DGIdb - VANDETANIB Drug Record

VANDETANIB chembl:CHEMBL24828 ApprovedAntineoplastic

Alternate Names:

VANDETANIB
GNF-PF-2188
ZD-64
ZD-6474
ZACTIMA
CAPRELSA
CH 331
N-(4-BROMO-2-FLUOROPHENYL)-6-METHOXY-7-((1-METHYL-4-PIPERIDINYL)METHOXY)-4-QUINAZOLINAMINE
CAPRELSA®
N-(4-BROMO-2-FLUOROPHENYL)-6-METHOXY-7-((1-METHYLPIPERIDIN-4-YL)METHOXY)QUINAZOLIN-4-AMINE
ZD6474
ZD 6474
4-(4-BROMO-2-FLUOROANILINO)-6-METHOXY-7-[(1-METHYLPIPERIDIN-4-YL)METHOXY]QUINAZOLINE
chemidplus:443913-73-3
rxcui:1098413
pubchem.compound:3081361
drugbank:05294
chembl:CHEMBL24828

Drug Info:

FDA Approval	not approved
Drug Class	small molecule
Drug Indications	antineoplastic agent
FDA Approval	Medullary thyroid cancer
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 substrates
Drug Categories	drugs causing inadvertant photosensitivity
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	kinase inhibitor
Drug Categories	narrow therapeutic index drugs
Drug Categories	oct2 inhibitors
Drug Categories	p-glycoprotein inhibitors
Drug Categories	photosensitizing agents
Drug Categories	qtc prolonging agents
Drug Categories	tyrosine kinase inhibitors

(14 More Sources)

Publications:

