==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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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]
CategoriesAntineoplastic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetGonadotropin-releasing hormone receptor
Information of corresponding available drug in the market
Brand NameEligard
CompanyAtrix Labs/QLT In
Brand DiscriptionELIGARD is a sterile polymeric matrix formulation of leuprolide acetate, a GnRH agonist, for subcutaneous injection, designed to deliver leuprolide acetate at a controlled rate over a one-, three-, four- or six-month therapeutic period.
Prescribed forEligard is used to treat the symptoms of prostate cancer in men.
Chemical Name5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate
FormulationELIGARD is prefilled and supplied in two separate, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the ATRIGEL De
Physcial AppearnceSuspension
Route of AdministrationSubcutaneous Injection
Recommended Dosage7.5mg-1 injection/month, 22.5mg-1 injection per 3 month, 30mg-1 injection per 4 month, 45 mg- 1 injection every 6 month.
ContraindicationHypersensitivity and pregnancy
Side EffectsRare pain or unusual sensations in your back; numbness, weakness, or tingly feeling in your legs or feet; muscle weakness or loss of use; loss of bowel or bladder control; or liver problems - nausea, upper stomach pain, itching, tired feeling, loss of apetite.
Useful LinkSequence 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
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)