Overview
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 Encorafenib. On June 27, 2018, the Food and Drug Administration approved the combination of Encorafenib 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.
Indication
⑴与encorafenib联合，用于治疗经检测到的BRAF V600E或V600K突变的不可切除或转移性黑色素瘤患者。 ⑵与安可非尼联合，用于治疗具有BRAFV600E突变的转移性癌症（非小细胞肺癌）的成年患者。
Associated Conditions
- Metastatic Melanoma
- Metastatic Non-Small Cell Lung Cancer
- Unresectable Melanoma
Research Report
Binimetinib: A Comprehensive Review of its Pharmacology, Clinical Efficacy, and Safety
1. Introduction to Binimetinib
1.1. Overview, Chemical Properties, and DrugBank Identification
Binimetinib, identified by DrugBank ID DB11967 and CAS Number 606143-89-9, is an orally administered small molecule kinase inhibitor.[1] It is also marketed under the brand name Mektovi® and has been referred to by investigational codes such as ARRY-162, MEK162, and ARRY-438162.[2]
Chemically, binimetinib belongs to the class of benzimidazoles. Its structure is specifically 1-methyl-1H-benzimidazole substituted at positions 4, 5, and 6 by fluorine, (4-bromo-2-fluorophenyl)nitrilo, and N-(2-hydroxyethoxy)aminocarbonyl groups, respectively.[1] The molecular formula for binimetinib is C17H15BrF2N5O3, and it has a molecular weight of approximately 441.2 g/mol.[1] The complex heterocyclic structure, featuring a benzimidazole core common in kinase inhibitors, along with fluorine and bromine substitutions (which can modulate pharmacokinetic properties like lipophilicity and metabolic stability) and an N-(2-hydroxyethoxy)aminocarbonyl group (potentially involved in target binding), underpins its specific and potent biological activity.[1]
Table 1: Key Characteristics of Binimetinib
| Characteristic | Detail |
|---|---|
| DrugBank ID | DB11967 |
| CAS Number | 606143-89-9 |
| Common Synonyms | Mektovi, ARRY-162, MEK162, ARRY-438162 |
| Type | Small Molecule |
| Molecular Formula | C17H15BrF2N5O3 |
| Molecular Weight | ~441.2 g/mol |
| Therapeutic Class | Kinase Inhibitor, MEK Inhibitor |
| Key Approved Indications | - Unresectable or metastatic melanoma with BRAF V600E or V600K mutations (in combination with encorafenib) <br> - Metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation (in combination with encorafenib) |
Sources: User Query,.[1]
1.2. Therapeutic Class and General Use
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2023/12/06 | Phase 2 | Recruiting | National Cancer Center, Japan | ||
2023/07/03 | Phase 2 | Active, not recruiting | |||
2023/04/12 | Phase 1 | Completed | |||
2022/11/14 | Phase 3 | Recruiting | |||
2022/10/03 | Phase 2 | Recruiting | |||
2022/10/03 | Phase 2 | Recruiting | |||
2022/09/26 | Phase 2 | Terminated | |||
2022/09/26 | Phase 2 | Recruiting | |||
2022/08/22 | Phase 2 | Recruiting | |||
2022/05/02 | Phase 1 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Array BioPharma Inc. | 70255-010 | ORAL | 15 mg in 1 1 | 10/18/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 9/20/2018 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| MEKTOVI FILM-COATED TABLET 15MG | SIN16826P | TABLET, FILM COATED | 15mg | 7/19/2023 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| MEKTOVI binimetinib 15 mg film-coated tablet blister pack | 295440 | Medicine | A | 1/3/2019 |
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