Frisk et al., 2001, CGH alterations in medullary thyroid carcinomas in relation to the RET M918T mutation and clinical outcome., Int. J. Oncol.
Carlomagno et al., 2009, Identification of tyrosine 806 as a molecular determinant of RET kinase sensitivity to ZD6474., Endocr. Relat. Cancer
Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.
Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.
Gupta-Abramson et al., 2008, Phase II trial of sorafenib in advanced thyroid cancer., J. Clin. Oncol.
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.
Sherman, 2011, Targeted therapies for thyroid tumors., Mod. Pathol.
Drilon et al., 2013, Response to Cabozantinib in patients with RET fusion-positive lung adenocarcinomas., Cancer Discov
Renaud et al., 1975, Effects of 5,6-dihydroxytryptamine on tyrosine-hydroxylase activity in central catecholaminergic neurons of the rat., Biochem. Pharmacol.
Santoro et al., 1998, Molecular biology of the MEN2 gene., J. Intern. Med.
Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol
Couto et al., 2012, AZD1480 blocks growth and tumorigenesis of RET- activated thyroid cancer cell lines., PLoS ONE
Yoh et al., 2017, Vandetanib in patients with previously treated RET-rearranged advanced non-small-cell lung cancer (LURET): an open-label, multicentre phase 2 trial., Lancet Respir Med
Wells et al., 2012, Vandetanib in patients with locally advanced or metastatic medullary thyroid cancer: a randomized, double-blind phase III trial., J. Clin. Oncol.
Wells et al., 2010, Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer., J. Clin. Oncol.
Kato et al., 2017, RET Aberrations in Diverse Cancers: Next-Generation Sequencing of 4,871 Patients., Clin. Cancer Res.
Lee et al., 2017, Vandetanib in pretreated patients with advanced non-small cell lung cancer-harboring RET rearrangement: a phase II clinical trial., Ann. Oncol.
Coxon et al., 2012, Anti-tumor activity of motesanib in a medullary thyroid cancer model., J. Endocrinol. Invest.
Gautschi et al., 2013, A patient with lung adenocarcinoma and RET fusion treated with vandetanib., J Thorac Oncol
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Dabir et al., 2014, RET mutation and expression in small-cell lung cancer., J Thorac Oncol
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Carr et al., 2010, Phase II study of daily sunitinib in FDG-PET-positive, iodine-refractory differentiated thyroid cancer and metastatic medullary carcinoma of the thyroid with functional imaging correlation., Clin. Cancer Res.
Carlomagno et al., 2004, Disease associated mutations at valine 804 in the RET receptor tyrosine kinase confer resistance to selective kinase inhibitors., Oncogene
Vitagliano et al., 2011, The tyrosine kinase inhibitor ZD6474 blocks proliferation of RET mutant medullary thyroid carcinoma cells., Endocr. Relat. Cancer
Gautschi et al., 2017, Targeting RET in Patients With RET-Rearranged Lung Cancers: Results From the Global, Multicenter RET Registry., J. Clin. Oncol.
Egawa et al., 1998, Genotype-phenotype correlation of patients with multiple endocrine neoplasia type 2 in Japan., Jpn. J. Clin. Oncol.
Elisei et al., 2008, Prognostic significance of somatic RET oncogene mutations in sporadic medullary thyroid cancer: a 10-year follow-up study., J. Clin. Endocrinol. Metab.
Verbeek et al., 2011, The effects of four different tyrosine kinase inhibitors on medullary and papillary thyroid cancer cells., J. Clin. Endocrinol. Metab.
Hatem et al., 2016, Vandetanib as a potential new treatment for estrogen receptor-negative breast cancers., Int. J. Cancer
Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics
Herbst RS et al., 2004, Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 2., J Clin Oncol
Bonner JA et al., 2006, Radiotherapy plus cetuximab for squamous-cell carcinoma of the head and neck., N Engl J Med
Normanno N et al., 2006, Epidermal growth factor receptor (EGFR) signaling in cancer., Gene
Giaccone G et al., 2004, Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1., J Clin Oncol
Vermorken JB et al., 2008, Platinum-based chemotherapy plus cetuximab in head and neck cancer., N Engl J Med
Lee et al., 2015, A Multicenter, Phase II, Randomized, Noncomparative Clinical Trial of Radiation and Temozolomide with or without Vandetanib in Newly Diagnosed Glioblastoma Patients., Clin. Cancer Res.
Thatcher N et al., 2005, Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer)., Lancet
Jonker et al., 2007, Cetuximab for the treatment of colorectal cancer., N. Engl. J. Med.
Rossi A et al., 2013, Should epidermal growth factor receptor tyrosine kinase inhibitors be considered ideal drugs for the treatment of selected advanced non-small cell lung cancer patients?, Cancer Treat Rev
Yang et al., 2001, Development of ABX-EGF, a fully human anti-EGF receptor monoclonal antibody, for cancer therapy., Crit. Rev. Oncol. Hematol.
Van Cutsem et al., 2009, Cetuximab and chemotherapy as initial treatment for metastatic colorectal cancer., N. Engl. J. Med.
Giusti RM et al., 2008, U.S. Food and Drug Administration approval: panitumumab for epidermal growth factor receptor-expressing metastatic colorectal carcinoma with progression following fluoropyrimidine-, oxaliplatin-, and irinotecan-containing chemotherapy regimens., Clin Cancer Res
Jorissen RN et al., 2003, Epidermal growth factor receptor: mechanisms of activation and signalling., Exp Cell Res
Mayo C et al., 2012, Pharmacogenetics of EGFR in lung cancer: perspectives and clinical applications., Pharmacogenomics
Nilsson et al., 2016, KDR Amplification Is Associated with VEGF-Induced Activation of the mTOR and Invasion Pathways but does not Predict Clinical Benefit to the VEGFR TKI Vandetanib., Clin. Cancer Res.
Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
Alferez et al., 2010, Effects of vandetanib on adenoma formation in a dextran sodium sulphate enhanced Apc(MIN/+) mouse model., Int. J. Oncol.

VANDETANIB EPHA10

Interaction Score: 1.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHB3

Interaction Score: 1.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Ephrin receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB RET

Interaction Score: 0.7

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

Direct Interaction? True

PMIDs:
11351254 19029224 20368568 19255327 18541894 25366691 8007 21455200 23533264 17 9681850 24433361 23056499 27825616 22025146 20065189 27683183 27803005 21422803 23584301 10592235 25122427 25157968 20847059 15184865 20943719 28447912 9839497 18073307 21470995 26686064 2015

Sources:
ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC OncoKB PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions CGI
VANDETANIB EPHB6

Interaction Score: 0.52

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHA1

Interaction Score: 0.52

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHA4

Interaction Score: 0.52

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHA6

Interaction Score: 0.34

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHA8

Interaction Score: 0.34

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHA7

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHB2

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHB1

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EPHA3

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB PTK6

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase BRK inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DrugBank ChemblInteractions
VANDETANIB EPHA5

