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Identification
NameLeuprolide
Accession NumberDB00007  (BTD00009, BIOD00009)
TypeBiotech
GroupsApproved, Investigational
DescriptionLeuprolide 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.
Protein structureDb00007
Related Articles
Protein chemical formulaC59H84N16O12
Protein average weight1209.3983 Da
Sequences
>Leuprolide
PHWSYLLR
Download FASTA Format
Synonyms
(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
Leuprorelin
Leuprorelina
Leuproreline
Leuprorelinum
PGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-NHC2H5
PGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-nhet
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EligardKitSanofi Aventis U.S. Llc2002-01-232016-10-13Us
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2005-01-07Not applicableUs
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2002-08-26Not applicableUs
EligardKitSanofi Aventis U.S. Llc2002-01-232016-10-13Us
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2005-01-07Not applicableUs
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2002-08-26Not applicableUs
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2002-05-15Not applicableUs
EligardKitSanofi Aventis U.S. Llc2002-01-232016-10-13Us
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2003-02-26Not applicableUs
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2002-05-15Not applicableUs
EligardKitSanofi Aventis U.S. Llc2002-01-232016-10-13Us
EligardKitSubcutaneousTolmar Pharmaceuticals Inc.2003-02-26Not applicableUs
Eligard 22.5mgInjection, powder, for suspension, extended release28.2 mgSubcutaneousSanofi Aventis Canada Inc2003-12-01Not applicableCanada
Eligard 30 mgInjection, powder, for suspension, extended release35.8 mgSubcutaneousSanofi Aventis Canada Inc2004-04-29Not applicableCanada
Eligard 45 mgInjection, powder, for suspension, extended release58.2 mgSubcutaneousSanofi Aventis Canada Inc2005-08-15Not applicableCanada
Eligard 7.5mgInjection, powder, for suspension, extended release10.2 mgSubcutaneousSanofi Aventis Canada Inc2003-12-01Not applicableCanada
Leuprolide Acetate InjectionLiquid5 mgSubcutaneousNovopharm LimitedNot applicableNot applicableCanada
LupronLiquid5 mgSubcutaneousAbbvie Corporation1985-12-31Not applicableCanada
Lupron DepotKitAbb Vie Inc.1990-10-22Not applicableUs
Lupron DepotKitAbb Vie Inc.1995-12-22Not applicableUs
Lupron DepotInjection, powder, for suspension, extended release30 mgIntramuscularAbbvie Corporation1999-09-13Not applicableCanada
Lupron DepotKitAbb Vie Inc.1995-12-22Not applicableUs
Lupron DepotInjection, powder, for suspension, extended release7.5 mgIntramuscularAbbvie Corporation1989-12-31Not applicableCanada
Lupron DepotInjection, powder, for suspension, extended release11.25 mgIntramuscularAbbvie Corporation1999-09-13Not applicableCanada
Lupron DepotKitAbb Vie Inc.2010-11-08Not applicableUs
Lupron DepotKitAbb Vie Inc.1995-12-22Not applicableUs
Lupron DepotInjection, powder, for suspension, extended release3.75 mgIntramuscularAbbvie Corporation1992-12-31Not applicableCanada
Lupron DepotInjection, powder, for suspension, extended release11.25 mgIntramuscularAbbvie CorporationNot applicableNot applicableCanada
Lupron DepotKitAbb Vie Inc.1989-01-26Not applicableUs
Lupron DepotInjection, powder, for suspension, extended release22.5 mgIntramuscularAbbvie Corporation1997-01-29Not applicableCanada
Lupron DepotInjection, powder, for suspension, extended release15 mgIntramuscularAbbvie CorporationNot applicableNot applicableCanada
Lupron Depot-pedKitAbb Vie Inc.1993-04-16Not applicableUs
Lupron Depot-pedKitAbb Vie Inc.1993-04-16Not applicableUs
Lupron Depot-pedKitAbb Vie Inc.1993-04-16Not applicableUs
Lupron Depot-pedKitAbb Vie Inc.1993-04-16Not applicableUs
Lupron Depot-pedKitAbb Vie Inc.1993-04-16Not applicableUs
Lupron Depot-pedKitREMEDYREPACK INC.2015-07-28Not applicableUs
Zeulide DepotInjection, powder, for suspension, extended release; Kit5.06 mgIntramuscularPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Leuprolide AcetateInjection, solution1 mg/.2mLSubcutaneousEon Labs, Inc.1998-08-04Not applicableUs
Leuprolide AcetateKitSun Pharma Global FZE2014-12-15Not applicableUs
Leuprolide AcetateKitTeva Parenteral Medicines, Inc.2000-11-06Not applicableUs
Leuprolide AcetateKitSandoz Inc1998-08-04Not applicableUs
Leuprolide AcetateKitSubcutaneousSun Pharma Global Inc.2009-03-03Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EnantoneNot Available
LeuplinTakeda
LeuProMaxxBaxter/Teva
LeupromerNot Available
LutrateNot Available
MemryteCuraxis
Prostap 3Takeda UK
Prostap SRTakeda UK
ViadurBayer AG
Brand mixtures
NameLabellerIngredients
Lupaneta PackAbb Vie Inc.
