Repositioning Candidate Details
| Candidate ID: | R1423 |
| Source ID: | DB11967 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Binimetinib |
| Synonyms: | Binimetinib |
| Molecular Formula: | C17H15BrF2N4O3 |
| SMILES: | CN1C=NC2=C(F)C(NC3=CC=C(Br)C=C3F)=C(C=C12)C(=O)NOCCO |
| Structure: |
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| DrugBank Description: | Binimetinib, also known as _Mektovi_, is a potent and selective oral mitogen-activated protein kinase 1/2 (MEK 1/2) inhibitor which is combined with . On June 27, 2018, the Food and Drug Administration approved the combination of and binimetinib (BRAFTOVI and MEKTOVI, from Array BioPharma Inc.) in combination for patients with unresectable or metastatic melanoma with the BRAF V600E or V600K mutations, as detected by an FDA-approved test. |
| CAS Number: | 606143-89-9 |
| Molecular Weight: | 441.233 |
| DrugBank Indication: | On June 27, 2018, the Food and Drug Administration approved encorafenib and binimetinib in combination patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test . |
| DrugBank Pharmacology: | Binimetinib is a MEK inhibitor. MEK is an enzyme that regulates the biosynthesis of the inflammatory cytokines TNF, IL-6 and IL-1. MEK inhibitors interfere with these biosynthetic processes . It is a chemotherapeutic agent that has anti-tumor activity , . |
| DrugBank MoA: | Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. The inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors. This process can result in the inhibition of growth factor-mediated cell signaling. This may lead to the inhibition of tumor cell proliferation and an inhibition in the production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are themselves threonine and tyrosine kinases that possess a dual specificity. They subsequently contribute critically to the activation of the RAS/RAF/MEK/ERK pathway and are typically upregulated in a number of different tumor cell types . |
| Targets: | Interleukin-6; Tumor necrosis factor; Interleukin-1 beta; Mitogen-activated protein kinase kinase kinase 1 inhibitor; Dual specificity mitogen-activated protein kinase kinase 2 inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class |
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