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB EGFR

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

combination therapy Vandetanib + Temozolomide

PMIDs:
18681783 14990633 16467544 16377102 14990632 18784101 25910950 16257339 18003960 23022519 11255078 19339720 18316547 12648464 22594511

Sources:
ClearityFoundationBiomarkers ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial PharmGKB JAX-CKB TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions
VANDETANIB APC

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colon cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
20811697

Sources:
JAX-CKB
VANDETANIB TEK

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase TIE-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DrugBank ChemblInteractions
VANDETANIB KDR

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
26578684 20124951

Sources:
ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC PharmGKB JAX-CKB TdgClinicalTrial TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions
VANDETANIB EPHB4

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB FLT1

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC TdgClinicalTrial ChemblInteractions
VANDETANIB FLT4

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Zactima

Novel drug target Established target

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial TdgClinicalTrial TALC ChemblInteractions
VANDETANIB EPHA2

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB TYRO3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ACVR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB LRRK2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB LTK

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ATM

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Vandetanib + Everolimus

Indication/Tumor Type thyroid medullary carcinoma

Response Type predicted – sensitive

PMIDs:
27683183

Sources:
JAX-CKB
VANDETANIB AXL

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ERBB3

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB PTEN

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase II

Response Type no benefit

PMIDs:
25910950

Sources:
ClearityFoundationBiomarkers JAX-CKB
VANDETANIB MAP4K5

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ROCK2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ABL1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Pan-TK inhibitor

Alteration ABL1:V299L

PMIDs:
None found

Sources:
DTC CGI
VANDETANIB BTK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB MAP4K4

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB FYN

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ERBB4

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB MAP2K2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB VEGFA

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
VANDETANIB MAP2K1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB ALK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB AURKB

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB LCK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB PDGFRB

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB FGFR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB SRC

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase SRC inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB MAPK14

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB MTOR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB KRAS

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers
VANDETANIB ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VANDETANIB IDH1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Vandetanib + Temozolomide

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

PMIDs:
25910950

Sources:
JAX-CKB
VANDETANIB HTT

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB YES1

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB GMNN

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB05294
- Version: 5.1.7
Alternate Names:

VANDETANIB DrugBank Drug Name

443913-73-3 CAS Number

Caprelsa Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antineoplastic agents

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
MyCancerGenome: VANDETANIB
- Version: 20-Jun-2017
Alternate Names:

AZD6474 Development Name

VANDETANIB Generic Name

ZACTIMA Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Medullary thyroid cancer

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Publications:

CGI: Vandetanib

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: Vandetanib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Lee et al., 2015, A Multicenter, Phase II, Randomized, Noncomparative Clinical Trial of Radiation and Temozolomide with or without Vandetanib in Newly Diagnosed Glioblastoma Patients., Clin. Cancer Res.

Alferez et al., 2010, Effects of vandetanib on adenoma formation in a dextran sodium sulphate enhanced Apc(MIN/+) mouse model., Int. J. Oncol.

Kato et al., 2017, RET Aberrations in Diverse Cancers: Next-Generation Sequencing of 4,871 Patients., Clin. Cancer Res.

DoCM: VANDETANIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Frisk et al., 2001, CGH alterations in medullary thyroid carcinomas in relation to the RET M918T mutation and clinical outcome., Int. J. Oncol.

Lam et al., 2010, Phase II clinical trial of sorafenib in metastatic medullary thyroid cancer., J. Clin. Oncol.

Kloos et al., 2009, Phase II trial of sorafenib in metastatic thyroid cancer., J. Clin. Oncol.

PharmGKB: vandetanib

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol

Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics

Funke S et al., 2008, Pharmacogenetics in colorectal cancer: a systematic review., Pharmacogenomics

CIViC: VANDETANIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Yoh et al., 2017, Vandetanib in patients with previously treated RET-rearranged advanced non-small-cell lung cancer (LURET): an open-label, multicentre phase 2 trial., Lancet Respir Med

Lee et al., 2017, Vandetanib in pretreated patients with advanced non-small cell lung cancer-harboring RET rearrangement: a phase II clinical trial., Ann. Oncol.

