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Mektovi(binimetinib)
Mektovi (binimetinib) is a small molecule pharmaceutical. Binimetinib was first approved as Mektovi on 2018-06-27. It is used to treat melanoma in the USA. It has been approved in Europe to treat melanoma. The pharmaceutical is active against dual specificity mitogen-activated protein kinase kinase 2 and dual specificity mitogen-activated protein kinase kinase 1. In addition, it is known to target serine/threonine-protein kinase B-raf.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
neoplasmsD009369
Trade Name
FDA
EMA
Mektovi
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Binimetinib
Tradename
Company
Number
Date
Products
MEKTOVIArray BiopharmaN-210498 RX2018-06-27
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
mektoviNew Drug Application2020-10-01
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
melanomaD008545
Agency Specific
FDA
EMA
Expiration
Code
BINIMETINIB, MEKTOVI, ARRAY BIOPHARMA INC
2025-06-27ODE-194
2023-06-27NCE
Patent Expiration
Patent
Expires
Flag
FDA Information
Binimetinib, Mektovi, Array Biopharma Inc
95620162033-10-18DS, DP
95983762033-10-18U-2330
99809442033-10-18U-2334
93144642031-07-04U-2332
98502292030-08-27U-2333
100057612030-08-27U-2331
77770502023-03-13DS, DP
81786932023-03-13DS, DP
81932292023-03-13U-2330
85132932023-03-13U-2331
ATC Codes
L: Antineoplastic and immunomodulating agents
L01: Antineoplastic agents
L01E: Protein kinase inhibitors, antineoplastic and immunomodulating agents
L01EE: Mitogen-activated protein kinase (mek) inhibitors
L01EE03: Binimetinib
HCPCS
No data
Clinical
Clinical Trials
126 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369C8017131126
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
MelanomaD00854514213336
Colorectal neoplasmsD015179108217
Biliary tract neoplasmsD001661C24.94316
Fallopian tube neoplasmsD005185112
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Non-small-cell lung carcinomaD00228911815
Pancreatic neoplasmsD010190EFO_0003860C25457
Lung neoplasmsD008175C34.90637
Brain neoplasmsD001932EFO_0003833C71245
Breast neoplasmsD001943EFO_0003869C50144
Triple negative breast neoplasmsD064726334
Colonic neoplasmsD003110C18224
Multiple myelomaD009101C90.033
Thyroid neoplasmsD013964EFO_0003841123
Rectal neoplasmsD012004213
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Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Hepatic insufficiencyD04855022
Renal cell carcinomaD00229211
AdenocarcinomaD00023011
Gene rearrangementD01532111
Small cell carcinomaD01828811
Myeloid leukemia acuteD015470C92.011
Monocytic leukemia acuteD00794811
Myelomonocytic leukemia acuteD015479C92.511
Myeloid leukemiaD007951C9211
Erythroblastic leukemia acuteD004915EFO_1001257C94.011
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Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameBINIMETINIB
INNbinimetinib
Description
Binimetinib is a member of the class of benzimidazoles that is 1-methyl-1H-benzimidazole which is substituted at positions 4, 5, and 6 by fluorine, (4-bromo-2-fluorophenyl)nitrilo, and N-(2-hydroxyethoxy)aminocarbonyl groups, respectively. It is a MEK1 and MEK2 inhibitor (IC50= 12 nM). Approved by the FDA for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation in combination with encorafenib. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of benzimidazoles, a member of bromobenzenes, a member of monofluorobenzenes, a hydroxamic acid ester and a secondary amino compound.
Classification
Small molecule
Drug classtyrosine kinase inhibitors: tyrosine kinase inhibitors; MEK (MAPK kinase) inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
Cn1cnc2c(F)c(Nc3ccc(Br)cc3F)c(C(=O)NOCCO)cc21
Identifiers
PDB7M0U
CAS-ID606143-89-9
RxCUI2049122
ChEMBL IDCHEMBL3187723
ChEBI ID
PubChem CID10288191
DrugBankDB11967
UNII ID181R97MR71 (ChemIDplus, GSRS)
Target
Agency Approved
MAP2K2
MAP2K2
MAP2K1
MAP2K1
Organism
Homo sapiens
Gene name
MAP2K2
Gene synonyms
MEK2, MKK2, PRKMK2
NCBI Gene ID
Protein name
dual specificity mitogen-activated protein kinase kinase 2
Protein synonyms
ERK activator kinase 2, MAP kinase kinase 2, MAPK/ERK kinase 2, MEK 2, mitogen-activated protein kinase kinase 2, p45
Uniprot ID
Mouse ortholog
Map2k2 (26396)
dual specificity mitogen-activated protein kinase kinase 2 (Q9D7B0)
Alternate
BRAF
BRAF
Organism
Homo sapiens
Gene name
BRAF
Gene synonyms
BRAF1, RAFB1
NCBI Gene ID
Protein name
serine/threonine-protein kinase B-raf
Protein synonyms
94 kDa B-raf protein, B-Raf proto-oncogene serine/threonine-protein kinase (p94), B-Raf serine/threonine-protein, murine sarcoma viral (v-raf) oncogene homolog B1, p94, Proto-oncogene B-Raf, v-raf murine sarcoma viral oncogene homolog B, v-Raf murine sarcoma viral oncogene homolog B1
Uniprot ID
Mouse ortholog
Braf (109880)
serine/threonine-protein kinase B-raf (P28028)
Variants
Clinical Variant
No data
Financial
Mektovi - Pfizer
$
£
Mock data
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Tabular view
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 2,533 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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230 adverse events reported
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