DGIdb - RIBOCICLIB Drug Record

RIBOCICLIB chembl:CHEMBL3545110 ApprovedAntineoplastic

Alternate Names:

LEE011
LEE-011A
NVP-LEE011
RIBOCICLIB
LEE-011
pubchem.compound:44631912
rxcui:1873916
chembl:CHEMBL3545110
drugbank:11730
chemidplus:1211441-98-3

Drug Info:

Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
FDA Approval	Breast cancer (HR+, HER2-)
Drug Class	Small molecule inhibitor
Drug Groups	investigational
Drug Categories	antineoplastic agents
Drug Categories	antineoplastic and immunomodulating agents
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strong)
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	highest risk qtc-prolonging agents
Drug Categories	kinase inhibitor
Drug Categories	protein kinase inhibitors
Drug Categories	qtc prolonging agents

(11 More Sources)

Publications:

Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.
Bortolozzi R et al., 2018, Ribociclib, a Cdk4/Cdk6 kinase inhibitor, enhances glucocorticoid sensitivity in B-acute lymphoblastic leukemia (B-All)., Biochem Pharmacol
Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell
Vu et al., 2016, Targeting mutant NRAS signaling pathways in melanoma., Pharmacol. Res.
Lee HJ et al., 2018, A selective cyclin-dependent kinase 4, 6 dual inhibitor, Ribociclib (LEE011) inhibits cell proliferation and induces apoptosis in aggressive thyroid cancer., Cancer Lett
Olanich ME et al., 2015, CDK4 Amplification Reduces Sensitivity to CDK4/6 Inhibition in Fusion-Positive Rhabdomyosarcoma., Clin Cancer Res
Condorelli R et al., 2018, Polyclonal RB1 mutations and acquired resistance to CDK 4/6 inhibitors in patients with metastatic breast cancer., Ann Oncol
Infante et al., 2016, A Phase I Study of the Cyclin-Dependent Kinase 4/6 Inhibitor Ribociclib (LEE011) in Patients with Advanced Solid Tumors and Lymphomas., Clin. Cancer Res.
Pikman et al., 2017, Synergistic Drug Combinations with a CDK4/6 Inhibitor in T-cell Acute Lymphoblastic Leukemia., Clin. Cancer Res.
Dickson, 2014, Molecular pathways: CDK4 inhibitors for cancer therapy., Clin. Cancer Res.
Tripathy et al., 2017, Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors., Clin. Cancer Res.
Xue Y et al., 2019, CDK4/6 inhibitors target SMARCA4-determined cyclin D1 deficiency in hypercalcemic small cell carcinoma of the ovary., Nat Commun

RIBOCICLIB CDK6

Interaction Score: 1.68

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 6 inhibitor

Direct Interaction yes

Drug family CDK4/6 inhibitor

PMIDs:
24045179 29408328

Sources:
TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome ChemblInteractions CGI
RIBOCICLIB CDK4

Interaction Score: 1.29

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name LEE011

Novel drug target Novel Target

Specific Action of the Ligand Inhibition

PMIDs:
24045179 25810375 29408328

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI
RIBOCICLIB CCND2

Interaction Score: 1.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers
RIBOCICLIB CCND3

Interaction Score: 1.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers
RIBOCICLIB SMARCA4

Interaction Score: 1.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30718512

Sources:
CIViC
RIBOCICLIB RB1

Interaction Score: 0.93

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
29236940 27542767 28151717 24795392

Sources:
JAX-CKB CIViC
RIBOCICLIB CCND1

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29306020

Sources:
ClearityFoundationBiomarkers CIViC
RIBOCICLIB NOTCH1

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ribociclib + Everolimus

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB
RIBOCICLIB CDKN2A

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers OncoKB
RIBOCICLIB NRAS

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Binimetinib + Ribociclib

Evidence Type Actionable

Approval Status Phase Ib/II

PMIDs:
26987942

Sources:
OncoKB JAX-CKB CIViC
RIBOCICLIB PGR

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
RIBOCICLIB BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Encorafenib + Ribociclib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
28351928

Sources:
JAX-CKB
RIBOCICLIB ERBB2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
RIBOCICLIB PIK3CA

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25002028

Sources:
CIViC
RIBOCICLIB ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RIBOCICLIB ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB

DrugBank: DB11730
- Version: 5.1.7
Alternate Names:

RIBOCICLIB DrugBank Drug Name

1211441-98-3 CAS Number

Kisqali Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.
MyCancerGenome: RIBOCICLIB
- Version: 20-Jun-2017
Alternate Names:

KISQALI Trade Name

Drug Info:

Drug Class Small molecule inhibitor

FDA Approval Breast cancer (HR+, HER2-)

Publications:
MyCancerGenome: LEE011
- Version: 20-Jun-2017
Alternate Names:

LEE011 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
TdgClinicalTrial: LEE011
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

JAX-CKB: Ribociclib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Infante et al., 2016, A Phase I Study of the Cyclin-Dependent Kinase 4/6 Inhibitor Ribociclib (LEE011) in Patients with Advanced Solid Tumors and Lymphomas., Clin. Cancer Res.

