DGIdb - REGORAFENIB Drug Record

REGORAFENIB chembl:CHEMBL1946170 ApprovedAntineoplastic

Alternate Names:

REGORAFENIB
BAY-734506 MONOHYDRATE
STIVARGA
BAY-73-4506
BAY-734506
RÉGORAFÉNIB
STIVARGA®
REGORAFENIBUM
BAY 73-4506
chemidplus:755037-03-7
drugbank:08896
chembl:CHEMBL1946170
rxcui:1312397
pubchem.compound:11167602

Drug Info:

FDA Approval	not approved
Drug Class	small molecule
Drug Indications	antineoplastic agent
FDA Approval	Colorectal cancer, Gastrointestinal stromal tumors
Drug Class	Kinase Inhibitors
Drug Categories	bradycardia-causing agents
Drug Categories	cytochrome p-450 cyp2b6 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c8 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c9 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	hepatotoxic agents
Drug Categories	kinase inhibitor
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	tyrosine kinase inhibitors
Drug Categories	ugt1a9 inhibitors
Drug Categories	ugt1a9 substrates

(12 More Sources)

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer
Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer
Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.
Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.
Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.
Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus
Kollàr et al., 2014, Regorafenib treatment for advanced, refractory gastrointestinal stromal tumor: a report of the UK managed access program., Clin Sarcoma Res
Tong J et al., 2017 Feb 9, FBW7 mutations mediate resistance of colorectal cancer to targeted therapies by blocking Mcl-1 degradation., Oncogene

REGORAFENIB BRAF

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.

REGORAFENIB RET

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

REGORAFENIB KIT

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type decreased response

Approval Status Preclinical - Cell culture

Approval Status Phase II

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.

Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.

REGORAFENIB KRAS

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family Pan-kinase inhibitor

Alteration KRAS:.

Indication/Tumor Type breast cancer

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus

REGORAFENIB PDGFRA

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Drug family Pan-kinase inhibitor

Publications:

Kollàr et al., 2014, Regorafenib treatment for advanced, refractory gastrointestinal stromal tumor: a report of the UK managed access program., Clin Sarcoma Res
REGORAFENIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name regorafenib, BAY 73-4506

Novel drug target Established target

Endogenous Drug? False

Publications:

Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus
REGORAFENIB RAF1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase RAF inhibitor

Publications:
REGORAFENIB FLT1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Notes

Publications:
REGORAFENIB DDR2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Discoidin domain-containing receptor 2 inhibitor

Direct Interaction yes

Publications:
REGORAFENIB TEK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name regorafenib, BAY 73-4506

Novel drug target Novel Target

Notes

Publications:
REGORAFENIB FLT4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Notes

Publications:
REGORAFENIB PDGFRB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Notes

Publications:
REGORAFENIB ABL1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Publications:
REGORAFENIB FGFR2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
REGORAFENIB FRK

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase FRK inhibitor

Direct Interaction yes

Publications:
REGORAFENIB MAPK11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction MAP kinase p38 beta inhibitor

Direct Interaction yes

Publications:
REGORAFENIB FGFR1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 1 inhibitor

Direct Interaction yes

Publications:
REGORAFENIB NTRK1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
REGORAFENIB EPHA2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
REGORAFENIB ARAF

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
REGORAFENIB FBXW7

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical - Cell culture

Publications:

Tong J et al., 2017 Feb 9, FBW7 mutations mediate resistance of colorectal cancer to targeted therapies by blocking Mcl-1 degradation., Oncogene

REGORAFENIB PIK3CA

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

Publications:

Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.

REGORAFENIB EGFR

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pimasertib + Regorafenib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Publications:

Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

REGORAFENIB APC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Clinical Study

Publications:

Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus

REGORAFENIB NRAS

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

Publications:

Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

Napolitano et al., 2015, Primary and Acquired Resistance of Colorectal Cancer to Anti-EGFR Monoclonal Antibody Can Be Overcome by Combined Treatment of Regorafenib with Cetuximab., Clin. Cancer Res.

REGORAFENIB VHL

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal cell carcinoma

Response Type predicted – sensitive

Approval Status Preclinical - Cell line xenograft

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

REGORAFENIB YES1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
REGORAFENIB VEGFA

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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

REGORAFENIB Generic Name

STIVARGA Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Colorectal cancer, Gastrointestinal stromal tumors

Publications:
DrugBank: DB08896
- Version: 5.1.7
Alternate Names:

REGORAFENIB DrugBank Drug Name

755037-03-7 CAS Number

Stivarga Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antineoplastic agents

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Publications:

JAX-CKB: Regorafenib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.

Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

CIViC: REGORAFENIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.

Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.

