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Namespace Prefixes

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Statements

Subject Item
n2:DB05482
rdf:type
n3:Drug
n3:description
LE-SN38 is NeoPharm's NeoLipid liposomal formulation of SN-38, the active metabolite of irinotecan (Camptosar), a chemotherapeutic pro-drug approved for the treatment of advanced colorectal cancer. LE-SN38 is the Company's NeoLipid(R) Liposomal formulation of SN-38, the active, but poorly soluble, metabolite of Camptosar(R), a chemotherapeutic pro-drug, which is used as a first-line and second-line treatment for advanced colorectal cancer. A pro-drug is a compound that is converted into the active drug in the body. However, Camptosar(R) is converted into SN-38 in colorectal cancer cells at different rates in different patients, and this variability in conversion rates may result in suboptimal treatment. By employing the Company's proprietary NeoLipid(R) technology to directly deliver SN-38, the Company hopes to minimize treatment variability. A Phase I clinical trial was completed in 2005 and showed the potential for decreased side effects, particularly diarrhea, compared to published results of Camptosar(R). The results of that trial were presented at the American Society of Clinical Oncology (ASCO) meeting in June 2005, and were used to determine the Phase II study dose.
n3:generalReferences
# Xuan T, Zhang JA, Ahmad I: HPLC method for determination of SN-38 content and SN-38 entrapment efficiency in a novel liposome-based formulation, LE-SN38. J Pharm Biomed Anal. 2006 May 3;41(2):582-8. Epub 2006 Jan 18. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16386867 # Peikov V, Ugwu S, Parmar M, Zhang A, Ahmad I: pH-dependent association of SN-38 with lipid bilayers of a novel liposomal formulation. Int J Pharm. 2005 Aug 11;299(1-2):92-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15996839 # Pal A, Khan S, Wang YF, Kamath N, Sarkar AK, Ahmad A, Sheikh S, Ali S, Carbonaro D, Zhang A, Ahmad I: Preclinical safety, pharmacokinetics and antitumor efficacy profile of liposome-entrapped SN-38 formulation. Anticancer Res. 2005 Jan-Feb;25(1A):331-41. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15816556 # Khan S, Ahmad A, Guo W, Wang YF, Abu-Qare A, Ahmad I: A simple and sensitive LC/MS/MS assay for 7-ethyl-10-hydroxycamptothecin (SN-38) in mouse plasma and tissues: application to pharmacokinetic study of liposome entrapped SN-38 (LE-SN38). J Pharm Biomed Anal. 2005 Feb 7;37(1):135-42. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15664753 # Lei S, Chien PY, Sheikh S, Zhang A, Ali S, Ahmad I: Enhanced therapeutic efficacy of a novel liposome-based formulation of SN-38 against human tumor models in SCID mice. Anticancer Drugs. 2004 Sep;15(8):773-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15494639 # Zhang JA, Xuan T, Parmar M, Ma L, Ugwu S, Ali S, Ahmad I: Development and characterization of a novel liposome-based formulation of SN-38. Int J Pharm. 2004 Feb 11;270(1-2):93-107. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14726126 # Khan S, Ahmad A, Ahmad I: A sensitive and rapid liquid chromatography tandem mass spectrometry method for quantitative determination of 7-ethyl-10-hydroxycamptothecin (SN-38) in human plasma containing liposome-based SN-38 (LE-SN38). Biomed Chromatogr. 2003 Dec;17(8):493-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14648604 # Guo W, Ahmad A, Khan S, Dahhani F, Wang YF, Ahmad I: Determination by liquid chromatography with fluorescence detection of total 7-ethyl-10-hydroxy-camptothecin (SN-38) in beagle dog plasma after intravenous administration of liposome-based SN-38 (LE-SN38). J Chromatogr B Analyt Technol Biomed Life Sci. 2003 Jul 5;791(1-2):85-92. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12798168
n3:group
investigational
n3:indication
Investigated for use/treatment in colorectal cancer.
owl:sameAs
n12:DB05482
dcterms:title
LE-SN38
adms:identifier
n6:104842 n7:94634 n9:DB05482 n10:50099247
n3:mechanismOfAction
The entrapment of SN-38 in lipsomes results in a more stable and more soluble form of the drug. This allows for increased affinity of SN-38 to lipid membranes and improved delivery of the drug to tumor sites. SN-38 is a highly effective cytotoxic topoisomerase I inhibitor.
n3:synonym
Liposome entrapped 7-ethyl-10-hydroxycamptothecin Liposome entrapped SN38
n3:IUPAC-Name
n4:271B44F6-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B44FC-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B44FB-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B44F8-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B44F9-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B44FA-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B44F4-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B44F5-363D-11E5-9242-09173F13E4C5 n4:271B44F2-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B44F3-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n4:271B4502-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4503-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B44FD-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B44FE-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4500-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B44FF-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4501-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B4508-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B450A-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B450B-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4507-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4506-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4509-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B44F7-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4504-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4505-363D-11E5-9242-09173F13E4C5