DGIdb - COBIMETINIB Drug Record

COBIMETINIB chembl:CHEMBL2146883 ApprovedAntineoplastic

Alternate Names:

RG-7420
GDC-0973
COTELLIC
COBIMETINIB
XL-518
RG-7421
XL 518
GDC0973
XL518
RG7420
GDC 0973
RG 7420
pubchem.compound:16222096
chemidplus:934660-93-2
rxcui:1722365
chembl:CHEMBL2146883
drugbank:05239

Drug Info:

FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent
FDA Approval	Melanoma (with BRAF V600E or V600K mutation)
Drug Class	Kinase Inhibitor
Pharmaceutical Developer	Exelixis
Source Reported Drug Name(s)	GDC-0973/XL518
Drug Class	MEK Inhibitor
Notes	allosteric inhibitor
Drug Class	Kinase Inhibitors

(15 More Sources)

Publications:

Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature
Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.
Diamond et al., 2016, Diverse and Targetable Kinase Alterations Drive Histiocytic Neoplasms., Cancer Discov
Singh et al., 2015, Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cells., J. Exp. Clin. Cancer Res.
Ribas A et al., 2014, Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study., Lancet Oncol
Ascierto PA et al., 2016, Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial., Lancet Oncol
Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.
Kirouac et al., 2017, Clinical responses to ERK inhibition in BRAF(V600E)-mutant colorectal cancer predicted using a computational model., NPJ Syst Biol Appl
McEvoy CR et al., 2019, Profound MEK inhibitor response in a cutaneous melanoma harboring a GOLGA4-RAF1 fusion., J Clin Invest

COBIMETINIB MAP2K7

Interaction Score: 2.28

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Negative

PMIDs:
None found

Sources:
MyCancerGenome GuideToPharmacology MyCancerGenomeClinicalTrial
COBIMETINIB MAP2K1

Interaction Score: 1.09

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor

Novel drug target Novel Target

PMIDs:
26566875 26384788

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial OncoKB
COBIMETINIB MAP2K5

Interaction Score: 0.91

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
COBIMETINIB MAP2K3

Interaction Score: 0.76

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
COBIMETINIB MAP2K2

Interaction Score: 0.67

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Direct Interaction yes

Direct Interaction? True

PMIDs:
None found

Sources:
MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial OncoKB
COBIMETINIB MAP2K4

Interaction Score: 0.65

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
COBIMETINIB MAP2K6

Interaction Score: 0.65

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
COBIMETINIB BRAF

Interaction Score: 0.6

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status FDA approved

Approval Status Phase Ib/II

combination therapy Atezolizumab + Vemurafenib + Cobimetinib

PMIDs:
25037139 27480103 25265494 23934108 22084396 28649441

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB FDA OncoKB
COBIMETINIB RAF1

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30835257

Sources:
CIViC OncoKB
COBIMETINIB ARAF

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
OncoKB
COBIMETINIB NF1

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers OncoKB
COBIMETINIB KRAS

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Atezolizumab + Cobimetinib

Indication/Tumor Type colorectal cancer

Response Type predicted – sensitive

PMIDs:
23934108 22084396

Sources:
ClearityFoundationBiomarkers JAX-CKB OncoKB
COBIMETINIB NRAS

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
OncoKB
COBIMETINIB PIK3CA

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0941 + cobimetinib

Indication/Tumor Type colorectal adenocarcinoma

Response Type sensitive

PMIDs:
22084396

Sources:
JAX-CKB

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

COTELLIC Trade Name

Drug Info:

Drug Class Kinase Inhibitor

FDA Approval Melanoma (with BRAF V600E or V600K mutation)

Publications:
CancerCommons: GDC-0973
- Version: 25-July-2013
Alternate Names:

16222096 PubChem Drug ID

GDC-0973 Drug Development Name

GDC-0973 PubChem Drug Name

Drug Info:

Drug Class MEK Inhibitor

Source Reported Drug Name(s) GDC-0973/XL518

Pharmaceutical Developer Exelixis

Publications:
MyCancerGenome: GDC-0973
- Version: 20-Jun-2017
Alternate Names:

GDC-0973 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Publications:
TdgClinicalTrial: GDC-0973
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:
TTD: RG7420
- Version: 2020.06.01
Alternate Names:

D0O2FN TTD Drug ID

Drug Info:

Publications:

Akinleye A et al., 2013, MEK and the inhibitors: from bench to bedside., J Hematol Oncol

JAX-CKB: Cobimetinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Hatzivassiliou et al., 2013, Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers., Nature

Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.

Larkin et al., 2014, Combined vemurafenib and cobimetinib in BRAF-mutated melanoma., N. Engl. J. Med.

JAX-CKB: cobimetinib
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.