Hatem et al., 2016, Vandetanib as a potential new treatment for estrogen receptor-negative breast cancers., Int. J. Cancer

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

VANDETANIB Primary Drug Name

VANDETANIB Drug Generic Name

CAPRELSA Drug Trade Name

Drug Info:

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

CHEMBL24828 ChEMBL Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178102343
- Version: 29-September-2020
Alternate Names:

VANDETANIB GuideToPharmacology Ligand Name

Drug Info:

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

D0G6QF TTD Drug ID

Drug Info:

Publications:
ChemblInteractions: CHEMBL24828
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL24828
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:

Mechanism of Interaction	Ephrin receptor inhibitor
Direct Interaction	yes

Trial Name	Zactima
Novel drug target	Established target
Direct Interaction?	True

Mechanism of Interaction	Tyrosine-protein kinase BRK inhibitor
Direct Interaction	yes

Indication/Tumor Type	colon cancer
Response Type	sensitive
Approval Status	Preclinical

Mechanism of Interaction	Tyrosine-protein kinase TIE-2 inhibitor
Direct Interaction	yes

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

combination therapy	Vandetanib + Everolimus
Indication/Tumor Type	thyroid medullary carcinoma
Response Type	predicted – sensitive

Mechanism of Interaction	Epidermal growth factor receptor inhibitor
Direct Interaction	yes

Evidence Type	Actionable
Approval Status	Phase II
Response Type	no benefit

Mechanism of Interaction	Tyrosine-protein kinase SRC inhibitor
Direct Interaction	yes

combination therapy	Vandetanib + Temozolomide
Indication/Tumor Type	glioblastoma multiforme
Response Type	sensitive

VANDETANIB	DrugBank Drug Name
443913-73-3	CAS Number
Caprelsa	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	antineoplastic agents

AZD6474	Development Name
VANDETANIB	Generic Name
ZACTIMA	Trade Name

VANDETANIB	Primary Drug Name
VANDETANIB	Drug Generic Name
CAPRELSA	Drug Trade Name

VANDETANIB Drug Record

VANDETANIB chembl:CHEMBL24828 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Ephrin receptor inhibitor

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Zactima Novel drug target Established target Direct Interaction? True

PMIDs: 11351254 19029224 20368568 19255327 18541894 25366691 8007 21455200 23533264 17 9681850 24433361 23056499 27825616 22025146 20065189 27683183 27803005 21422803 23584301 10592235 25122427 25157968 20847059 15184865 20943719 28447912 9839497 18073307 21470995 26686064 2015

Sources: ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC OncoKB PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase BRK inhibitor Direct Interaction yes

PMIDs: None found

Sources: DrugBank ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Zactima Novel drug target Established target combination therapy Vandetanib + Temozolomide

PMIDs: 18681783 14990633 16467544 16377102 14990632 18784101 25910950 16257339 18003960 23022519 11255078 19339720 18316547 12648464 22594511

Sources: ClearityFoundationBiomarkers ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial PharmGKB JAX-CKB TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colon cancer Response Type sensitive Approval Status Preclinical

PMIDs: 20811697

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Tyrosine-protein kinase TIE-2 inhibitor Direct Interaction yes

PMIDs: None found

Sources: DrugBank ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 26578684 20124951

Sources: ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC PharmGKB JAX-CKB TdgClinicalTrial TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Ephrin receptor inhibitor Direct Interaction yes

PMIDs: None found

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Ephrin receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

Direct Interaction? True

PMIDs:
11351254 19029224 20368568 19255327 18541894 25366691 8007 21455200 23533264 17 9681850 24433361 23056499 27825616 22025146 20065189 27683183 27803005 21422803 23584301 10592235 25122427 25157968 20847059 15184865 20943719 28447912 9839497 18073307 21470995 26686064 2015

Sources:
ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC OncoKB PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase BRK inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

combination therapy Vandetanib + Temozolomide

PMIDs:
18681783 14990633 16467544 16377102 14990632 18784101 25910950 16257339 18003960 23022519 11255078 19339720 18316547 12648464 22594511

Sources:
ClearityFoundationBiomarkers ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial PharmGKB JAX-CKB TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colon cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
20811697

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase TIE-2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
26578684 20124951

Sources:
ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC PharmGKB JAX-CKB TdgClinicalTrial TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Ephrin receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zactima

Novel drug target Established target

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial DTC TdgClinicalTrial ChemblInteractions