| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/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. (en)
|
| http://linked.open...y/drugbank/dosage
| |
| http://linked.open...generalReferences
| - # Salama AK, Kim KB: Trametinib (GSK1120212) in the treatment of melanoma. Expert Opin Pharmacother. 2013 Apr;14(5):619-27. doi: 10.1517/14656566.2013.770475. Epub 2013 Feb 23. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23432625 (en)
|
| http://linked.open...gy/drugbank/group
| |
| http://linked.open...drugbank/halfLife
| - Elimination half-life = 3.9-4.8 days. (en)
|
| http://linked.open...ugbank/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. (en)
|
| sameAs
| |
| Title
| |
| adms:identifier
| |
| http://linked.open...mechanismOfAction
| - 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. (en)
|
| http://linked.open...y/drugbank/patent
| |
| http://linked.open...outeOfElimination
| - 80% of the dose is excreted in the feces. <20% of the dose is excreted in the urine with <0.1% of the excreted dose in the form of the parent compound. (en)
|
| http://linked.open.../drugbank/synonym
| - GSK 1120212 (en)
- JTP 74057 (en)
- Trametinib Dimethyl Sulfoxide (en)
- Trametinibum (en)
|
| http://linked.open...drugbank/toxicity
| - Most common adverse reactions (≥20%) for trametinib include rash, diarrhea, and lymphedema. (en)
|
| http://linked.open...umeOfDistribution
| - Apparent volume of distribution (Vd/F) = 214 L (en)
|
| http://linked.open.../drug/hasAHFSCode
| |
| http://linked.open...k/foodInteraction
| - When taken with a high-fat, high-calorie meal, AUC and Cmax decreased. Tmax was also prolonged compared to fasted conditions. (en)
|
| http://linked.open...nk/proteinBinding
| - 97.4% bound to human plasma proteins. (en)
|
| foaf:page
| |
| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
| |
| http://linked.open...Molecular-Formula
| |
| http://linked.open.../Molecular-Weight
| |
| http://linked.open...noisotopic-Weight
| |
| http://linked.open...y/drugbank/SMILES
| |
| http://linked.open.../Water-Solubility
| |
| http://linked.open...ogy/drugbank/logP
| |
| http://linked.open...ogy/drugbank/logS
| |
| http://linked.open...l/drug/hasATCCode
| |
| http://linked.open...nd-Acceptor-Count
| |
| http://linked.open...-Bond-Donor-Count
| |
| http://linked.open...drugbank/InChIKey
| |
| http://linked.open...urface-Area--PSA-
| |
| http://linked.open...nk/Polarizability
| |
| http://linked.open...bank/Refractivity
| |
| http://linked.open...atable-Bond-Count
| |
| http://linked.open...ugbank/absorption
| - Trametinib is rapidly absorbed. When an oral administration of trametinib was given to patients with BRAF V600 mutation-positive melanoma, peak plasma concentration occurred 1.5 hours post-dose (Tmax). A single 2 mg oral dose has a bioavailability of 72%. When a dose of 2mg/day is given, the peak plasma concentration (Cmax) is 22.2 ng/mL. (en)
|
| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
|
| http://linked.open...casRegistryNumber
| |
| http://linked.open...rugbank/clearance
| - Apparent clearance = 4.9 L/h. (en)
|
| http://linked.open...k/Bioavailability
| |
| http://linked.open...bank/Ghose-Filter
| |
| http://linked.open...nk/MDDR-Like-Rule
| |
| http://linked.open...k/Number-of-Rings
| |
| http://linked.open...siological-Charge
| |
| http://linked.open...bank/Rule-of-Five
| |
| http://linked.open...tional-IUPAC-Name
| |
| http://linked.open...strongest-acidic-
| |
| http://linked.open...-strongest-basic-
| |
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