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Namespace Prefixes

PrefixIRI
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dctermshttp://purl.org/dc/terms/
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n13http://linked.opendata.cz/resource/drugbank/drug/DB04905/identifier/pubchem-compound/
n7http://bio2rdf.org/drugbank:
n11http://linked.opendata.cz/resource/drugbank/drug/DB04905/identifier/pubchem-substance/
admshttp://www.w3.org/ns/adms#
n12http://linked.opendata.cz/resource/drugbank/drug/DB04905/identifier/drugbank/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n4http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
n10http://linked.opendata.cz/resource/drugbank/drug/DB04905/identifier/chemspider/

Statements

Subject Item
n2:DB04905
rdf:type
n3:Drug
n3:description
Tesmilifene is a novel potentiator of chemotherapy which, when added to doxorubicin, achieved an unexpected and very large survival advantage over doxorubicin alone in a randomized trial in advanced breast cancer.
n3:generalReferences
# Liu J, Tu D, Dancey J, Reyno L, Pritchard KI, Pater J, Seymour LK: Quality of life analyses in a clinical trial of DPPE (tesmilifene) plus doxorubicin versus doxorubicin in patients with advanced or metastatic breast cancer: NCIC CTG Trial MA.19. Breast Cancer Res Treat. 2006 Dec;100(3):263-71. Epub 2006 Jul 6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16823511 # Vincent M: Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump. Med Hypotheses. 2006;66(4):715-31. Epub 2006 Jan 18. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16413681 # Raghavan D, Brandes LJ, Klapp K, Snyder T, Styles E, Tsao-Wei D, Lieskovsky G, Quinn DI, Ramsey EW: Phase II trial of tesmilifene plus mitoxantrone and prednisone for hormone refractory prostate cancer: high subjective and objective response in patients with symptomatic metastases. J Urol. 2005 Nov;174(5):1808-13; discussion 1813. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16217292 # Brandes LJ, Queen GM, LaBella FS: N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine (DPPE) a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs. Cancer Chemother Pharmacol. 2000;45(4):298-304. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10755318 # Brandes LJ, Hogg GR: Study of the in-vivo antioestrogenic action of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE), a novel intracellular histamine antagonist and antioestrogen binding site ligand. J Reprod Fertil. 1990 May;89(1):59-67. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/2374133
n3:group
investigational
n3:indication
Intended for the treatment of various forms of cancer.
owl:sameAs
n7:DB04905
dcterms:title
Tesmilifene
adms:identifier
n9:50085260 n10:97190 n11:10234594 n12:DB04905 n13:108092
n3:mechanismOfAction
Although the exact mechanism of action is not known, one study (PMID: 16413681) proposes that tesmilifene may be an activating p-gp substrate, which enables the p-gp pump to extrude typical p-gp substrates (such as anthracyclines or taxanes) more efficiently. This process consumes ATP, since the p-gp is absolutely, and highly dependent on ATP hydrolysis. The mechanism of cell death is likely to result not from the presence of chemotherapy inside the cell (in fact the chemotherapy is extruded) but, directly or indirectly, from the enhanced consumption of ATP. The ATP may be consumed below a threshold necessary for survival, or, (more likely) the enhanced ATP production required to maintain ATP levels may result in the generation of reactive oxygen species (ROS) to an extent that overwhelms the cell’s ability to inactivate them. The result would be additional cell death, but only in the mdr+ population. The doxorubicin would continue to act on the drug sensitive remainder of the cell population, but without the help of tesmilifene.
n3:synonym
N,N-diethyl-2-((4-phenylmethyl)phenoxy)ethanamine Depmpe DPPE
n3:IUPAC-Name
n4:271B5E53-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5E59-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5E58-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5E55-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5E56-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5E57-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5E51-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5E4F-363D-11E5-9242-09173F13E4C5 n4:271B5E52-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5E50-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n4:271B5E5F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5E60-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5E5A-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5E5B-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5E5D-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5E5C-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5E5E-363D-11E5-9242-09173F13E4C5
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
98774-23-3
n3:category
n3:Bioavailability
n4:271B5E64-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5E66-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5E67-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5E63-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5E62-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5E65-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5E54-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5E61-363D-11E5-9242-09173F13E4C5