General
Preferred name
Ribociclib
Synonyms
LEE-011, NVP-LEE011 ()
LEE011 ()
LEE011 succinate ()
RIBOCICLIB SUCCINATE ()
Ribociclib succinate hydrate ()
LEE011 (succinate hydrate) ()
LEE 011 ()
LEE-011 ()
A-1277 ()
N,N-Dimethyl 7-cyclopentyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide ()
Ribociclib hydrochloride ()
LEE-011A ()
LEE011A ()
NVP-LEE011 ()
LEE011 (succinate) ()
LEE011 (hydrochloride) ()
Ribociclib (LEE011) ()
LEE011 hydrochloride ()
LEE011 succinate, Kisqali ()
Kisqali ()
LEE-011-BBA ()
LEE011-BBA ()
Birociclib ()
P&D ID
PD010313
CAS
1211441-98-3
1374639-75-4
1211443-80-9
Tags
available
drug
Approved by
EMA
FDA
First approval
2017
Drug Status
investigational
approved
Drug indication
Breast cancer
Solid tumour/cancer
Hormone receptor positive and HER2-negative advanced or metastatic breast cancer
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA
Inhibition of cyclin-dependent kinase 4 and 6 (CDK4/6) may provide protection against oncogenic processes in specific tissue types. For example, CDK4 is not required for normal mammary tissue development based on knockout mouse studies, but it is needed for growth of Ras-induced mammary tumors, suggesting a potential therapeutic window for treatment with lower toxicity.; Ribociclib was reported to be a most selective CDK4/6 inhibitor and to have dose dependent antitumor activity in a number of preclinical models. It inhibited growth of tumor cells by arresting the cells at the G1 checkpoint, which prevents the tumor cells from proliferating.
ABSORPTION
Ribociclib is orally bioavailable, highly selective inhibitor of CDK4/6 kinases with inhibitory IC50 concentrations in the low nanomolar range. ; Following oral dosing, ribociclib was rapidly absorbed with median Tmax ranging from 1 to 5 hours. Plasma concentrations increased approximately 2- to 3-fold from Cycle 1 Day 1 to Cycle 1 Day 18/21 due to accumulation, with steady state reached by approximately Day 8 on the basis of trough concentrations after repeated daily dosing. Dose-proportionality analyses demonstrated that exposure to ribociclib increased with dose, with both Cmax and area under the curve (AUC) increasing slightly more than proportional to dose, over the dose range 50â1,200 mg/day
DESCRIPTION
Ribociclib is a selective, orally available inhibitor of the cyclin-dependent kinases CDK4 and CDK6 .
(GtoPdb)
DESCRIPTION
Kisqali (ribociclib) is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). These proteins, when over-activated, can enable cancer cells to grow and divide too quickly. Targeting CDK4/6 with enhanced precision may play a role in ensuring that cancer cells do not continue to replicate uncontrollably.
(PKIDB)
DESCRIPTION
High affinity HDAC4 negative allosteric modulator; also binds S100A9; antiangiogenic
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
12
Organisms
0
Compound Sets
30
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
CDK inhibitor database (CDKiDB)
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
Other bioactive compounds
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
48
Molecular Weight
434.25
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
3
cLogP
2.8
TPSA
91.21
Fraction CSP3
0.48
Chiral centers
0.0
Largest ring
6.0
QED
0.64
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
CDK4,CDK6
Pathway
Cell Cycle/Checkpoint
Angiogenesis
Tyrosine Kinase/Adaptors
Cell Cycle/DNA Damage
Target
CDK4
VEGFR4
VEGFR6
CDK6
CDK
CDK4, CDK6
CDK4/6 inhibitor
Primary Target
Cyclin-dependent Kinase
MOA
Inhibitor
CDK inhibitor
CDK4 Inhibitors
CDK6 Inhibitors
Jak3 Inhibitors
Member status
virtual
Indication
breast cancer
Source data
