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Statements

Subject Item
n2:DB00007
rdf:type
n3:Drug
n3:description
Leuprolide belongs to the general class of drugs known as hormones or hormone antagonists. It is a synthetic 9 residue peptide analog of gonadotropin releasing hormone. Leuprolide is used to treat advanced prostate cancer. It is also used to treat uterine fibroids and endometriosis. Leuprolide is also under investigation for possible use in the treatment of mild to moderate Alzheimer's disease.
n3:dosage
n8:271B3EE1-363D-11E5-9242-09173F13E4C5 n8:271B3EE2-363D-11E5-9242-09173F13E4C5 n8:271B3EE3-363D-11E5-9242-09173F13E4C5 n8:271B3EE0-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Saleh FM, Niel T, Fishman MJ: Treatment of paraphilia in young adults with leuprolide acetate: a preliminary case report series. J Forensic Sci. 2004 Nov;49(6):1343-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15568711 # Geier MR, Geier DA: The potential importance of steroids in the treatment of autistic spectrum disorders and other disorders involving mercury toxicity. Med Hypotheses. 2005;64(5):946-54. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15780490 # Doraiswamy PM, Xiong GL: Pharmacological strategies for the prevention of Alzheimer's disease. Expert Opin Pharmacother. 2006 Jan;7(1):1-10. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16370917 # Sequence Information "Link":http://www.freepatentsonline.com/EP1790656.html # "RxMed":http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20(General%20Monographs-%20L)/LUPRON%20DEPOT.html
n3:group
investigational approved
n3:halfLife
~3 hours
n3:indication
For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty
owl:sameAs
n26:DB00007 n27:DB00007
dcterms:title
Leuprolide
adms:identifier
n10:6427 n11:DB00007 n14:0024-0793-75 n16:C07612 n17:D08113 n18:Leuprolide n19:PA450203
n3:mechanismOfAction
Leuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.
n3:packager
n7:271B3ED8-363D-11E5-9242-09173F13E4C5 n7:271B3ED6-363D-11E5-9242-09173F13E4C5 n7:271B3ED7-363D-11E5-9242-09173F13E4C5 n7:271B3ED0-363D-11E5-9242-09173F13E4C5 n7:271B3ED1-363D-11E5-9242-09173F13E4C5 n7:271B3ECE-363D-11E5-9242-09173F13E4C5 n7:271B3ECF-363D-11E5-9242-09173F13E4C5 n7:271B3ED4-363D-11E5-9242-09173F13E4C5 n7:271B3ED5-363D-11E5-9242-09173F13E4C5 n7:271B3ED2-363D-11E5-9242-09173F13E4C5 n7:271B3ED3-363D-11E5-9242-09173F13E4C5
n3:routeOfElimination
Excretion in urine
n3:synonym
(D-Leu(6),des-gly-NH2(10),pro-ethylamide(9))-gonadotropin-releasing hormone L-Pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-L-proline ethylamide Leuprorelinum Leuprorelina PGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-nhet Leuprorelin PGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-NHC2H5 Leuproreline
n3:toxicity
In rats subcutaneous administration of 250 to 500 times the recommended human dose, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a clinical counterpart of this phenomenon. In early clinical trials with leuprolide acetate doses as high as 20 mg/day for up to two years caused no adverse effects differing from those observed with the 1 mg/day dose.
n3:volumeOfDistribution
* 27 L [intravenous bolus administration to healthy male volunteers]
n22:hasAHFSCode
n24:10-00-00
n3:proteinBinding
43% to 49%
n3:salt
n3:synthesisReference
Daniel Kadzimirzs, Gerhard Jas, Volker Autze, "Solution-Phase Synthesis of Leuprolide and Its Intermediates." U.S. Patent US20090005535, issued January 01, 2009.
n12:hasConcept
n13:M0025473
foaf:page
n6:leuprolide.html n15:eligard.htm
n3:Molecular-Formula
n20:271B3EE6-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n20:271B3EE5-363D-11E5-9242-09173F13E4C5
n22:hasATCCode
n23:L02AE02
n3:absorption
Bioavailability by subcutaneous administration is comparable to that by intravenous administration.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
53714-56-0
n3:category
n3:clearance
* 8.34 L/h [healthy male receiving a 1-mg IV bolus]
n3:containedIn
n4:271B3EDA-363D-11E5-9242-09173F13E4C5 n4:271B3EDB-363D-11E5-9242-09173F13E4C5 n4:271B3ED9-363D-11E5-9242-09173F13E4C5 n4:271B3EDE-363D-11E5-9242-09173F13E4C5 n4:271B3EDF-363D-11E5-9242-09173F13E4C5 n4:271B3EDC-363D-11E5-9242-09173F13E4C5 n4:271B3EDD-363D-11E5-9242-09173F13E4C5
n3:Hydrophobicity
n20:271B3EE4-363D-11E5-9242-09173F13E4C5