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Namespace Prefixes

PrefixIRI
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dctermshttp://purl.org/dc/terms/
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n16http://linked.opendata.cz/resource/drugbank/drug/DB08911/identifier/wikipedia/
n7http://www.drugs.com/
n20http://www.rxlist.com/
n12http://bio2rdf.org/drugbank:
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n18http://linked.opendata.cz/resource/drugbank/drug/DB08911/identifier/kegg-drug/
n17http://linked.opendata.cz/resource/drugbank/drug/DB08911/identifier/drugbank/
n10http://linked.opendata.cz/resource/drugbank/patent/
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owlhttp://www.w3.org/2002/07/owl#
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n5http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
n19http://linked.opendata.cz/resource/atc/
n8http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB08911
rdf:type
n3:Drug
n3: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.
n3:dosage
n4:271B5C92-363D-11E5-9242-09173F13E4C5 n4:271B5C93-363D-11E5-9242-09173F13E4C5 n4:271B5C8F-363D-11E5-9242-09173F13E4C5 n4:271B5C90-363D-11E5-9242-09173F13E4C5 n4:271B5C91-363D-11E5-9242-09173F13E4C5
n3: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
n3:group
approved
n3:halfLife
Elimination half-life = 3.9-4.8 days.
n3: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.
owl:sameAs
n12:DB08911
dcterms:title
Trametinib
adms:identifier
n15:0173-0848-13 n16:Trametinib n17:DB08911 n18:D10175
n3: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.
n3:patent
n10:7378423
n3:routeOfElimination
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.
n3:synonym
GSK 1120212 Trametinibum Trametinib Dimethyl Sulfoxide JTP 74057
n3:toxicity
Most common adverse reactions (≥20%) for trametinib include rash, diarrhea, and lymphedema.
n3:volumeOfDistribution
Apparent volume of distribution (Vd/F) = 214 L
n8:hasAHFSCode
n9:10-00%20
n3:foodInteraction
When taken with a high-fat, high-calorie meal, AUC and Cmax decreased. Tmax was also prolonged compared to fasted conditions.
n3:proteinBinding
97.4% bound to human plasma proteins.
foaf:page
n7:mekinist.html n20:mekinist-drug.htm
n3:IUPAC-Name
n5:271B5C98-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B5C9E-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B5C9D-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B5C9A-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B5C9B-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B5C9C-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B5C96-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B5C94-363D-11E5-9242-09173F13E4C5 n5:271B5C97-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B5C95-363D-11E5-9242-09173F13E4C5
n8:hasATCCode
n19:L01XE25
n3:H-Bond-Acceptor-Count
n5:271B5CA4-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B5CA5-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B5C9F-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B5CA0-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B5CA2-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B5CA1-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B5CA3-363D-11E5-9242-09173F13E4C5
n3: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.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
871700-17-3
n3:clearance
Apparent clearance = 4.9 L/h.
n3:Bioavailability
n5:271B5CAA-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B5CAC-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B5CAD-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B5CA9-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B5CA8-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B5CAB-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B5C99-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B5CA6-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B5CA7-363D-11E5-9242-09173F13E4C5