Identification

Name
Leuprolide
Accession Number
DB00007  (BTD00009, BIOD00009)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
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.

Protein structure
Db00007
Protein chemical formula
C59H84N16O12
Protein average weight
1209.3983 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
Product Ingredients
IngredientUNIICASInChI Key
Leuprolide acetate37JNS02E7V74381-53-6RGLRXNKKBLIBQS-XNHQSDQCSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EligardKitSanofi Aventis2002-01-232016-10-13Us
EligardKitSubcutaneousTolmar Inc2003-02-26Not applicableUs
EligardKitSubcutaneousTolmar Inc2002-08-26Not applicableUs
EligardKitSanofi Aventis2002-01-232016-10-13Us
EligardKitSubcutaneousTolmar Inc2005-01-07Not applicableUs
EligardKitSubcutaneousTolmar Inc2003-02-26Not applicableUs
EligardKitSubcutaneousTolmar Inc2002-05-15Not applicableUs
EligardKitSanofi Aventis2002-01-232016-10-13Us
EligardKitSubcutaneousTolmar Inc2005-01-07Not applicableUs
EligardKitSubcutaneousTolmar Inc2002-08-26Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Leuprolide AcetateKitTeva Parenteral Medicines, Inc.2000-11-062016-12-16Us
Leuprolide AcetateKitSun Pharma Global FZE2014-12-15Not applicableUs
Leuprolide AcetateKitSandoz1998-08-04Not applicableUs
Leuprolide AcetateKitSubcutaneousSun Pharma Global Inc.2009-03-032017-09-05Us
Leuprolide AcetateInjection, solution1 mg/.2mLSubcutaneousEon Labs, Inc.1998-08-04Not applicableUs
International/Other Brands
Enantone / Leuplin (Takeda) / LeuProMaxx (Baxter/Teva) / Leupromer / Lutrate / Memryte (Curaxis) / Prostap 3 (Takeda UK) / Prostap SR (Takeda UK) / Viadur (Bayer AG)
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Lupaneta PackLeuprolide acetate + Norethisterone acetateKitAbbvie2013-07-01Not applicableUs
Lupaneta PackLeuprolide acetate + Norethisterone acetateKitAbbvie2013-07-01Not applicableUs
Categories
UNII
EFY6W0M8TG
CAS number
53714-56-0

Pharmacology

Indication

For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty

Structured Indications
Pharmacodynamics

Used 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 action

Leuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.

TargetActionsOrganism
AGonadotropin-releasing hormone receptor
agonist
Human
Absorption

Bioavailability by subcutaneous administration is comparable to that by intravenous administration.

Volume of distribution
  • 27 L [intravenous bolus administration to healthy male volunteers]
Protein binding

43% to 49%

Metabolism

Primarily degraded by peptidase and not by cytochrome P450 enzymes.

