DGIdb - BINIMETINIB Drug Record

BINIMETINIB chembl:CHEMBL3187723 ApprovedAntineoplastic

Alternate Names:

BINIMETINIB
MEKTOVI
ARRY-438162
ARRY 438162
NVP-MEK162
MEK-162
ARRY-162
MEK162
ARRY 162
chembl:CHEMBL3187723
pubchem.compound:10288191
drugbank:11967
chemidplus:606143-89-9

Drug Info:

Notes	allosteric inhibitor
Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antiinflammatory agent,DMARD,antineoplastic agent

(11 More Sources)

Publications:

Woodfield et al., 2016, Binimetinib inhibits MEK and is effective against neuroblastoma tumor cells with low NF1 expression., BMC Cancer
Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.
Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol
Bendell et al., 2017, A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor., Br. J. Cancer
Ascierto et al., 2013, MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study., Lancet Oncol.
Niessner et al., 2016, PI3K Pathway Inhibition Achieves Potent Antitumor Activity in Melanoma Brain Metastases In Vitro and In Vivo., Clin. Cancer Res.
Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med
Gao Y et al., 2019, V211D Mutation in MEK1 Causes Resistance to MEK Inhibitors in Colon Cancer., Cancer Discov
Koelblinger P et al., 2017, A review of binimetinib for the treatment of mutant cutaneous melanoma., Future Oncol
Raja et al., 2015, Assessment of the In Vivo Activity of PI3K and MEK Inhibitors in Genetically Defined Models of Colorectal Cancer., Mol. Cancer Ther.
Kiessling et al., 2015, Mutant HRAS as novel target for MEK and mTOR inhibitors., Oncotarget
Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.
Dummer et al., 2017, Binimetinib versus dacarbazine in patients with advanced NRAS-mutant melanoma (NEMO): a multicentre, open-label, randomised, phase 3 trial., Lancet Oncol.
Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
Morgan et al., 2001, Cell-cycle-dependent activation of mitogen-activated protein kinase kinase (MEK-1/2) in myeloid leukemia cell lines and induction of growth inhibition and apoptosis by inhibitors of RAS signaling., Blood
Kiessling et al., 2016, Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma., PLoS ONE
Vu et al., 2016, Targeting mutant NRAS signaling pathways in melanoma., Pharmacol. Res.
Thumar et al., 2014, MEK targeting in N-RAS mutated metastatic melanoma., Mol. Cancer
Yan J et al., 2018, Analysis of NRAS gain in 657 patients with melanoma and evaluation of its sensitivity to a MEK inhibitor., Eur J Cancer
Lee et al., 2016, Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models., Oncotarget
Dhawan et al., 2016, Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling., Nature
Hamidi et al., 2014, KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition., Br. J. Cancer
Kim et al., 2016, Phosphoproteomics Reveals MAPK Inhibitors Enhance MET- and EGFR-Driven AKT Signaling in KRAS-Mutant Lung Cancer., Mol. Cancer Res.
Monk BJ et al., 2020, MILO/ENGOT-ov11: Binimetinib Versus Physician's Choice Chemotherapy in Recurrent or Persistent Low-Grade Serous Carcinomas of the Ovary, Fallopian Tube, or Primary Peritoneum., J Clin Oncol
Carita et al., 2016, Dual inhibition of protein kinase C and p53-MDM2 or PKC and mTORC1 are novel efficient therapeutic approaches for uveal melanoma., Oncotarget
Chen et al., 2014, Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutations., Oncogene

BINIMETINIB GNA11

Interaction Score: 1.29

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MEK162 + AEB071

Indication/Tumor Type uveal melanoma

Response Type sensitive

PMIDs:
27507190 24141786

Sources:
JAX-CKB
BINIMETINIB NF1

Interaction Score: 1.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26925841

Sources:
ClearityFoundationBiomarkers CIViC
BINIMETINIB MAP2K7

Interaction Score: 1.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial TTD
BINIMETINIB NRAS

Interaction Score: 1.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BYL719 + MEK162

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

PMIDs:
24569456 28284557 28152546 28514312 11238126 23414587 27307593 26821351 26987942 24588908 29245078

Sources:
JAX-CKB CIViC OncoKB
BINIMETINIB MAP2K5

Interaction Score: 0.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
BINIMETINIB MAP2K4

