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	protein kinase inhibitors
Drug Categories	myelosuppressive agents
Drug Categories	immunosuppressive agents
Drug Categories	heterocyclic compounds, 1-ring
Drug Categories	heterocyclic compounds
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 cyp2d6 substrates
Drug Categories	azoles
Drug Categories	antineoplastic and immunomodulating agents
Drug Categories	antineoplastic agents
Drug Groups	approved
Drug Type	small molecule
Drug Categories	tyrosine kinase inhibitors
Drug Categories	narrow therapeutic index drugs
Drug Categories	kinase inhibitor
Drug Categories	cytochrome p-450 substrates
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp3a substrates

(9 More Sources)

Publications:

Treon et al., 2015, Ibrutinib in previously treated Waldenström's macroglobulinemia., N. Engl. J. Med.
Grommes C et al., 2017, Ibrutinib Unmasks Critical Role of Bruton Tyrosine Kinase in Primary CNS Lymphoma., Cancer Discov
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
Agarwal R et al., 2019, Dynamic molecular monitoring reveals that SWI-SNF mutations mediate resistance to ibrutinib plus venetoclax in mantle cell lymphoma., Nat Med
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
Robichaux JP et al., 2019, Pan-Cancer Landscape and Analysis of ERBB2 Mutations Identifies Poziotinib as a Clinically Active Inhibitor and Enhancer of T-DM1 Activity., Cancer Cell
Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature
Xargay-Torrent S et al., 2015, The splicing modulator sudemycin induces a specific antitumor response and cooperates with ibrutinib in chronic lymphocytic leukemia., Oncotarget
Dwivedi P et al., 2019, Time resolved quantitative phospho-tyrosine analysis reveals Bruton's Tyrosine kinase mediated signaling downstream of the mutated granulocyte-colony stimulating factor receptors., Leukemia
Brach D et al., 2017, EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL., Mol Cancer Ther

IBRUTINIB BTK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BTK inhibitor

Alteration BTK:C481S

Alteration BTK:C481.

Publications:

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

IBRUTINIB LYN

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

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
IBRUTINIB EGFR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

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

IBRUTINIB ERBB2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

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

Robichaux JP et al., 2019, Pan-Cancer Landscape and Analysis of ERBB2 Mutations Identifies Poziotinib as a Clinically Active Inhibitor and Enhancer of T-DM1 Activity., Cancer Cell

IBRUTINIB YES1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB SRC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
IBRUTINIB ERBB4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
IBRUTINIB BLK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB TEC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB JAK3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB BMX

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB TXK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB HCK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB FYN

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB ITK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
IBRUTINIB LCK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

IBRUTINIB MYD88

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Pdx

Response Type no benefit

Publications:

Treon et al., 2015, Ibrutinib in previously treated Waldenström's macroglobulinemia., N. Engl. J. Med.

Grommes C et al., 2017, Ibrutinib Unmasks Critical Role of Bruton Tyrosine Kinase in Primary CNS Lymphoma., Cancer Discov

IBRUTINIB TP53

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

Publications:

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

IBRUTINIB ATM

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6738 + Ibrutinib

Indication/Tumor Type chronic lymphocytic leukemia

Response Type sensitive

Publications:

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

Agarwal R et al., 2019, Dynamic molecular monitoring reveals that SWI-SNF mutations mediate resistance to ibrutinib plus venetoclax in mantle cell lymphoma., Nat Med

IBRUTINIB PLCG2

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration PLCG2:R665W,L845F

Drug family BTK inhibitor

Clinical Status early trials

Publications:

Woyach et al., 2014, Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib., N. Engl. J. Med.
IBRUTINIB DNMT3A

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature
IBRUTINIB SF3B1

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Xargay-Torrent S et al., 2015, The splicing modulator sudemycin induces a specific antitumor response and cooperates with ibrutinib in chronic lymphocytic leukemia., Oncotarget
IBRUTINIB FLT3

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature

IBRUTINIB CSF3R

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ibrutinib + Ruxolitinib

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Publications:

Dwivedi P et al., 2019, Time resolved quantitative phospho-tyrosine analysis reveals Bruton's Tyrosine kinase mediated signaling downstream of the mutated granulocyte-colony stimulating factor receptors., Leukemia

IBRUTINIB NPM1

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature
IBRUTINIB NOTCH1

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type predicted - resistant

Publications:

Agarwal R et al., 2019, Dynamic molecular monitoring reveals that SWI-SNF mutations mediate resistance to ibrutinib plus venetoclax in mantle cell lymphoma., Nat Med
IBRUTINIB EZH2

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

Publications:

Brach D et al., 2017, EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL., Mol Cancer Ther
IBRUTINIB CYP2D6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
IBRUTINIB SMAD3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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.