Route of elimination

Excretion in urine

Half life

~3 hours

Clearance
  • 8.34 L/h [healthy male receiving a 1-mg IV bolus]
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.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Leuprolide.Investigational
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.Investigational, Withdrawn
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Leuprolide.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Leuprolide.Experimental
AICA ribonucleotideThe therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Leuprolide.Experimental, Investigational
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
AllicinThe therapeutic efficacy of Allicin can be decreased when used in combination with Leuprolide.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
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
Bempedoic acidThe therapeutic efficacy of Bempedoic acid can be decreased when used in combination with Leuprolide.Investigational
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.Investigational, 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
Capromab pendetideLeuprolide may decrease effectiveness of Capromab pendetide as a diagnostic agent.Approved
CarbutamideThe therapeutic efficacy of Carbutamide can be decreased when used in combination with Leuprolide.Experimental
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, Investigational
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
CymarinCymarin may decrease the cardiotoxic activities of Leuprolide.Experimental
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, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Leuprolide.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) 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
GitoformateGitoformate may decrease the cardiotoxic activities of Leuprolide.Experimental
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Leuprolide.Investigational, 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, Investigational
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 HumanThe therapeutic efficacy of Insulin Human can be decreased when used in combination with Leuprolide.Approved, Investigational
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
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Leuprolide.Experimental
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
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Leuprolide.Experimental
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
OleandrinOleandrin may decrease the cardiotoxic activities of Leuprolide.Experimental, 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
PeruvosidePeruvoside may decrease the cardiotoxic activities of Leuprolide.Experimental
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Leuprolide.Approved, Investigational, 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
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Leuprolide.Experimental
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
SotagliflozinThe therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Leuprolide.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
ThioridazineLeuprolide may increase the QTc-prolonging activities of Thioridazine.Approved, Withdrawn
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.Investigational, 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 Interactions
Not 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
KEGG Drug
D08113
KEGG Compound
C07612
PubChem Substance
46507635
ChEBI
6427
ChEMBL
CHEMBL1201199
Therapeutic Targets Database
DAP000020
PharmGKB
PA450203
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Leuprolide
ATC Codes
L02AE02 — Leuprorelin
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (477 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic SciencePuberty, Delayed / Puberty, Precocious1
0WithdrawnBasic ScienceHigh Blood Pressure (Hypertension)1
1Active Not RecruitingTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
1Active Not RecruitingTreatmentProstate Cancer1
1CompletedBasic ScienceBMI >30 kg/m21
1CompletedBasic ScienceThere Are no Conditions Under Study. Healthy Volunteers1
1CompletedTreatmentProstate Cancer3
1Not Yet RecruitingTreatmentProstate Cancer1
1TerminatedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer1
1, 2Active Not RecruitingTreatmentAdenocarcinoma, Prostate / Stage IIA Prostate Cancer / Stage IIA Prostate Cancer AJCC v7 / Stage IIB Prostate Cancer / Stage IIB Prostate Cancer AJCC v71
1, 2Active Not RecruitingTreatmentProstate Cancer1
1, 2CompletedTreatmentProstate Cancer3
1, 2CompletedTreatmentProstatic Neoplasms1
1, 2Not Yet RecruitingTreatmentPremenopausal Breast Cancer1
1, 2RecruitingTreatmentAdenocarcinoma, Prostate / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
1, 2TerminatedTreatmentProstate Cancer1
1, 2TerminatedTreatmentProstate Cancer / Prostatic Neoplasms1
2Active Not RecruitingSupportive CareHodgkins Disease (HD) / Leukemia Acute Myeloid Leukemia (AML) / Multiple Myeloma (MM) / Myeloproliferative Disorders / Non-Hodgkin's Lymphoma (NHL)1
2Active Not RecruitingTreatmentAcute Lymphocytic Leukemia (ALL) / Acute Myelogenous Leukaemia (AML) / Myelodysplastic Syndrome RAEB 1 / Myelodysplastic Syndrome RAEB 21
2Active Not RecruitingTreatmentAdenocarcinoma, Prostate / High Risk Prostate Cancer / Prostate Cancer1
2Active Not RecruitingTreatmentAdenocarcinoma, Prostate / Recurrent Prostate Carcinoma / Stage IV Prostate Cancer1
2Active Not RecruitingTreatmentFibrolamellar Carcinoma / Fibrolamellar Liver Cancer1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentProstate Cancer10
2CompletedPreventionMelanoma1
2CompletedTreatmentAcanthosis Nigricans / Polycystic Ovaries Syndrome1
2CompletedTreatmentAdenocarcinoma of the Prostate / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2CompletedTreatmentAdenocarcinoma, Prostate / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
2CompletedTreatmentAlzheimer's Disease (AD)2
2CompletedTreatmentAmenorrhea / Ovarian Function Insufficiency / Premature Ovarian Failure (POF)1
2CompletedTreatmentAmyotrophic Lateral Sclerosis (ALS) / Spinal Muscular Atrophy (SMA) / Spinobulbar Muscular Atrophy1
2CompletedTreatmentCancer, Breast1
2CompletedTreatmentCancers / Hormonal Cycling / Prostate1
2CompletedTreatmentContraception / Hypogonadism1
2CompletedTreatmentEndometriosis4
2CompletedTreatmentHyperandrogenism1
2CompletedTreatmentInsulin Resistance / One to five years postmenopausal1
2CompletedTreatmentMetastatic Cancers / Prostate Cancer1
2CompletedTreatmentProstate Cancer17
2CompletedTreatmentProstate Cancer / Prostatic Adenocarcinoma / Prostatic Neoplasms1
