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1039 details
Primary information
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, 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
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
CategoriesHormonal and Fertility Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameEnantone
CompanyTakeda
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearnceSolution
Route of AdministrationInjection
Recommended DosageOne3.75 mg DPS mnthly or one 11.25 mg DPS every 3 month as a single SC/IM injection.
ContraindicationHypersensitivity, undiagnosed abnormal vag bleeding, pregnancy, lactation
Side EffectsWeightloss, Parosmia (distortion of the sense of smell, as in smelling odours that are not present), Nausea (feeling of having an urge to vomit), Musculoskeletal Stiffness (stiffness of the body's muscles, joints, tendons, ligaments and nerves), Mood Swinng.
Useful Linkhttp://www.eligard.com
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)