DGIdb - CABOZANTINIB Drug Record

CABOZANTINIB chembl:CHEMBL2105717 ApprovedAntineoplastic

Alternate Names:

CABOMETYX
XL-184 FREE BASE
XL-184
CABOZANTINIB
BMS-907351
COMETRIQ
CABOMETYX®
BMS 907351
XL 184
BMS907351
COMETRIQ®
XL184
pubchem.compound:25102847
chembl:CHEMBL2105717
rxcui:1363268
drugbank:08875
chemidplus:849217-68-1

Drug Info:

FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
FDA Approval	Medullary thyroid cancer, Renal cell carcinoma
Drug Class	Kinase Inhibitors

(12 More Sources)

Publications:

Drilon et al., 2016, Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial., Lancet Oncol.
Sherman et al., 2016, Correlative analyses of RET and RAS mutations in a phase 3 trial of cabozantinib in patients with progressive, metastatic medullary thyroid cancer., Cancer
Kurzrock et al., 2011, Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer., J. Clin. Oncol.
Bentzien et al., 2013, In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer., Thyroid
Gautschi et al., 2017, Targeting RET in Patients With RET-Rearranged Lung Cancers: Results From the Global, Multicenter RET Registry., J. Clin. Oncol.
Renaud et al., 1975, Effects of 5,6-dihydroxytryptamine on tyrosine-hydroxylase activity in central catecholaminergic neurons of the rat., Biochem. Pharmacol.
Wilson et al., 1976, Some properties of the redox components of cytochrome c oxidase and their interactions., Arch. Biochem. Biophys.
Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
Falchook et al., 2016, Effect of the RET Inhibitor Vandetanib in a Patient With RET Fusion-Positive Metastatic Non-Small-Cell Lung Cancer., J. Clin. Oncol.
Gautschi et al., 2013, A patient with lung adenocarcinoma and RET fusion treated with vandetanib., J Thorac Oncol
Drilon et al., 2013, Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas., Cancer Discov
Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.
Chong et al., 2017, Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer., Clin. Cancer Res.
Davare et al., 2015, Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors., Proc. Natl. Acad. Sci. U.S.A.
Katayama et al., 2015, Cabozantinib overcomes crizotinib resistance in ROS1 fusion-positive cancer., Clin. Cancer Res.
Drilon et al., 2016, A Novel Crizotinib-Resistant Solvent-Front Mutation Responsive to Cabozantinib Therapy in a Patient with ROS1-Rearranged Lung Cancer., Clin. Cancer Res.
Zhao et al., 2014, Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants., Cancer Sci.
Gebreyohannes et al., 2016, Cabozantinib Is Active against Human Gastrointestinal Stromal Tumor Xenografts Carrying Different KIT Mutations., Mol. Cancer Ther.
Cohen et al., 2015, Pharmacological Inhibition of KIT Activates MET Signaling in Gastrointestinal Stromal Tumors., Cancer Res.
Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov
Neal et al., 2016, Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial., Lancet Oncol.
Li et al., 2017, Acquired MET Y1248H and D1246N Mutations Mediate Resistance to MET Inhibitors in Non-Small Cell Lung Cancer., Clin. Cancer Res.
Sameni et al., 2016, Cabozantinib (XL184) Inhibits Growth and Invasion of Preclinical TNBC Models., Clin. Cancer Res.
Goyal et al., 2017, A phase 2 and biomarker study of cabozantinib in patients with advanced cholangiocarcinoma., Cancer
Paik et al., 2015, Response to MET inhibitors in patients with stage IV lung adenocarcinomas harboring MET mutations causing exon 14 skipping., Cancer Discov
Nakatani M et al., 2017, The Anti-tumor Effect of Cabozantinib on Ovarian Clear Cell Carcinoma <i>In Vitro</i> and <i>In Vivo</i>., Anticancer Res
Song et al., 2015, Potent antitumor activity of cabozantinib, a c-MET and VEGFR2 inhibitor, in a colorectal cancer patient-derived tumor explant model., Int. J. Cancer
Daud et al., 2017, Phase II randomised discontinuation trial of the MET/VEGF receptor inhibitor cabozantinib in metastatic melanoma., Br. J. Cancer

CABOZANTINIB RET

Interaction Score: 1.23

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
27825636 27525386 21606412 23705946 28447912 17 8007 2015 25366691 23584301 23533264

