DGIdb - IBRUTINIB Drug Record

IBRUTINIB chembl:CHEMBL1873475 ApprovedAntineoplasticImmunotherapy

Alternate Names:

PCI 32765
PCI-32765
CRA-032765
PCI-32765-00
IMBRUVICA
IBRUTINIB
PC-32765
IMBRUVICA®
1-[(3R)-3-[4-AMINO-3-(4-PHENOXYPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-1-YL]PIPERIDIN-1-YL]PROP-2-EN-1-ONE
PCI32765
chembl:CHEMBL1873475
rxcui:1442981
chemidplus:936563-96-1
drugbank:09053
pubchem.compound:24821094

Drug Info:

FDA Approval	not approved
Drug Class	small molecule
Drug Indications	antineoplastic agent
FDA Approval	Mantle cell lymphoma, Chronic lymphocytic leukemia, Waldenstrom's macroglobulinemia
Drug Class	Kinase Inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 substrates
Drug Categories	kinase inhibitor
Drug Categories	narrow therapeutic index drugs
Drug Categories	tyrosine kinase inhibitors

(10 More Sources)

Publications:

Treon et al., 2015, Ibrutinib in previously treated Waldenström's macroglobulinemia., N. Engl. J. Med.
Kwok et al., 2016, ATR inhibition induces synthetic lethality and overcomes chemoresistance in TP53- or ATM-defective chronic lymphocytic leukemia cells., Blood
Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.
Sivina M et al., 2014, The bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) blocks hairy cell leukaemia survival, proliferation and B cell receptor signalling: a new therapeutic approach., Br J Haematol
Sharma et al., 2016, Identification of a structurally novel BTK mutation that drives ibrutinib resistance in CLL., Oncotarget
Maddocks et al., 2015, Etiology of Ibrutinib Therapy Discontinuation and Outcomes in Patients With Chronic Lymphocytic Leukemia., JAMA Oncol
Burger et al., 2016, Clonal evolution in patients with chronic lymphocytic leukaemia developing resistance to BTK inhibition., Nat Commun
Kim et al., 2015, Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia., Drugs
Puig de la Bellacasa R et al., 2014, 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-(8H)-ones as BCR kinase inhibitors for B lymphoid malignancies., Eur J Med Chem
Li X et al., 2014, Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity., J Med Chem
Wang et al., 2016, Bruton's Tyrosine Kinase Inhibitors Prevent Therapeutic Escape in Breast Cancer Cells., Mol. Cancer Ther.
Chong et al., 2017, Mapping genetic vulnerabilities reveals BTK as a novel therapeutic target in oesophageal cancer., Gut

IBRUTINIB PLCG2

Interaction Score: 7.41

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration PLCG2:R665W,L845F

Drug family BTK inhibitor

Clinical Status early trials

PMIDs:
24869598

Sources:
CGI DoCM
IBRUTINIB MYD88

Interaction Score: 1.48

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Pdx

Response Type no benefit

PMIDs:
25853747

Sources:
JAX-CKB CIViC
IBRUTINIB BTK

Interaction Score: 1.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BTK inhibitor

Alteration BTK:C481S

Alteration BTK:C481.

PMIDs:
24869598 24697238 27626698 26182309 27199251 25802231 25222877

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions CGI DoCM COSMIC CIViC GuideToPharmacology PharmGKB TTD
IBRUTINIB BMX

Interaction Score: 0.82

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology TTD
IBRUTINIB TXK

Interaction Score: 0.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB TEC

Interaction Score: 0.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB LYN

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
25222877

Sources:
DTC GuideToPharmacology
IBRUTINIB MYC

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28830912

Sources:
CIViC
IBRUTINIB ITK

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB HCK

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB ATM

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6738 + Ibrutinib

Indication/Tumor Type chronic lymphocytic leukemia

Response Type sensitive

PMIDs:
26563132

Sources:
JAX-CKB
IBRUTINIB ERBB2

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
27256378 28830912

Sources:
JAX-CKB CIViC GuideToPharmacology
IBRUTINIB BLK

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB FYN

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB ERBB4

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB JAK3

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB EGFR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
24915291

Sources:
DTC GuideToPharmacology
IBRUTINIB LCK

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB SRC

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
IBRUTINIB YES1

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DTC GuideToPharmacology
IBRUTINIB TP53

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
26563132

Sources:
JAX-CKB
IBRUTINIB SMAD3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
IBRUTINIB CYP2D6

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

DrugBank: DB09053
- Version: 5.1.7
Alternate Names:

IBRUTINIB DrugBank Drug Name

936563-96-1 CAS Number

Imbruvica Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antineoplastic agents

Publications:

Kim et al., 2015, Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia., Drugs
MyCancerGenome: IBRUTINIB
- Version: 20-Jun-2017
Alternate Names:

PCI-32765 Development Name

IBRUTINIB Generic Name

IMBRUVICA Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Mantle cell lymphoma, Chronic lymphocytic leukemia, Waldenstrom's macroglobulinemia

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Publications:

DTC: IBRUTINIB

Version: 02-September-2020

Alternate Names:

CHEMBL1873475 ChEMBL Drug ID

Drug Info:

Publications:

Li X et al., 2014, Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity., J Med Chem

Puig de la Bellacasa R et al., 2014, 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-(8H)-ones as BCR kinase inhibitors for B lymphoid malignancies., Eur J Med Chem

PharmGKB: ibrutinib

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Sivina M et al., 2014, The bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) blocks hairy cell leukaemia survival, proliferation and B cell receptor signalling: a new therapeutic approach., Br J Haematol

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

JAX-CKB: Ibrutinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Kwok et al., 2016, ATR inhibition induces synthetic lethality and overcomes chemoresistance in TP53- or ATM-defective chronic lymphocytic leukemia cells., Blood

Chong et al., 2017, Mapping genetic vulnerabilities reveals BTK as a novel therapeutic target in oesophageal cancer., Gut

Wang et al., 2016, Bruton's Tyrosine Kinase Inhibitors Prevent Therapeutic Escape in Breast Cancer Cells., Mol. Cancer Ther.

CGI: Ibrutinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

Burger et al., 2016, Clonal evolution in patients with chronic lymphocytic leukaemia developing resistance to BTK inhibition., Nat Commun

DoCM: IBRUTINIB
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

CIViC: IBRUTINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.

Maddocks et al., 2015, Etiology of Ibrutinib Therapy Discontinuation and Outcomes in Patients With Chronic Lymphocytic Leukemia., JAMA Oncol

Sharma et al., 2016, Identification of a structurally novel BTK mutation that drives ibrutinib resistance in CLL., Oncotarget

TTD: Ibrutinib
- Version: 2020.06.01
Alternate Names:

D04SHG TTD Drug ID

D09KTS TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103494
- Version: 29-September-2020
Alternate Names:

IBRUTINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1873475
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1873475
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
COSMIC: Ibrutinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

Alteration	PLCG2:R665W,L845F
Drug family	BTK inhibitor
Clinical Status	early trials

Evidence Type	Actionable
Approval Status	Preclinical - Pdx
Response Type	no benefit

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

combination therapy	AZD6738 + Ibrutinib
Indication/Tumor Type	chronic lymphocytic leukemia
Response Type	sensitive

IBRUTINIB	DrugBank Drug Name
936563-96-1	CAS Number
Imbruvica	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	antineoplastic agents

PCI-32765	Development Name
IBRUTINIB	Generic Name
IMBRUVICA	Trade Name

IBRUTINIB Drug Record

IBRUTINIB chembl:CHEMBL1873475 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Alteration PLCG2:R665W,L845F Drug family BTK inhibitor Clinical Status early trials

PMIDs: 24869598

Sources: CGI DoCM

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Pdx Response Type no benefit

PMIDs: 25853747

Sources: JAX-CKB CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family BTK inhibitor Alteration BTK:C481S Alteration BTK:C481.

PMIDs: 24869598 24697238 27626698 26182309 27199251 25802231 25222877

Sources: DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions CGI DoCM COSMIC CIViC GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 25222877

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28830912

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: combination therapy AZD6738 + Ibrutinib Indication/Tumor Type chronic lymphocytic leukemia Response Type sensitive

PMIDs: 26563132

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 27256378 28830912

Sources: JAX-CKB CIViC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 24915291

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: None found

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration PLCG2:R665W,L845F

Drug family BTK inhibitor

Clinical Status early trials

PMIDs:
24869598

Sources:
CGI DoCM

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Pdx

Response Type no benefit

PMIDs:
25853747

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BTK inhibitor

Alteration BTK:C481S

Alteration BTK:C481.

PMIDs:
24869598 24697238 27626698 26182309 27199251 25802231 25222877

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions CGI DoCM COSMIC CIViC GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
25222877

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
28830912

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6738 + Ibrutinib

Indication/Tumor Type chronic lymphocytic leukemia

Response Type sensitive

PMIDs:
26563132

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
27256378 28830912

Sources:
JAX-CKB CIViC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
24915291

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

n/a