2CompletedTreatmentProstatic Neoplasms1
2CompletedTreatmentRecurrent Prostate Cancer2
2CompletedTreatmentUterine Leiomyomas1
2Not Yet RecruitingTreatmentNewly Diagnosed Oligometastatic Prostate Cancer1
2Not Yet RecruitingTreatmentProstate Cancer1
2RecruitingNot AvailableEndometriosis1
2RecruitingSupportive CareAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2RecruitingTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
2RecruitingTreatmentCancers / Prostate Cancer1
2RecruitingTreatmentCastration-Resistant Prostate Cancer (CRPC) / Prostate Cancer1
2RecruitingTreatmentEndometriosis1
2RecruitingTreatmentLeukemias / Multiple Myeloma (MM) / Myelodysplastic Syndrome / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2RecruitingTreatmentNeoplasms, Breast2
2RecruitingTreatmentPelvic Nodal / Prostatic Neoplasms1
2RecruitingTreatmentProstate Cancer8
2TerminatedPreventionUterine Leiomyomas1
2TerminatedTreatmentAdenocarcinoma, Prostate / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2TerminatedTreatmentCancer, Breast1
2TerminatedTreatmentHodgkins Disease (HD) / Mantle Cell Lymphoma (MCL) / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2TerminatedTreatmentProstate Cancer3
2TerminatedTreatmentProstatic Neoplasms1
2Unknown StatusTreatmentProstate Cancer2
2Unknown StatusTreatmentProstatic Neoplasms1
2WithdrawnNot AvailableProstate Cancer1
2WithdrawnTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2WithdrawnTreatmentProstate Cancer2
2, 3RecruitingTreatmentCastration-resistant Prostate Cancer Patients With Oligometastases1
2, 3RecruitingTreatmentStage I Prostate Adenocarcinoma / Stage II Prostate Adenocarcinoma / Stage III Prostate Adenocarcinoma1
2, 3Unknown StatusNot AvailableMenopausal Hot Flushes1
2, 3Unknown StatusTreatmentPedophilia1
3Active Not RecruitingTreatmentGastrointestinal Complications / Prostate Cancer / Sexual Dysfunctions / Urinary Complications1
3Active Not RecruitingTreatmentPrecocious Puberty, Central1
3Active Not RecruitingTreatmentProstate Cancer3
3Active Not RecruitingTreatmentUterine Leiomyomas1
3CompletedTreatmentAdenocarcinoma, Prostate1
3CompletedTreatmentBMI >30 kg/m21
3CompletedTreatmentCancer, Breast2
3CompletedTreatmentCancers / Fertility Preservation1
3CompletedTreatmentCentral Precocious Puberty (CPP) / Depot Formulation / GnRH Analog / Gonadotrophin-releasing Hormone (GnRH) / Gonadotrophin-releasing Hormone Agonist (GnRHa) / Leuprolide Acetate / Lupron / Luteinizing Hormone (LH) / Pediatrics Central Precocious Puberty / Precocious / Suppression of LH / Tanner Staging1
3CompletedTreatmentIdiopathic Short Stature (ISS)1
3CompletedTreatmentMalignant Neoplasm of Female Breast1
3CompletedTreatmentProstate Cancer15
3CompletedTreatmentPuberty, Precocious2
3CompletedTreatmentUterine Leiomyomas1
3Not Yet RecruitingTreatmentUterine Leiomyomas1
3RecruitingTreatmentCancer of the Prostate / Hormone Sensitive Prostate Cancer / Prostate Cancer1
3RecruitingTreatmentCancer, Breast1
3RecruitingTreatmentMetastases1
3RecruitingTreatmentProstate Cancer2
3TerminatedSupportive CareProstate Cancer1
3TerminatedTreatmentIsolated Angiitis of Central Nervous System / Lung Disease Interstitial Diffuse / Lung Disease With Systemic Sclerosis / Lupus Erythematosus, Systemic / Systemic Vasculitis1
3TerminatedTreatmentPedophilia1
3TerminatedTreatmentProstate Cancer4
3TerminatedTreatmentProstatic Neoplasms1
3Unknown StatusTreatmentDysmenorrhea / Endometriosis / Painful Intercourse1
3Unknown StatusTreatmentInfertilities1
3Unknown StatusTreatmentProstate Cancer1
4Active Not RecruitingBasic ScienceContraception / Fertility1
4Active Not RecruitingTreatmentPuberty, Precocious1
4CompletedNot AvailableEffect of Two Protocols of Ovarian Stimulation on Oocyte Quality1
4CompletedNot AvailableEndometriosis1
4CompletedNot AvailableProstate Cancer1
4CompletedPreventionOvarian Hyperstimulation Syndrome1
4CompletedTreatmentCentral Precocious Puberty (CPP)2
4CompletedTreatmentEndometriosis / Infertilities1
4CompletedTreatmentInfertilities / Polycystic Ovarian Syndrome1
4CompletedTreatmentProstate Cancer3
4Not Yet RecruitingBasic ScienceMenopause1
4Not Yet RecruitingTreatmentAmenorrhea / Endometriosis / Quality of Life1
4RecruitingTreatmentAbortions spontaneous / Egg Retrieval / IVF Cycle / Ovarian Hyperstimulation / Ovarian Stimulation / Pregnancy1
4RecruitingTreatmentEgg Donation1
4RecruitingTreatmentLeiomyomas3
4RecruitingTreatmentPrecocious Puberty, Central1
4RecruitingTreatmentProstate Cancer1
4TerminatedOtherMetastatic Hormone Refractory Prostate Cancer1
4TerminatedTreatmentObstructive Sleep Apnea (OSA) / Polycystic Ovaries Syndrome1
4TerminatedTreatmentProstate Cancer1
4Unknown StatusPreventionCentral Precocious Puberty (CPP)1
4WithdrawnTreatmentInfertilities1
Not AvailableActive Not RecruitingOtherLuteal Phase Defect1
Not AvailableCompletedNot AvailableAdvanced Prostate Carcinoma1
Not AvailableCompletedNot AvailableBMI >30 kg/m21
Not AvailableCompletedNot AvailableCancer, Breast2
Not AvailableCompletedNot AvailableProstate Cancer3
Not AvailableCompletedNot AvailableProstatic Neoplasms1
Not AvailableCompletedBasic ScienceBMI >30 kg/m21
Not AvailableCompletedBasic ScienceCardiovascular Disease (CVD) / Cognitive Impairments / Endothelial Dysfunction / Executive Dysfunction1
Not AvailableCompletedBasic ScienceCoronary Heart Disease (CHD)1
Not AvailableCompletedBasic SciencePostpartum Depression1
Not AvailableCompletedScreeningPuberty, Precocious1
Not AvailableCompletedTreatmentEndometriosis / Infertilities1
Not AvailableCompletedTreatmentFertility1
Not AvailableCompletedTreatmentHemangiomas1
Not AvailableCompletedTreatmentHypogonadism2
Not AvailableCompletedTreatmentNatural Cycle in Vitro Fertilization (IVF)1
Not AvailableCompletedTreatmentProstate Cancer1
Not AvailableCompletedTreatmentProstatic Neoplasms1
Not AvailableNot Yet RecruitingNot AvailableProstate Cancer1
Not AvailableNot Yet RecruitingBasic ScienceBMI >30 kg/m2 / Hyperandrogenemia / Polycystic Ovaries Syndrome1
Not AvailableRecruitingNot AvailablePremenopausal Breast Cancer1
Not AvailableRecruitingNot AvailableProstate Cancer1
Not AvailableRecruitingNot AvailablePuberty, Precocious1
Not AvailableRecruitingBasic ScienceBMI >30 kg/m2 / Menopause1
Not AvailableRecruitingTreatmentAdenocarcinoma of the Prostate1
Not AvailableUnknown StatusBasic ScienceDepression / Menopausal Hot Flushes / Menopause1
Not AvailableUnknown StatusDiagnosticEndometrial Receptivity / Ovarian Hyperstimulation Syndrome1
Not AvailableUnknown StatusTreatmentImplantation, Embryo1
Not AvailableUnknown StatusTreatmentInfertilities2
Not AvailableWithdrawnOtherHigh Blood Pressure (Hypertension)1