Salts
Name/CASStructureProperties
Leuprolide acetate
74381-53-6
Thumb
  • InChI Key: RGLRXNKKBLIBQS-XNHQSDQCSA-N
  • Monoisotopic Mass: 1268.666591604
  • Average Mass: 1269.4502
DBSALT000105
Categories
UNIIEFY6W0M8TG
CAS number53714-56-0
Pharmacology
IndicationFor treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty
Structured Indications
PharmacodynamicsUsed in the palliative treatment of advanced prostate cancer. Leuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.
Mechanism of actionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.
TargetKindPharmacological actionActionsOrganismUniProt ID
Gonadotropin-releasing hormone receptorProteinyes
agonist
HumanP30968 details
Related Articles
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of distribution
  • 27 L [intravenous bolus administration to healthy male volunteers]
Protein binding43% to 49%
Metabolism

Primarily degraded by peptidase and not by cytochrome P450 enzymes.

Route of eliminationExcretion in urine
Half life~3 hours
Clearance
  • 8.34 L/h [healthy male receiving a 1-mg IV bolus]
ToxicityIn 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.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Leuprolide.Approved, Investigational
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Leuprolide.Withdrawn
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Leuprolide.Approved
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Leuprolide.Experimental
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Leuprolide.Approved
AmantadineAmantadine may increase the QTc-prolonging activities of Leuprolide.Approved
AmiodaroneLeuprolide may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Leuprolide.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Leuprolide.Approved
AnagrelideLeuprolide may increase the QTc-prolonging activities of Anagrelide.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Leuprolide.Investigational
ApomorphineApomorphine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
ArformoterolArformoterol may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
Arsenic trioxideLeuprolide may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherLeuprolide may increase the QTc-prolonging activities of Artemether.Approved
AsenapineLeuprolide may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirAtazanavir may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Leuprolide.Approved
AzithromycinLeuprolide may increase the QTc-prolonging activities of Azithromycin.Approved
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Leuprolide.Investigational
BedaquilineLeuprolide may increase the QTc-prolonging activities of Bedaquiline.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Leuprolide.Approved, Investigational
BortezomibBortezomib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Leuprolide.Withdrawn
BuserelinBuserelin may increase the QTc-prolonging activities of Leuprolide.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Leuprolide.Approved
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Leuprolide.Approved
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Leuprolide.Experimental
CeritinibLeuprolide may increase the QTc-prolonging activities of Ceritinib.Approved
ChloroquineLeuprolide may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazineLeuprolide may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Leuprolide.Approved
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Leuprolide.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Leuprolide.Experimental
CiprofloxacinLeuprolide may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideLeuprolide may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramLeuprolide may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinLeuprolide may increase the QTc-prolonging activities of Clarithromycin.Approved
ClomipramineClomipramine may increase the QTc-prolonging activities of Leuprolide.Approved, Vet Approved
ClozapineLeuprolide may increase the QTc-prolonging activities of Clozapine.Approved
Corifollitropin AlfaThe therapeutic efficacy of Corifollitropin Alfa can be increased when used in combination with Leuprolide.Approved
CrizotinibLeuprolide may increase the QTc-prolonging activities of Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Leuprolide.Approved, Investigational
DabrafenibDabrafenib may increase the QTc-prolonging activities of Leuprolide.Approved
DasatinibDasatinib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Leuprolide.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Leuprolide.Investigational
DesfluraneDesflurane may increase the QTc-prolonging activities of Leuprolide.Approved
DesipramineDesipramine may increase the QTc-prolonging activities of Leuprolide.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Leuprolide.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Leuprolide.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Leuprolide.Approved
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Leuprolide.Approved
DisopyramideLeuprolide may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Leuprolide.Approved, Investigational
DofetilideLeuprolide may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronLeuprolide may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneLeuprolide may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Leuprolide.Approved
DronedaroneLeuprolide may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolLeuprolide may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Leuprolide.Approved