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.

CGI: 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.

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

JAX-CKB: Ibrutinib

Version: 15-September-2020

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

Agarwal R et al., 2019, Dynamic molecular monitoring reveals that SWI-SNF mutations mediate resistance to ibrutinib plus venetoclax in mantle cell lymphoma., Nat Med

Dwivedi P et al., 2019, Time resolved quantitative phospho-tyrosine analysis reveals Bruton's Tyrosine kinase mediated signaling downstream of the mutated granulocyte-colony stimulating factor receptors., Leukemia

GuideToPharmacologyInteractions: 178103494
- Version: 20-July-2020
Alternate Names:

IBRUTINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Ibrutinib
- Version: 2020.06.01
Alternate Names:

D04SHG TTD Drug ID

D09KTS TTD Drug ID

Drug Info:

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

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:

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

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

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

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

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

combination therapy	Ibrutinib + Ruxolitinib
Evidence Type	Actionable
Approval Status	Preclinical - Cell culture

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

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: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: 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

Interaction Types & Directionality: inhibitor (inhibitory)

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: n/a

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

Publications: Treon et al., 2015, Ibrutinib in previously treated Waldenström's macroglobulinemia., N. Engl. J. Med. Grommes C et al., 2017, Ibrutinib Unmasks Critical Role of Bruton Tyrosine Kinase in Primary CNS Lymphoma., Cancer Discov

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical Response Type sensitive

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

Interaction Types & Directionality: n/a

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

Interaction Types & Directionality: n/a

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

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

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Patient cell culture Response Type predicted - sensitive

Publications: Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Patient cell culture Response Type predicted - sensitive

Publications: Xargay-Torrent S et al., 2015, The splicing modulator sudemycin induces a specific antitumor response and cooperates with ibrutinib in chronic lymphocytic leukemia., Oncotarget

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Patient cell culture Response Type predicted - sensitive

Publications: Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Ibrutinib + Ruxolitinib Evidence Type Actionable Approval Status Preclinical - Cell culture

Publications: Dwivedi P et al., 2019, Time resolved quantitative phospho-tyrosine analysis reveals Bruton's Tyrosine kinase mediated signaling downstream of the mutated granulocyte-colony stimulating factor receptors., Leukemia

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Patient cell culture Response Type predicted - sensitive

Publications: Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Phase II Response Type predicted - resistant

Publications: Agarwal R et al., 2019, Dynamic molecular monitoring reveals that SWI-SNF mutations mediate resistance to ibrutinib plus venetoclax in mantle cell lymphoma., Nat Med

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BTK inhibitor

Alteration BTK:C481S

Alteration BTK:C481.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Pdx

Response Type no benefit

Publications:

Treon et al., 2015, Ibrutinib in previously treated Waldenström's macroglobulinemia., N. Engl. J. Med.

Grommes C et al., 2017, Ibrutinib Unmasks Critical Role of Bruton Tyrosine Kinase in Primary CNS Lymphoma., Cancer Discov

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

Publications:

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

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6738 + Ibrutinib

Indication/Tumor Type chronic lymphocytic leukemia

Response Type sensitive

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration PLCG2:R665W,L845F

Drug family BTK inhibitor

Clinical Status early trials

Publications:

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

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Xargay-Torrent S et al., 2015, The splicing modulator sudemycin induces a specific antitumor response and cooperates with ibrutinib in chronic lymphocytic leukemia., Oncotarget

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ibrutinib + Ruxolitinib

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Publications:

Dwivedi P et al., 2019, Time resolved quantitative phospho-tyrosine analysis reveals Bruton's Tyrosine kinase mediated signaling downstream of the mutated granulocyte-colony stimulating factor receptors., Leukemia

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Patient cell culture

Response Type predicted - sensitive

Publications:

Tyner JW et al., 2018, Functional genomic landscape of acute myeloid leukaemia., Nature

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type predicted - resistant

Publications:

Agarwal R et al., 2019, Dynamic molecular monitoring reveals that SWI-SNF mutations mediate resistance to ibrutinib plus venetoclax in mantle cell lymphoma., Nat Med

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

Publications:

Brach D et al., 2017, EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL., Mol Cancer Ther

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

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

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Alternate Names:

CHEMBL1873475 ChEMBL Drug ID

Publications:

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

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