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

REGORAFENIB Primary Drug Name

REGORAFENIB Drug Generic Name

STIVARGA Drug Trade Name

Drug Info:

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

CHEMBL1946170 ChEMBL Drug ID

Drug Info:

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

D09GDD TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178102514
- Version: 29-September-2020
Alternate Names:

REGORAFENIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1946170
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
ChemblInteractions: CHEMBL1946170
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
CGI: Regorafenib
- Version: 27-September-2017
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:

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

Notes
Mechanism of Interaction	Tyrosine-protein kinase receptor RET inhibitor
Direct Interaction	yes

Response Type	decreased response
Approval Status	Preclinical - Cell culture
Approval Status	Phase II

Drug family	Pan-kinase inhibitor
Alteration	KRAS:.
Indication/Tumor Type	breast cancer

Direct Interaction	yes
Mechanism of Interaction	Platelet-derived growth factor receptor inhibitor
Drug family	Pan-kinase inhibitor

Trial Name	regorafenib, BAY 73-4506
Novel drug target	Established target
Endogenous Drug?	False

Direct Interaction	yes
Mechanism of Interaction	Serine/threonine-protein kinase RAF inhibitor

Direct Interaction	yes
Mechanism of Interaction	Vascular endothelial growth factor receptor inhibitor
Notes

Mechanism of Interaction	Discoidin domain-containing receptor 2 inhibitor
Direct Interaction	yes

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

Mechanism of Interaction	Fibroblast growth factor receptor 2 inhibitor
Direct Interaction	yes

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

Mechanism of Interaction	MAP kinase p38 beta inhibitor
Direct Interaction	yes

Mechanism of Interaction	Fibroblast growth factor receptor 1 inhibitor
Direct Interaction	yes

Indication/Tumor Type	colorectal cancer
Response Type	resistant
Approval Status	Preclinical - Cell culture

combination therapy	Pimasertib + Regorafenib
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive

Indication/Tumor Type	renal cell carcinoma
Response Type	predicted – sensitive
Approval Status	Preclinical - Cell line xenograft

REGORAFENIB	DrugBank Drug Name
755037-03-7	CAS Number
Stivarga	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	antineoplastic agents

REGORAFENIB	Primary Drug Name
REGORAFENIB	Drug Generic Name
STIVARGA	Drug Trade Name

REGORAFENIB Drug Record

REGORAFENIB chembl:CHEMBL1946170 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor Direct Interaction yes

Publications: Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Response Type decreased response Approval Status Preclinical - Cell culture Approval Status Phase II

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family Pan-kinase inhibitor Alteration KRAS:. Indication/Tumor Type breast cancer

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Platelet-derived growth factor receptor inhibitor Drug family Pan-kinase inhibitor

Publications: Kollàr et al., 2014, Regorafenib treatment for advanced, refractory gastrointestinal stromal tumor: a report of the UK managed access program., Clin Sarcoma Res

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name regorafenib, BAY 73-4506 Novel drug target Established target Endogenous Drug? False

Publications: Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serine/threonine-protein kinase RAF inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor Notes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Discoidin domain-containing receptor 2 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name regorafenib, BAY 73-4506 Novel drug target Novel Target Notes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor Notes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Platelet-derived growth factor receptor inhibitor Direct Interaction yes Notes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction MAP kinase p38 beta inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Fibroblast growth factor receptor 1 inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type resistant Approval Status Preclinical - Cell culture

Publications: Tong J et al., 2017 Feb 9, FBW7 mutations mediate resistance of colorectal cancer to targeted therapies by blocking Mcl-1 degradation., Oncogene

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type resistant Approval Status Preclinical

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Pimasertib + Regorafenib Indication/Tumor Type non-small cell lung carcinoma Response Type sensitive

Publications: Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type sensitive Approval Status Clinical Study

Publications: Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type resistant Approval Status Preclinical

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type renal cell carcinoma Response Type predicted – sensitive Approval Status Preclinical - Cell line xenograft

Publications: Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Tyrosine-protein kinase receptor RET inhibitor

Direct Interaction yes

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type decreased response

Approval Status Preclinical - Cell culture

Approval Status Phase II

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family Pan-kinase inhibitor

Alteration KRAS:.

Indication/Tumor Type breast cancer

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Drug family Pan-kinase inhibitor

Publications:

Kollàr et al., 2014, Regorafenib treatment for advanced, refractory gastrointestinal stromal tumor: a report of the UK managed access program., Clin Sarcoma Res

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name regorafenib, BAY 73-4506

Novel drug target Established target

Endogenous Drug? False

Publications:

Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase RAF inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Discoidin domain-containing receptor 2 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name regorafenib, BAY 73-4506

Novel drug target Novel Target

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase ABL inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 2 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase FRK inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction MAP kinase p38 beta inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Fibroblast growth factor receptor 1 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical - Cell culture

Publications:

Tong J et al., 2017 Feb 9, FBW7 mutations mediate resistance of colorectal cancer to targeted therapies by blocking Mcl-1 degradation., Oncogene

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pimasertib + Regorafenib

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

Publications:

Martinelli et al., 2013, Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells., Int. J. Cancer

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Clinical Study

Publications:

Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type resistant

Approval Status Preclinical

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type renal cell carcinoma

Response Type predicted – sensitive

Approval Status Preclinical - Cell line xenograft

Publications:

Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Alternate Names:

REGORAFENIB Generic Name

STIVARGA Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Colorectal cancer, Gastrointestinal stromal tumors

Alternate Names:

REGORAFENIB DrugBank Drug Name

755037-03-7 CAS Number

Stivarga Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antineoplastic agents

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Alternate Names:

REGORAFENIB Primary Drug Name

REGORAFENIB Drug Generic Name

STIVARGA Drug Trade Name

Alternate Names:

CHEMBL1946170 ChEMBL Drug ID

Alternate Names:

D09GDD TTD Drug ID