EliglustatLeuprolide may increase the QTc-prolonging activities of Eliglustat.Approved
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Leuprolide.Approved
EribulinEribulin may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
ErythromycinLeuprolide may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramLeuprolide may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Leuprolide.Approved, Investigational
EzogabineEzogabine may increase the QTc-prolonging activities of Leuprolide.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Leuprolide.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Leuprolide.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
FlecainideLeuprolide may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluconazoleFluconazole may increase the QTc-prolonging activities of Leuprolide.Approved
FluoxetineLeuprolide may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolLeuprolide may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FormoterolFormoterol may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
FoscarnetFoscarnet may increase the QTc-prolonging activities of Leuprolide.Approved
Gadobenic acidLeuprolide may increase the QTc-prolonging activities of Gadobenic acid.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Leuprolide.Approved
GemifloxacinLeuprolide may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Leuprolide.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Leuprolide.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Leuprolide.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Leuprolide.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Leuprolide.Approved
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Leuprolide.Approved
GoserelinLeuprolide may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronLeuprolide may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Leuprolide.Investigational
HaloperidolLeuprolide may increase the QTc-prolonging activities of Haloperidol.Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Leuprolide.Approved
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Leuprolide.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
IbutilideLeuprolide may increase the QTc-prolonging activities of Ibutilide.Approved
IloperidoneLeuprolide may increase the QTc-prolonging activities of Iloperidone.Approved
ImipramineImipramine may increase the QTc-prolonging activities of Leuprolide.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Leuprolide.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Leuprolide.Approved
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Leuprolide.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Leuprolide.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Leuprolide.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Leuprolide.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Leuprolide.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Leuprolide.Approved
IsofluraneIsoflurane may increase the QTc-prolonging activities of Leuprolide.Approved, Vet Approved
IsradipineIsradipine may increase the QTc-prolonging activities of Leuprolide.Approved
ItraconazoleItraconazole may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Leuprolide.Approved
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LenvatinibLeuprolide may increase the QTc-prolonging activities of Lenvatinib.Approved
LevofloxacinLeuprolide may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Leuprolide.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Leuprolide.Approved
LithiumLithium may increase the QTc-prolonging activities of Leuprolide.Approved
LopinavirLeuprolide may increase the QTc-prolonging activities of Lopinavir.Approved
LumefantrineLeuprolide may increase the QTc-prolonging activities of Lumefantrine.Approved
MaprotilineMaprotiline may increase the QTc-prolonging activities of Leuprolide.Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Leuprolide.Approved
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Leuprolide.Approved
MethadoneLeuprolide may increase the QTc-prolonging activities of Methadone.Approved
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Leuprolide.Approved
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Leuprolide.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Leuprolide.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Leuprolide.Approved
MirabegronMirabegron may increase the QTc-prolonging activities of Leuprolide.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Leuprolide.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Leuprolide.Approved, Investigational
MoexiprilMoexipril may increase the QTc-prolonging activities of Leuprolide.Approved
MoxifloxacinLeuprolide may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Leuprolide.Approved, Investigational
NelfinavirNelfinavir may increase the QTc-prolonging activities of Leuprolide.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Leuprolide.Approved
NilotinibLeuprolide may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Leuprolide.Approved
NortriptylineNortriptyline may increase the QTc-prolonging activities of Leuprolide.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
OfloxacinLeuprolide may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
OlodaterolOlodaterol may increase the QTc-prolonging activities of Leuprolide.Approved
OndansetronLeuprolide may increase the QTc-prolonging activities of Ondansetron.Approved
