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Namespace Prefixes

Prefix	IRI
n2	http://linked.opendata.cz/resource/drugbank/drug/
dcterms	http://purl.org/dc/terms/
n12	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/wikipedia/
n8	http://linked.opendata.cz/resource/drugbank/company/
n21	http://linked.opendata.cz/resource/mesh/concept/
n26	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/pharmgkb/
foaf	http://xmlns.com/foaf/0.1/
n25	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/pdb/
n22	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/kegg-compound/
n17	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/bindingdb/
n23	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/pubchem-compound/
n24	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/pubchem-substance/
n9	http://bio2rdf.org/drugbank:
n18	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/kegg-drug/
n15	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/drugbank/
adms	http://www.w3.org/ns/adms#
n29	http://linked.opendata.cz/resource/drugbank/patent/
n19	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/national-drug-code-directory/
n5	http://wifo5-03.informatik.uni-mannheim.de/drugbank/resource/drugs/
rdf	http://www.w3.org/1999/02/22-rdf-syntax-ns#
owl	http://www.w3.org/2002/07/owl#
n20	http://linked.opendata.cz/ontology/mesh/
n3	http://linked.opendata.cz/ontology/drugbank/
n16	http://www.drugs.com/cdi/
n10	http://linked.opendata.cz/resource/drugbank/property/
n7	http://www.rxlist.com/cgi/generic2/
n13	http://linked.opendata.cz/resource/drugbank/drug/DB01157/identifier/chemspider/
xsdh	http://www.w3.org/2001/XMLSchema#
n28	http://linked.opendata.cz/resource/atc/
n27	http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item: n2:DB01157
rdf:type: n3:Drug
n3:description: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against pneumocystis pneumonia in AIDS patients. Myelosuppression is its dose-limiting toxic effect. [PubChem]
n3:group: investigational approved
n3:halfLife: 11 to 20 hours
n3:indication: For use, with concurrent leucovorin administration (leucovorin protection), as an alternative therapy for the treatment of moderate-to-severe Pneumocystis carinii pneumonia (PCP) in immunocompromised patients, including patients with the acquired immunodeficiency syndrome (AIDS). Also used to treat several types of cancer including colon cancer.
owl:sameAs: n5:DB01157 n9:DB01157
dcterms:title: Trimetrexate
adms:identifier: n12:Trimetrexate n13:5381 n15:DB01157 n17:18268 n18:D06238 n19:58178-020-10 n22:C11154 n23:5583 n24:46505247 n25:TMQ n26:PA451790
n3:mechanismOfAction: In vitro studies have shown that trimetrexate is a competitive inhibitor of dihydrofolate reductase (DHFR) from bacterial, protozoan, and mammalian sources. DHFR catalyzes the reduction of intracellular dihydrofolate to the active coenzyme tetrahydrofolate. Inhibition of DHFR results in the depletion of this coenzyme, leading directly to interference with thymidylate biosynthesis, as well as inhibition of folate-dependent formyltransferases, and indirectly to inhibition of p.r.n. biosynthesis. The end result is disruption of DNA, RNA, and protein synthesis, with consequent cell death.
n3:packager: n8:271B4B5E-363D-11E5-9242-09173F13E4C5 n8:271B4B5D-363D-11E5-9242-09173F13E4C5
n3:patent: n29:6017922
n3:routeOfElimination: Ten to 30% of the administered dose is excreted unchanged in the urine.
n3:synonym: SID26755046 Trimetrexato SID50110873 CI-898 Neutrexin TMQ Trimetrexate Trimetrexatum TMX
n3:toxicity: The LD50 of intravenous trimetrexate in mice is 62 mg/kg (186 mg/m2). Myelosuppression is a dose-limiting toxic effect.
n3:volumeOfDistribution: * 20 ± 8 L/m2 * 36.9 ± 6 L/m2 [cancer patients]
n3:proteinBinding: 95% (over the concentration range of 18.75 to 1000 ng/mL)
n3:synthesisReference: Martin Stogniew, Javad M. Zadei, "Compositions comprising trimetrexate and methods of their synthesis and use." U.S. Patent US6258821, issued January, 1974.
n20:hasConcept: n21:M0025316
foaf:page: n7:trimetrexate.htm n16:trimetrexate.html
n3:IUPAC-Name: n10:271B4B63-363D-11E5-9242-09173F13E4C5
n3:InChI: n10:271B4B69-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula: n10:271B4B68-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight: n10:271B4B65-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight: n10:271B4B66-363D-11E5-9242-09173F13E4C5
n3:SMILES: n10:271B4B67-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility: n10:271B4B79-363D-11E5-9242-09173F13E4C5 n10:271B4B61-363D-11E5-9242-09173F13E4C5
n3:logP: n10:271B4B5F-363D-11E5-9242-09173F13E4C5 n10:271B4B7B-363D-11E5-9242-09173F13E4C5 n10:271B4B62-363D-11E5-9242-09173F13E4C5
n3:logS: n10:271B4B60-363D-11E5-9242-09173F13E4C5
n3:pKa: n10:271B4B7C-363D-11E5-9242-09173F13E4C5
n27:hasATCCode: n28:P01AX07
n3:H-Bond-Acceptor-Count: n10:271B4B6F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count: n10:271B4B70-363D-11E5-9242-09173F13E4C5
n3:InChIKey: n10:271B4B6A-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-: n10:271B4B6B-363D-11E5-9242-09173F13E4C5
n3:Polarizability: n10:271B4B6D-363D-11E5-9242-09173F13E4C5
n3:Refractivity: n10:271B4B6C-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count: n10:271B4B6E-363D-11E5-9242-09173F13E4C5
n3:affectedOrganism: Pneumocystis carinii Humans and other mammals Bacteria and protozoa
n3:casRegistryNumber: 52128-35-5
n3:category
n3:clearance: * 38 +/- 15 mL/min/m2 [patients with acquired immunodeficiency syndrome (AIDS) who had Pneumocystis carinii pneumonia (4 patients) or toxoplasmosis (2 patients). Trimetrexate was administered intravenously as a bolus injection at a dose of 30 mg/m2/day along with leucovorin 20 mg/m2 every 6 hours for 21 days] * 53 +/- 41 mL/min/m2 [Cancer patients with advanced solid tumors using various dosage regimensreceiving a single-dose administration of 10 to 130 mg/m2] * 30 +/- 8 mL/min/m2 [Cancer patients with advanced solid tumors using various dosage regimensafter a five-day infusion]
n3:Bioavailability: n10:271B4B75-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter: n10:271B4B77-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule: n10:271B4B78-363D-11E5-9242-09173F13E4C5
n3:Melting-Point: n10:271B4B7A-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings: n10:271B4B74-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge: n10:271B4B73-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five: n10:271B4B76-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name: n10:271B4B64-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-: n10:271B4B71-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-: n10:271B4B72-363D-11E5-9242-09173F13E4C5