Pikman et al., 2017, Synergistic Drug Combinations with a CDK4/6 Inhibitor in T-cell Acute Lymphoblastic Leukemia., Clin. Cancer Res.

Dickson, 2014, Molecular pathways: CDK4 inhibitors for cancer therapy., Clin. Cancer Res.

CIViC: RIBOCICLIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Lee HJ et al., 2018, A selective cyclin-dependent kinase 4, 6 dual inhibitor, Ribociclib (LEE011) inhibits cell proliferation and induces apoptosis in aggressive thyroid cancer., Cancer Lett

Vu et al., 2016, Targeting mutant NRAS signaling pathways in melanoma., Pharmacol. Res.

Vora et al., 2014, CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors., Cancer Cell

TTD: LEE011
- Version: 2020.06.01
Alternate Names:

D08MXP TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103955
- Version: 29-September-2020
Alternate Names:

RIBOCICLIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3545110
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: LEE011
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
CGI: LEE011
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:
OncoKB: Ribociclib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
PharmGKB: ribociclib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3545110
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
FDA: Ribociclib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Cyclin-dependent kinase 6 inhibitor
Direct Interaction	yes
Drug family	CDK4/6 inhibitor

Trial Name	LEE011
Novel drug target	Novel Target
Specific Action of the Ligand	Inhibition

Indication/Tumor Type	T-cell adult acute lymphocytic leukemia
Response Type	resistant
Approval Status	Preclinical - Cell culture

combination therapy	Ribociclib + Everolimus
Indication/Tumor Type	T-cell adult acute lymphocytic leukemia
Response Type	sensitive

combination therapy	Binimetinib + Ribociclib
Evidence Type	Actionable
Approval Status	Phase Ib/II

combination therapy	Encorafenib + Ribociclib
Indication/Tumor Type	melanoma
Response Type	sensitive

RIBOCICLIB	DrugBank Drug Name
1211441-98-3	CAS Number
Kisqali	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

RIBOCICLIB Drug Record

RIBOCICLIB chembl:CHEMBL3545110 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclin-dependent kinase 6 inhibitor Direct Interaction yes Drug family CDK4/6 inhibitor

PMIDs: 24045179 29408328

Sources: TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome ChemblInteractions CGI

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name LEE011 Novel drug target Novel Target Specific Action of the Ligand Inhibition

PMIDs: 24045179 25810375 29408328

Sources: ClearityFoundationBiomarkers TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationBiomarkers

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationBiomarkers

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30718512

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type T-cell adult acute lymphocytic leukemia Response Type resistant Approval Status Preclinical - Cell culture

PMIDs: 29236940 27542767 28151717 24795392

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29306020

Sources: ClearityFoundationBiomarkers CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Ribociclib + Everolimus Indication/Tumor Type T-cell adult acute lymphocytic leukemia Response Type sensitive

PMIDs: 28151717

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationBiomarkers OncoKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Binimetinib + Ribociclib Evidence Type Actionable Approval Status Phase Ib/II

PMIDs: 26987942

Sources: OncoKB JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Encorafenib + Ribociclib Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 28351928

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25002028

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

DrugBank: DB11730

Alternate Names: RIBOCICLIB DrugBank Drug Name 1211441-98-3 CAS Number Kisqali Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

Publications: Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.

MyCancerGenome: RIBOCICLIB

Alternate Names: KISQALI Trade Name

Drug Info: Drug Class Small molecule inhibitor FDA Approval Breast cancer (HR+, HER2-)

Publications:

MyCancerGenome: LEE011

Alternate Names: LEE011 Development Name

Drug Info: Drug Class Kinase Inhibitors

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclin-dependent kinase 6 inhibitor

Direct Interaction yes

Drug family CDK4/6 inhibitor

PMIDs:
24045179 29408328

Sources:
TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome ChemblInteractions CGI

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name LEE011

Novel drug target Novel Target

Specific Action of the Ligand Inhibition

PMIDs:
24045179 25810375 29408328

Sources:
ClearityFoundationBiomarkers TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers

Interaction Types & Directionality:

n/a

PMIDs:
30718512

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
29236940 27542767 28151717 24795392

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

PMIDs:
29306020

Sources:
ClearityFoundationBiomarkers CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ribociclib + Everolimus

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Binimetinib + Ribociclib

Evidence Type Actionable

Approval Status Phase Ib/II

PMIDs:
26987942

Sources:
OncoKB JAX-CKB CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Encorafenib + Ribociclib

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
28351928

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
25002028

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Alternate Names:

RIBOCICLIB DrugBank Drug Name

1211441-98-3 CAS Number

Kisqali Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Rader et al., 2013, Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma., Clin. Cancer Res.

Alternate Names:

KISQALI Trade Name

Drug Info:

Drug Class Small molecule inhibitor

FDA Approval Breast cancer (HR+, HER2-)

Alternate Names:

LEE011 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

D08MXP TTD Drug ID

Alternate Names:

RIBOCICLIB GuideToPharmacology Ligand Name