OuabainOuabain may decrease the cardiotoxic activities of Leuprolide.Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Leuprolide.Approved, Vet Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Leuprolide.Approved, Vet Approved
PaliperidoneLeuprolide may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatLeuprolide may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
ParoxetineParoxetine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Leuprolide.Approved
PazopanibLeuprolide may increase the QTc-prolonging activities of Pazopanib.Approved
PentamidineLeuprolide may increase the QTc-prolonging activities of Pentamidine.Approved
PerflutrenLeuprolide may increase the QTc-prolonging activities of Perflutren.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Leuprolide.Approved, Withdrawn
PimozideLeuprolide may increase the QTc-prolonging activities of Pimozide.Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Leuprolide.Approved, Investigational
PosaconazolePosaconazole may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational, Vet Approved
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Leuprolide.Approved, Investigational
PrimaquineLeuprolide may increase the QTc-prolonging activities of Primaquine.Approved
ProcainamideLeuprolide may increase the QTc-prolonging activities of Procainamide.Approved
PromazineLeuprolide may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Leuprolide.Approved
PropafenoneLeuprolide may increase the QTc-prolonging activities of Propafenone.Approved
PropofolPropofol may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational, Vet Approved
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Leuprolide.Approved
QuetiapineLeuprolide may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineLeuprolide may increase the QTc-prolonging activities of Quinidine.Approved
QuinineLeuprolide may increase the QTc-prolonging activities of Quinine.Approved
RanolazineRanolazine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Leuprolide.Approved, Investigational
RilpivirineRilpivirine may increase the QTc-prolonging activities of Leuprolide.Approved
RisperidoneRisperidone may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
RitonavirRitonavir may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Leuprolide.Approved, Investigational
SalbutamolSalbutamol may increase the QTc-prolonging activities of Leuprolide.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Leuprolide.Approved
SaquinavirLeuprolide may increase the QTc-prolonging activities of Saquinavir.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Leuprolide.Approved
SertralineSertraline may increase the QTc-prolonging activities of Leuprolide.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Leuprolide.Approved, Vet Approved
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Leuprolide.Approved, Investigational
SolifenacinSolifenacin may increase the QTc-prolonging activities of Leuprolide.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
SotalolLeuprolide may increase the QTc-prolonging activities of Sotalol.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Leuprolide.Approved
SulfisoxazoleLeuprolide may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Leuprolide.Approved, Investigational
SunitinibSunitinib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
TamoxifenTamoxifen may increase the QTc-prolonging activities of Leuprolide.Approved
TelavancinLeuprolide may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinLeuprolide may increase the QTc-prolonging activities of Telithromycin.Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Leuprolide.Approved
TetrabenazineLeuprolide may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Leuprolide.Investigational
ThioridazineLeuprolide may increase the QTc-prolonging activities of Thioridazine.Approved
ThiothixeneThiothixene may increase the QTc-prolonging activities of Leuprolide.Approved
TizanidineTizanidine may increase the QTc-prolonging activities of Leuprolide.Approved
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Leuprolide.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Leuprolide.Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
ToremifeneLeuprolide may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Leuprolide.Approved, Investigational
TrazodoneTrazodone may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Leuprolide.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Leuprolide.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Leuprolide.Approved, Vet Approved
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Leuprolide.Withdrawn
VandetanibLeuprolide may increase the QTc-prolonging activities of Vandetanib.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Leuprolide.Approved
VemurafenibLeuprolide may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Leuprolide.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Leuprolide.Approved
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Leuprolide.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Leuprolide.Approved, Investigational
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
ZiprasidoneLeuprolide may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolLeuprolide may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Daniel Kadzimirzs, Gerhard Jas, Volker Autze, “Solution-Phase Synthesis of Leuprolide and Its Intermediates.” U.S. Patent US20090005535, issued January 01, 2009.

