Repositioning Candidate Details
| Candidate ID: | R1186 |
| Source ID: | DB08911 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Trametinib |
| Synonyms: | -- |
| Molecular Formula: | C26H23FIN5O4 |
| SMILES: | CN1C(=O)C(C)=C2N(C(=O)N(C3CC3)C(=O)C2=C1NC1=CC=C(I)C=C1F)C1=CC(NC(C)=O)=CC=C1 |
| Structure: |
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| DrugBank Description: | Trametinib dimethyl sulfoxide is a kinase inhibitor. Each 1-mg tablet contains 1.127 mg trametinib dimethyl sulfoxide equivalent to 1 mg of trametinib non-solvated parent. FDA approved on May 29, 2013 . The U.S. Food and Drug Administration approved (Tafilnar) and Mekinist (trametinib), administered together, for the treatment of anaplastic thyroid cancer (ATC) that cannot be removed by surgery or has spread to other parts of the body (metastatic), and has a type of abnormal gene, BRAF V600E (BRAF V600E mutation-positive) . Thyroid cancer is a disease in which cancer cells form in the tissues of the thyroid. Anaplastic thyroid cancer is a rare, aggressive type of thyroid cancer. The National Institutes of Health (NIH) estimates there will be 53,990 new cases of thyroid cancer and an estimated 2,060 deaths from the disease in the United States in 2018. Anaplastic thyroid cancer accounts for approximately 1 to 2 percent of all thyroid cancers . |
| CAS Number: | 871700-17-3 |
| Molecular Weight: | 615.3948 |
| DrugBank Indication: | Trametinib is indicated for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test . In May 2018, it was approved for use with for the treatment of treat anaplastic thyroid cancer caused by an abnormal BRAF V600E gene . |
| DrugBank Pharmacology: | Trametinib is an anticancer agent which causes apoptosis (or programmed cell death) and inhibits cell proliferation, which are both important in the treatment of malignancies . |
| DrugBank MoA: | Trametinib is a reversible, allosteric inhibitor of mitogen-activated extracellular signal regulated kinase 1 _(MEK1)_ and _MEK2_ activation and of_ MEK1_ and _MEK2_ kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. Trametinib helps with melanoma with the BRAF V600E or V600K as the mutation results in the constitutive activation of the BRAF pathway which includes MEK1 and MEK2 . |
| Targets: | Dual specificity mitogen-activated protein kinase kinase 1 antagonist&inhibitor; Dual specificity mitogen-activated protein kinase kinase 2 antagonist&inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
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