CIViC: COBIMETINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

McEvoy CR et al., 2019, Profound MEK inhibitor response in a cutaneous melanoma harboring a GOLGA4-RAF1 fusion., J Clin Invest

Ribas A et al., 2014, Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study., Lancet Oncol

Ascierto PA et al., 2016, Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial., Lancet Oncol

TALC: GDC-0973
- Version: 12-May-2016
Alternate Names:

GDC-0973 Drug Synonym

GDC-0973 Primary Drug Name

XL518 Drug Synonym

Drug Info:

Publications:
GuideToPharmacology: 223365961
- Version: 29-September-2020
Alternate Names:

COBIMETINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2146883
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2146883
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:
ClearityFoundationBiomarkers: GDC-0973
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: XL518
- Version: 15-June-2013
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: GDC-0973
- Version: 30-February-2014
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

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

Direct Interaction	yes
Mechanism of Interaction	Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
Novel drug target	Novel Target

Approval Status	FDA approved
Approval Status	Phase Ib/II
combination therapy	Atezolizumab + Vemurafenib + Cobimetinib

combination therapy	Atezolizumab + Cobimetinib
Indication/Tumor Type	colorectal cancer
Response Type	predicted – sensitive

combination therapy	GDC-0941 + cobimetinib
Indication/Tumor Type	colorectal adenocarcinoma
Response Type	sensitive

16222096	PubChem Drug ID
GDC-0973	Drug Development Name
GDC-0973	PubChem Drug Name

GDC-0973	Drug Synonym
GDC-0973	Primary Drug Name
XL518	Drug Synonym

allosteric modulator
inhibitor (inhibitory)

allosteric modulator
inhibitor (inhibitory)

allosteric modulator
inhibitor (inhibitory)

COBIMETINIB Drug Record

COBIMETINIB chembl:CHEMBL2146883 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

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

PMIDs: None found

Sources: MyCancerGenome GuideToPharmacology MyCancerGenomeClinicalTrial

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor Novel drug target Novel Target

PMIDs: 26566875 26384788

Sources: TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor Direct Interaction yes Direct Interaction? True

PMIDs: None found

Sources: MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Approval Status FDA approved Approval Status Phase Ib/II combination therapy Atezolizumab + Vemurafenib + Cobimetinib

PMIDs: 25037139 27480103 25265494 23934108 22084396 28649441

Sources: ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30835257

Sources: CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationBiomarkers OncoKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Atezolizumab + Cobimetinib Indication/Tumor Type colorectal cancer Response Type predicted – sensitive

PMIDs: 23934108 22084396

Sources: ClearityFoundationBiomarkers JAX-CKB OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: OncoKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy GDC-0941 + cobimetinib Indication/Tumor Type colorectal adenocarcinoma Response Type sensitive

PMIDs: 22084396

Sources: JAX-CKB

MyCancerGenome: COBIMETINIB

Alternate Names: COTELLIC Trade Name

Drug Info: Drug Class Kinase Inhibitor FDA Approval Melanoma (with BRAF V600E or V600K mutation)

Publications:

CancerCommons: GDC-0973

Alternate Names: 16222096 PubChem Drug ID GDC-0973 Drug Development Name GDC-0973 PubChem Drug Name

Drug Info: Drug Class MEK Inhibitor Source Reported Drug Name(s) GDC-0973/XL518 Pharmaceutical Developer Exelixis

Publications:

MyCancerGenome: GDC-0973

Alternate Names: GDC-0973 Development Name

Drug Info: Drug Class Kinase Inhibitors Notes allosteric inhibitor

Publications:

TdgClinicalTrial: GDC-0973

Alternate Names:

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

Publications:

TTD: RG7420

Alternate Names: D0O2FN TTD Drug ID

Drug Info:

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Negative

PMIDs:
None found

Sources:
MyCancerGenome GuideToPharmacology MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor

Novel drug target Novel Target

PMIDs:
26566875 26384788

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions GuideToPharmacology CancerCommons MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Direct Interaction yes

Direct Interaction? True

PMIDs:
None found

Sources:
MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status FDA approved

Approval Status Phase Ib/II

combination therapy Atezolizumab + Vemurafenib + Cobimetinib

PMIDs:
25037139 27480103 25265494 23934108 22084396 28649441

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
30835257

Sources:
CIViC OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Atezolizumab + Cobimetinib

Indication/Tumor Type colorectal cancer

Response Type predicted – sensitive

PMIDs:
23934108 22084396

Sources:
ClearityFoundationBiomarkers JAX-CKB OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0941 + cobimetinib

Indication/Tumor Type colorectal adenocarcinoma

Response Type sensitive

PMIDs:
22084396

Sources:
JAX-CKB

Alternate Names:

COTELLIC Trade Name

Drug Info:

Drug Class Kinase Inhibitor

FDA Approval Melanoma (with BRAF V600E or V600K mutation)

Alternate Names:

16222096 PubChem Drug ID

GDC-0973 Drug Development Name

GDC-0973 PubChem Drug Name

Drug Info:

Drug Class MEK Inhibitor

Source Reported Drug Name(s) GDC-0973/XL518

Pharmaceutical Developer Exelixis

Alternate Names:

GDC-0973 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

D0O2FN TTD Drug ID

Publications:

Akinleye A et al., 2013, MEK and the inhibitors: from bench to bedside., J Hematol Oncol

Publications:

Hoeflich et al., 2012, Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition., Cancer Res.

Alternate Names:

GDC-0973 Drug Synonym

GDC-0973 Primary Drug Name

XL518 Drug Synonym

Alternate Names:

COBIMETINIB GuideToPharmacology Ligand Name