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
BINIMETINIB MAP2K6

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
BINIMETINIB MAP2K3

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
BINIMETINIB GNAQ

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MEK162 + AEB071

Indication/Tumor Type uveal melanoma

Response Type predicted – sensitive

PMIDs:
27507190

Sources:
JAX-CKB
BINIMETINIB MAP2K2

Interaction Score: 0.52

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name ARRY-162

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

PMIDs:
28587477

Sources:
MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial
BINIMETINIB MAP2K1

Interaction Score: 0.48

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

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

Direct Interaction yes

Trial Name ARRY-162

PMIDs:
31227518

Sources:
MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions CIViC MyCancerGenomeClinicalTrial
BINIMETINIB BRAF

Interaction Score: 0.42

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Encorafenib + Binimetinib

combination therapy Encorafenib + Binimetinib + Cetuximab

Evidence Type Actionable

PMIDs:
26577700 29573941 28152546 23414587 27307593 31566309

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB FDA OncoKB
BINIMETINIB APC

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

Evidence Type Actionable

Approval Status Preclinical

PMIDs:
26206338

Sources:
JAX-CKB
BINIMETINIB HRAS

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type predicted – sensitive

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
26544513

Sources:
JAX-CKB CIViC
BINIMETINIB KRAS

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung adenocarcinoma

Response Type decreased response

Approval Status Preclinical - Cell culture

PMIDs:
27167191 27556948 25167228 28152546 26206338 27422710 32822286

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC OncoKB
BINIMETINIB UGT1A1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
BINIMETINIB ATM

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Clinical Study

PMIDs:
28514312

Sources:
JAX-CKB
BINIMETINIB PTEN

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BYL719 + MEK162

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
26577700 26206338

Sources:
JAX-CKB

MyCancerGenome: MEK162
- Version: 20-Jun-2017
Alternate Names:

MEK162 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Publications:
TdgClinicalTrial: ARRY-162
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antiinflammatory agent,DMARD,antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:
TTD: ARRY-162
- Version: 2020.06.01
Alternate Names:

D0C4LF TTD Drug ID

Drug Info:

Publications:

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

JAX-CKB: Binimetinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Raja et al., 2015, Assessment of the In Vivo Activity of PI3K and MEK Inhibitors in Genetically Defined Models of Colorectal Cancer., Mol. Cancer Ther.

Bendell et al., 2017, A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor., Br. J. Cancer

Hamidi et al., 2014, KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition., Br. J. Cancer

JAX-CKB: MEK162

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Herkert et al., 2016, Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition., Cancer Res.

Gritsman et al., 2014, Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α., J. Clin. Invest.

Carita et al., 2016, Dual inhibition of protein kinase C and p53-MDM2 or PKC and mTORC1 are novel efficient therapeutic approaches for uveal melanoma., Oncotarget

CIViC: BINIMETINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Kopetz S et al., 2019, Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer., N Engl J Med

Dummer R et al., 2018, Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial., Lancet Oncol

Thumar et al., 2014, MEK targeting in N-RAS mutated metastatic melanoma., Mol. Cancer

TALC: MEK162
- Version: 12-May-2016
Alternate Names:

MEK162 Primary Drug Name

MEK162 Drug Synonym

Drug Info:

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

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3187723
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: MEK162
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3187723
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
ClearityFoundationClinicalTrial: MEK162
- Version: 15-June-2013
Alternate Names:

Drug Info:

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

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: MEK162
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:

combination therapy	MEK162 + AEB071
Indication/Tumor Type	uveal melanoma
Response Type	sensitive

combination therapy	BYL719 + MEK162
Indication/Tumor Type	acute myeloid leukemia
Response Type	sensitive

Novel drug target	Novel Target
Trial Name	ARRY-162
Mechanism of Interaction	Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Mechanism of Interaction	Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
Direct Interaction	yes
Trial Name	ARRY-162

combination therapy	Encorafenib + Binimetinib
combination therapy	Encorafenib + Binimetinib + Cetuximab
Evidence Type	Actionable

Response Type	no benefit
Evidence Type	Actionable
Approval Status	Preclinical

Indication/Tumor Type	urinary bladder cancer
Response Type	predicted – sensitive
Indication/Tumor Type	Advanced Solid Tumor

Indication/Tumor Type	lung adenocarcinoma
Response Type	decreased response
Approval Status	Preclinical - Cell culture

