Leuprolide,Leuprorelin.
Leuprorelin(INN)orleuprolideacetate(USAN)isagonadotropin-releasinghormoneago
NIST(GnRHagonist).BycausingconstantstimulationofthepituitaryGnRHreceptors,itinitiallycausesstimulation(flare),butthereafterdecreasespituitarysecretion(downregulation)ofgonadotropinsluteinizinghormone(LH)andfollicle-stimulatinghormone(FSH).LikeotherGnRHagonists,leuprolidemaybeusedinthetreatmentofhormone-responsivecancerssuchasprostatecancerorbreastcancer,estrogen-dependentconditions(suchasendometriosisoruterinefibroids),totreatprecociouspuberty,andtocontrolovarianstimulationinIVF.
LeuprolideHumanSyntheticisasingle,non-glycosylated,polypeptidechaincontaining9aminoacidsandhavingamolecularmassof1209Dalton.ThemolecularformulaisC59H84N16O12.
SterileFilteredWhitelyophilized(freeze-dried)powder.
TheLeuprorelinwaslyophilizedfromaconcentrated(1mg/ml)solutionwithnoadditives.
ItisrecommendedtoreconstitutethelyophilizedLeoprolideinsterile18MΩ-cmH2Onotlessthan100µg/ml,whichcanthenbefurtherdilutedtootheraqueoussolutions.
LyophilizedLeoprolidealthoughstableatroomtemperaturefor3weeks,shouldbestoreddesiccatedbelow-18°C.UponreconstitutionLeuprorelinshouldbestoredat4°Cbetween2-7daysandforfutureusebelow-18°C.Forlongtermstorageitisrecommendedtoaddacarrierprotein(0.1%HSAorBSA).Pleasepreventfreeze-thawcycles.
Greaterthan98.0%asdeterminedbyRP-HPLC.
pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt.
Prospec"sproductsarefurnishedforLABORATORYRESEARCHUSEONLY.Theproductmaynotbeusedasdrugs,agriculturalorpesticidalproducts,foodadditivesorhouseholdchemicals.