DGIdb - BRIGATINIB Drug Record

BRIGATINIB chembl:CHEMBL3545311 ApprovedAntineoplastic

Alternate Names:

BRIGATINIB
AP-26113
ALUNBRIG

Drug Info:

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational
Drug Categories	antineoplastic agents
Drug Categories	antineoplastic and immunomodulating agents
Drug Categories	bcrp/abcg2 inhibitors
Drug Categories	bcrp/abcg2 substrates
Drug Categories	cytochrome p-450 cyp2c8 substrates
Drug Categories	cytochrome p-450 cyp2c8 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp3a inducers
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inducers
Drug Categories	cytochrome p-450 cyp3a4 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 substrates
Drug Categories	kinase inhibitor
Drug Categories	mate 1 inhibitors
Drug Categories	mate 2 inhibitors
Drug Categories	mate inhibitors
Drug Categories	protein kinase inhibitors
Drug Categories	tyrosine kinase inhibitors

(6 More Sources)

Publications:

Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol
Siaw et al., 2016, Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice., Oncotarget
Kim et al., 2017, Brigatinib in Patients With Crizotinib-Refractory Anaplastic Lymphoma Kinase-Positive Non-Small-Cell Lung Cancer: A Randomized, Multicenter Phase II Trial., J. Clin. Oncol.
Fontana et al., 2015, Activity of second-generation ALK inhibitors against crizotinib-resistant mutants in an NPM-ALK model compared to EML4-ALK., Cancer Med
Yoda S et al., 2018, Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound <i>ALK</i> Mutations in ALK-Positive Lung Cancer., Cancer Discov
Gettinger et al., 2016, Activity and safety of brigatinib in ALK-rearranged non-small-cell lung cancer and other malignancies: a single-arm, open-label, phase 1/2 trial., Lancet Oncol.
Wu et al., 2016, Second- and third-generation ALK inhibitors for non-small cell lung cancer., J Hematol Oncol
Markham A, 2017, Brigatinib: First Global Approval., Drugs
Iragavarapu C et al., 2015, Novel ALK inhibitors in clinical use and development., J Hematol Oncol
Ceccon M et al., 2013, Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors., Mol Cancer Res
Uchibori et al., 2017, Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer., Nat Commun
Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.

BRIGATINIB ALK

Interaction Score: 1.83

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Wild type ALK

Direct Interaction? True

Endogenous Drug? False

PMIDs:
25588040 27049722 28475456 25727400 29650534 27836716 26951079 28597393 25888090 23239810

Sources:
DrugBank ChemblInteractions COSMIC CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB
BRIGATINIB IGF1R

Interaction Score: 0.54

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
28597393 23239810

Sources:
DrugBank GuideToPharmacology
BRIGATINIB ROS1

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26372962

Sources:
CIViC
BRIGATINIB EGFR

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
28287083 28597393 25888090 23239810

Sources:
DrugBank ChemblInteractions CIViC GuideToPharmacology
BRIGATINIB ABL1

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
28597393 23239810

Sources:
DrugBank
BRIGATINIB FLT3

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
28597393 23239810

Sources:
DrugBank
BRIGATINIB INSR

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology
BRIGATINIB ERBB4

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
BRIGATINIB MET

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
BRIGATINIB ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank

DrugBank: DB12267

Version: 5.1.7

Alternate Names:

BRIGATINIB DrugBank Drug Name

1197953-54-0 CAS Number

Alunbrig Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Ceccon M et al., 2013, Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors., Mol Cancer Res

Markham A, 2017, Brigatinib: First Global Approval., Drugs

Iragavarapu C et al., 2015, Novel ALK inhibitors in clinical use and development., J Hematol Oncol

PharmGKB: brigatinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol

CIViC: BRIGATINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Uchibori et al., 2017, Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer., Nat Commun

Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.

Yoda S et al., 2018, Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound <i>ALK</i> Mutations in ALK-Positive Lung Cancer., Cancer Discov

GuideToPharmacology: 223366074
- Version: 29-September-2020
Alternate Names:

BRIGATINIB GuideToPharmacology Ligand Name

Drug Info:

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

D08PIE TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3545311
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3545311
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:

Details of the Assay for Interaction	Wild type ALK
Direct Interaction?	True
Endogenous Drug?	False

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

Mechanism of Interaction	Epidermal growth factor receptor erbB1 inhibitor
Direct Interaction	yes
Specific Action of the Ligand	Inhibition

BRIGATINIB	DrugBank Drug Name
1197953-54-0	CAS Number
Alunbrig	Drug Brand

inhibitor (inhibitory)
binder

BRIGATINIB Drug Record

BRIGATINIB chembl:CHEMBL3545311 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Wild type ALK Direct Interaction? True Endogenous Drug? False

PMIDs: 25588040 27049722 28475456 25727400 29650534 27836716 26951079 28597393 25888090 23239810

Sources: DrugBank ChemblInteractions COSMIC CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 28597393 23239810

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26372962

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

PMIDs: 28287083 28597393 25888090 23239810

Sources: DrugBank ChemblInteractions CIViC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 28597393 23239810

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 28597393 23239810

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory) binder

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

PMIDs: None found

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: DrugBank

DrugBank: DB12267

Alternate Names: BRIGATINIB DrugBank Drug Name 1197953-54-0 CAS Number Alunbrig Drug Brand

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

PharmGKB: brigatinib

Alternate Names:

Drug Info:

Publications: Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol

CIViC: BRIGATINIB

Alternate Names:

Drug Info:

GuideToPharmacology: 223366074

Alternate Names: BRIGATINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Brigatinib

Alternate Names: D08PIE TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL3545311

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL3545311

Alternate Names:

Drug Info:

Publications:

OncoKB: Brigatinib

Alternate Names:

Drug Info:

Publications:

FDA: Brigatinib

Alternate Names:

Drug Info:

Publications:

COSMIC: Brigatinib

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Wild type ALK

Direct Interaction? True

Endogenous Drug? False

PMIDs:
25588040 27049722 28475456 25727400 29650534 27836716 26951079 28597393 25888090 23239810

Sources:
DrugBank ChemblInteractions COSMIC CIViC GuideToPharmacology PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
28597393 23239810

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
26372962

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor erbB1 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
28287083 28597393 25888090 23239810

Sources:
DrugBank ChemblInteractions CIViC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
28597393 23239810

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
28597393 23239810

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

binder

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
DrugBank

Alternate Names:

BRIGATINIB DrugBank Drug Name

1197953-54-0 CAS Number

Alunbrig Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol

Alternate Names:

BRIGATINIB GuideToPharmacology Ligand Name

Alternate Names:

D08PIE TTD Drug ID