US20090005535
General References
  1. 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:15568711 ]
  2. 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:15780490 ]
  3. Doraiswamy PM, Xiong GL: Pharmacological strategies for the prevention of Alzheimer's disease. Expert Opin Pharmacother. 2006 Jan;7(1):1-10. [PubMed:16370917 ]
  4. Link [Link]
  5. RxMed [Link]
External Links
ATC CodesL02AE02
AHFS Codes
  • 10:00.00
PDB Entries
FDA labelDownload (477 KB)
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Kit
Injection, powder, for suspension, extended releaseSubcutaneous28.2 mg
Injection, powder, for suspension, extended releaseSubcutaneous35.8 mg
Injection, powder, for suspension, extended releaseSubcutaneous58.2 mg
Injection, powder, for suspension, extended releaseSubcutaneous10.2 mg
Injection, solutionSubcutaneous1 mg/.2mL
KitSubcutaneous
Kit
LiquidSubcutaneous5 mg
Injection, powder, for suspension, extended releaseIntramuscular11.25 mg
Injection, powder, for suspension, extended releaseIntramuscular15 mg
Injection, powder, for suspension, extended releaseIntramuscular22.5 mg
Injection, powder, for suspension, extended releaseIntramuscular3.75 mg
Injection, powder, for suspension, extended releaseIntramuscular30 mg
Injection, powder, for suspension, extended releaseIntramuscular7.5 mg
Injection, powder, for suspension, extended release; kitIntramuscular5.06 mg
Prices
Unit descriptionCostUnit
Eligard 45 mg syringe2959.2USD syringe
Eligard 30 mg syringe1972.8USD syringe
Eligard 22.5 mg syringe1479.6USD syringe
Lupron 2-wk 1 mg/0.2 ml kit594.37USD kit
Eligard 7.5 mg syringe493.2USD syringe
Leuprolide Acetate 1 mg/0.2ml Kit 2.8ml 2-Week Kit400.74USD box
Leuprolide 2wk 1 mg/0.2 ml kit385.33USD kit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5728396 No1997-01-302017-01-30Us
US5932547 No1997-06-132017-06-13Us
US5985305 No1997-01-302017-01-30Us
US6036976 No1996-12-132016-12-13Us
US6113938 No1998-07-242018-07-24Us
US6124261 No1997-06-132017-06-13Us
US6132420 No1997-01-302017-01-30Us
US6156331 No1997-01-302017-01-30Us
US6235712 No1997-06-132017-06-13Us
US6375978 No1998-12-172018-12-17Us
US6395292 No1997-01-302017-01-30Us
US6565874 No1998-10-282018-10-28Us
US6626870 No2000-03-272020-03-27Us
US6773714 No1998-10-282018-10-28Us
US7429559 No1999-01-132019-01-13Us
US8815801 No2002-06-282022-06-28Us
US8921326 No2011-02-052031-02-05Us
US9283282 No1998-10-282018-10-28Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
hydrophobicity0.1Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Peptide binding
Specific Function:
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
Gene Name:
GNRHR
Uniprot ID:
P30968
Molecular Weight:
37730.355 Da
References
  1. Castellon E, Clementi M, Hitschfeld C, Sanchez C, Benitez D, Saenz L, Contreras H, Huidobro C: Effect of leuprolide and cetrorelix on cell growth, apoptosis, and GnRH receptor expression in primary cell cultures from human prostate carcinoma. Cancer Invest. 2006 Apr-May;24(3):261-8. [PubMed:16809153 ]
  2. Borroni R, Di Blasio AM, Gaffuri B, Santorsola R, Busacca M, Vigano P, Vignali M: Expression of GnRH receptor gene in human ectopic endometrial cells and inhibition of their proliferation by leuprolide acetate. Mol Cell Endocrinol. 2000 Jan 25;159(1-2):37-43. [PubMed:10687850 ]
  3. Imai A, Takagi A, Horibe S, Takagi H, Tamaya T: Fas and Fas ligand system may mediate antiproliferative activity of gonadotropin-releasing hormone receptor in endometrial cancer cells. Int J Oncol. 1998 Jul;13(1):97-100. [PubMed:9625809 ]
  4. Murase M, Uemura T, Gao M, Inada M, Funabashi T, Hirahara F: GnRH antagonist-induced down-regulation of the mRNA expression of pituitary receptors: comparisons with GnRH agonist effects. Endocr J. 2005 Feb;52(1):131-7. [PubMed:15758569 ]
  5. Khurana KK, Singh SB, Tatum AH, Schulz V, Badawy SZ: Maintenance of increased Bcl-2 expression in uterine leiomyomas after GnRH agonist therapy. J Reprod Med. 1999 Jun;44(6):487-92. [PubMed:10394541 ]
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Drug created on June 13, 2005 07:24 / Updated on December 09, 2016 03:14