hormone receptor positive, human epidermal growth factor receptor-2 negative (HR+/HER2-) advanced or metastatic breast cancer, in combination with an aromatase inhibitor (letrozole). It was approved under the FDA Breakthrough Therapy designation and Priority Review programs. Phase 3 trial NCT01958021 results are reported in [6]. Early phase trials in other cancers are underway. To view the current list of ribociclib trials link to ClinicalTrials.gov.
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, [4,7,10], 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 [4].