Sources:
TALC MyCancerGenome JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB FDA OncoKB
CABOZANTINIB ROS1

Interaction Score: 0.96

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Clinical Study

Response Type predicted – sensitive

PMIDs:
27370605 26372962 25351743 26673800

Sources:
JAX-CKB CGI CIViC
CABOZANTINIB GNA11

Interaction Score: 0.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28103611

Sources:
CIViC
CABOZANTINIB MET

Interaction Score: 0.69

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
28396313 27694386 26432786 28192597 25971939 21926191 21606412 29061793

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial TTD OncoKB
CABOZANTINIB CFLAR

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
CABOZANTINIB HGF

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-kinase inhibitor

Alteration HGF:over

PMIDs:
None found

Sources:
CGI
CABOZANTINIB KIT

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
24205792 27777285 25836719

Sources:
MyCancerGenome JAX-CKB
CABOZANTINIB HRAS

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Phase III

PMIDs:
27525386

Sources:
JAX-CKB
CABOZANTINIB KDR

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
21926191 21606412

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial GuideToPharmacology TTD
CABOZANTINIB TEK

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
CABOZANTINIB FLT3

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Approval Status Preclinical

PMIDs:
21926191

Sources:
MyCancerGenome JAX-CKB
CABOZANTINIB EGFR

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type unknown

PMIDs:
27694386 27825638

Sources:
JAX-CKB
CABOZANTINIB KRAS

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Phase III

PMIDs:
27525386

Sources:
JAX-CKB
CABOZANTINIB ABL1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-kinase inhibitor

Alteration ABL1:V299L

PMIDs:
None found

Sources:
CGI
CABOZANTINIB PIK3CA

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25242168

Sources:
CIViC
CABOZANTINIB YES1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

MyCancerGenome: CABOZANTINIB
- Version: 20-Jun-2017
Alternate Names:

CABOZANTINIB Generic Name

COMETRIQ Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Medullary thyroid cancer, Renal cell carcinoma

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

CGI: Cabozantinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Falchook et al., 2016, Effect of the RET Inhibitor Vandetanib in a Patient With RET Fusion-Positive Metastatic Non-Small-Cell Lung Cancer., J. Clin. Oncol.

Wilson et al., 1976, Some properties of the redox components of cytochrome c oxidase and their interactions., Arch. Biochem. Biophys.

Drilon et al., 2013, Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas., Cancer Discov

JAX-CKB: cabozantinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Neal et al., 2016, Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial., Lancet Oncol.

Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.

Sherman et al., 2016, Correlative analyses of RET and RAS mutations in a phase 3 trial of cabozantinib in patients with progressive, metastatic medullary thyroid cancer., Cancer

JAX-CKB: Cabozantinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Bahcall et al., 2016, Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer., Cancer Discov

Neal et al., 2016, Erlotinib, cabozantinib, or erlotinib plus cabozantinib as second-line or third-line treatment of patients with EGFR wild-type advanced non-small-cell lung cancer (ECOG-ACRIN 1512): a randomised, controlled, open-label, multicentre, phase 2 trial., Lancet Oncol.

CIViC: CABOZANTINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Sherman et al., 2016, Correlative analyses of RET and RAS mutations in a phase 3 trial of cabozantinib in patients with progressive, metastatic medullary thyroid cancer., Cancer

Drilon et al., 2016, Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial., Lancet Oncol.

Daud et al., 2017, Phase II randomised discontinuation trial of the MET/VEGF receptor inhibitor cabozantinib in metastatic melanoma., Br. J. Cancer

TALC: CABOZANTINIB
- Version: 12-May-2016
Alternate Names:

CABOZANTINIB Drug Generic Name

CABOZANTINIB Primary Drug Name

COMETRIQ Drug Trade Name

Drug Info:

Publications:
GuideToPharmacology: 178102511
- Version: 29-September-2020
Alternate Names:

CABOZANTINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
DTC: CABOZANTINIB
- Version: 02-September-2020
Alternate Names:

CHEMBL2105717 ChEMBL Drug ID

Drug Info:

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

D0IQ6P TTD Drug ID

Drug Info:

Publications:
ClearityFoundationClinicalTrial: CABOZANTINIB
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2105717
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: CABOZANTINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:

Details of the Assay for Interaction	In a biochemical assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Evidence Type	Actionable
Approval Status	Clinical Study
Response Type	predicted – sensitive

Notes
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Indication/Tumor Type	gastrointestinal stromal tumor
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	thyroid medullary carcinoma
Response Type	sensitive
Approval Status	Phase III

Indication/Tumor Type	Advanced Solid Tumor
Response Type	predicted – sensitive
Approval Status	Preclinical

CABOZANTINIB	Drug Generic Name
CABOZANTINIB	Primary Drug Name
COMETRIQ	Drug Trade Name

antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

Drug family	Pan-kinase inhibitor
Alteration	HGF:over

antagonist (inhibitory)
inhibitor (inhibitory)

CABOZANTINIB Drug Record

CABOZANTINIB chembl:CHEMBL2105717 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

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

Interaction Info: Details of the Assay for Interaction In a biochemical assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 27825636 27525386 21606412 23705946 28447912 17 8007 2015 25366691 23584301 23533264

Sources: TALC MyCancerGenome JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Clinical Study Response Type predicted – sensitive

PMIDs: 27370605 26372962 25351743 26673800

Sources: JAX-CKB CGI CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28103611

Sources: CIViC

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

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

PMIDs: 28396313 27694386 26432786 28192597 25971939 21926191 21606412 29061793

Sources: TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial TTD OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Drug family Pan-kinase inhibitor Alteration HGF:over

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type gastrointestinal stromal tumor Response Type sensitive Approval Status Preclinical

PMIDs: 24205792 27777285 25836719

Sources: MyCancerGenome JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type thyroid medullary carcinoma Response Type sensitive Approval Status Phase III

PMIDs: 27525386

Sources: JAX-CKB

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

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

PMIDs: 21926191 21606412

Sources: TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type predicted – sensitive Approval Status Preclinical

PMIDs: 21926191

Sources: MyCancerGenome JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Phase II Response Type unknown

PMIDs: 27694386 27825638

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type thyroid medullary carcinoma Response Type sensitive Approval Status Phase III

PMIDs: 27525386

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Drug family Pan-kinase inhibitor Alteration ABL1:V299L

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25242168

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

MyCancerGenome: CABOZANTINIB

Alternate Names: CABOZANTINIB Generic Name COMETRIQ Trade Name

Drug Info: Drug Class Kinase Inhibitors FDA Approval Medullary thyroid cancer, Renal cell carcinoma

Publications:

TdgClinicalTrial: CABOZANTINIB

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small molecule FDA Approval not approved

Publications:

CGI: Cabozantinib

Alternate Names:

Drug Info:

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
27825636 27525386 21606412 23705946 28447912 17 8007 2015 25366691 23584301 23533264

Sources:
TALC MyCancerGenome JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial PharmGKB FDA OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Clinical Study

Response Type predicted – sensitive

PMIDs:
27370605 26372962 25351743 26673800

Sources:
JAX-CKB CGI CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28103611

Sources:
CIViC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
28396313 27694386 26432786 28192597 25971939 21926191 21606412 29061793

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB CGI CIViC GuideToPharmacology MyCancerGenomeClinicalTrial TTD OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-kinase inhibitor

Alteration HGF:over

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type gastrointestinal stromal tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
24205792 27777285 25836719

Sources:
MyCancerGenome JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Phase III

PMIDs:
27525386

Sources:
JAX-CKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
21926191 21606412

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type predicted – sensitive

Approval Status Preclinical

PMIDs:
21926191

Sources:
MyCancerGenome JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type unknown

PMIDs:
27694386 27825638

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type thyroid medullary carcinoma

Response Type sensitive

Approval Status Phase III

PMIDs:
27525386

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-kinase inhibitor

Alteration ABL1:V299L

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

n/a

PMIDs:
25242168

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

CABOZANTINIB Generic Name

COMETRIQ Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Medullary thyroid cancer, Renal cell carcinoma

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

CABOZANTINIB Drug Generic Name

CABOZANTINIB Primary Drug Name

COMETRIQ Drug Trade Name

Alternate Names:

CABOZANTINIB GuideToPharmacology Ligand Name

Alternate Names:

CHEMBL2105717 ChEMBL Drug ID

Alternate Names:

D0IQ6P TTD Drug ID