Indication/Tumor Type	melanoma
Response Type	sensitive
Approval Status	Clinical Study

allosteric modulator
inhibitor (inhibitory)

allosteric modulator
inhibitor (inhibitory)

BINIMETINIB Drug Record

BINIMETINIB chembl:CHEMBL3187723 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: combination therapy MEK162 + AEB071 Indication/Tumor Type uveal melanoma Response Type sensitive

PMIDs: 27507190 24141786

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26925841

Sources: ClearityFoundationBiomarkers CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BYL719 + MEK162 Indication/Tumor Type acute myeloid leukemia Response Type sensitive

PMIDs: 24569456 28284557 28152546 28514312 11238126 23414587 27307593 26821351 26987942 24588908 29245078

Sources: JAX-CKB CIViC 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: 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: combination therapy MEK162 + AEB071 Indication/Tumor Type uveal melanoma Response Type predicted – sensitive

PMIDs: 27507190

Sources: JAX-CKB

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Novel drug target Novel Target Trial Name ARRY-162 Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

PMIDs: 28587477

Sources: MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 1 inhibitor Direct Interaction yes Trial Name ARRY-162

PMIDs: 31227518

Sources: MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Encorafenib + Binimetinib combination therapy Encorafenib + Binimetinib + Cetuximab Evidence Type Actionable

PMIDs: 26577700 29573941 28152546 23414587 27307593 31566309

Sources: ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info: Response Type no benefit Evidence Type Actionable Approval Status Preclinical

PMIDs: 26206338

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type urinary bladder cancer Response Type predicted – sensitive Indication/Tumor Type Advanced Solid Tumor

PMIDs: 26544513

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type lung adenocarcinoma Response Type decreased response Approval Status Preclinical - Cell culture

PMIDs: 27167191 27556948 25167228 28152546 26206338 27422710 32822286

Sources: ClearityFoundationBiomarkers JAX-CKB CIViC OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

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

PMIDs: 28514312

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BYL719 + MEK162 Indication/Tumor Type melanoma Response Type no benefit

PMIDs: 26577700 26206338

Sources: JAX-CKB

MyCancerGenome: MEK162

Alternate Names: MEK162 Development Name

Drug Info: Drug Class Kinase Inhibitors Notes allosteric inhibitor

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy MEK162 + AEB071

Indication/Tumor Type uveal melanoma

Response Type sensitive

PMIDs:
27507190 24141786

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
26925841

Sources:
ClearityFoundationBiomarkers CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BYL719 + MEK162

Indication/Tumor Type acute myeloid leukemia

Response Type sensitive

PMIDs:
24569456 28284557 28152546 28514312 11238126 23414587 27307593 26821351 26987942 24588908 29245078

Sources:
JAX-CKB CIViC OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial

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:

combination therapy MEK162 + AEB071

Indication/Tumor Type uveal melanoma

Response Type predicted – sensitive

PMIDs:
27507190

Sources:
JAX-CKB

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name ARRY-162

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

PMIDs:
28587477

Sources:
MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

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

Direct Interaction yes

Trial Name ARRY-162

PMIDs:
31227518

Sources:
MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Encorafenib + Binimetinib

combination therapy Encorafenib + Binimetinib + Cetuximab

Evidence Type Actionable

PMIDs:
26577700 29573941 28152546 23414587 27307593 31566309

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB FDA OncoKB

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type no benefit

Evidence Type Actionable

Approval Status Preclinical

PMIDs:
26206338

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type urinary bladder cancer

Response Type predicted – sensitive

Indication/Tumor Type Advanced Solid Tumor

PMIDs:
26544513

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung adenocarcinoma

Response Type decreased response

Approval Status Preclinical - Cell culture

PMIDs:
27167191 27556948 25167228 28152546 26206338 27422710 32822286

Sources:
ClearityFoundationBiomarkers JAX-CKB CIViC OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Clinical Study

PMIDs:
28514312

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BYL719 + MEK162

Indication/Tumor Type melanoma

Response Type no benefit

PMIDs:
26577700 26206338

Sources:
JAX-CKB

Alternate Names:

MEK162 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Drug Info:

Drug Indications antiinflammatory agent,DMARD,antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

D0C4LF TTD Drug ID

Publications:

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

Alternate Names:

MEK162 Primary Drug Name

MEK162 Drug Synonym