binimetinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5290 606143-89-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • binimetinib
  • mektovi
  • MEK162
  • ARRY-162
  • ARRY-438162
Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. In vitro, binimetinib inhibited extracellular signal-related kinase (ERK) phosphorylation in cellfree assays as well as viability and MEK-dependent phosphorylation of BRAF-mutant human melanoma cell lines. Binimetinib also inhibited in vivo ERK phosphorylation and tumor growth in BRAF-mutant murine xenograft models.
  • Molecular weight: 441.23
  • Formula: C17H15BrF2N4O3
  • CLOGP: 3.16
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 88.41
  • ALOGS: -3.95
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 20, 2018 EMA Pierre Fabre Medicament
June 27, 2018 FDA ARRAY BIOPHARMA INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XE41 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Metastatic malignant melanoma indication 443493003

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.84 acidic
pKa2 4.05 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL 8193229 March 13, 2023 METHOD OF TREATING MELANOMA
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL 8513293 March 13, 2023 INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL 10005761 Aug. 27, 2030 INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL 9850229 Aug. 27, 2030 INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA WITH A BRAF MUTATION
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL 9314464 July 4, 2031 INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA MEDIATED BY A B-RAF PROTEIN KINASE
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL 9598376 Oct. 18, 2033 METHOD OF TREATING MELANOMA
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL 9980944 Oct. 18, 2033 TREATMENT OF MELANOMA WITH A BRAF MUTATION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL June 27, 2023 NEW CHEMICAL ENTITY
15MG MEKTOVI ARRAY BIOPHARMA INC N210498 June 27, 2018 RX TABLET ORAL June 27, 2025 ENCORAFENIB IS INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION, AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Dual specificity mitogen-activated protein kinase kinase 1 Kinase INHIBITOR IC50 7.90 IUPHAR DRUG LABEL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase INHIBITOR IC50 7.90 IUPHAR DRUG LABEL

External reference:

IDSource
181R97MR71 UNII
9764 INN_ID
017616 NDDF
2049122 RXNORM
34461 MMSL
d08818 MMSL
4037645 VANDF
772195005 SNOMEDCT_US
772095008 SNOMEDCT_US
10288191 PUBCHEM_CID
CHEBI:145371 CHEBI
DB11967 DRUGBANK_ID
7921 IUPHAR_LIGAND_ID
D10604 KEGG_DRUG
CHEMBL3187723 ChEMBL_ID
C581313 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
MEKTOVI HUMAN PRESCRIPTION DRUG LABEL 1 70255-010 TABLET, FILM COATED 15 mg ORAL NDA 18 sections