Pharmacoeconomics

Manufacturers
Not 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; kitIntramuscular28.13 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)
US6036976No1996-12-132016-12-13Us
US8921326No2011-02-052031-02-05Us
US7429559No1999-01-132019-01-13Us
US8815801No2002-06-282022-06-28Us
US5728396No1997-01-302017-01-30Us
US6156331No1997-01-302017-01-30Us
US6375978No1998-12-172018-12-17Us
US6235712No1997-06-132017-06-13Us
US6113938No1998-07-242018-07-24Us
US6124261No1997-06-132017-06-13Us
US6395292No1997-01-302017-01-30Us
US6132420No1997-01-302017-01-30Us
US5985305No1997-01-302017-01-30Us
US5932547No1997-06-132017-06-13Us
US6565874No1998-10-282018-10-28Us
US6773714No1998-10-282018-10-28Us
US6626870No2000-03-272020-03-27Us
US9283282No1998-10-282018-10-28Us
US9254307No1998-10-282018-10-28Us
US8486455No1998-10-282018-10-28Us
US8840916No2000-11-132020-11-13Us
US8470359No2003-10-152023-10-15Us
US9539333No2000-11-132020-11-13Us

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity0.1Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not 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...
Gene Name
GNRHR
Uniprot ID
P30968
Uniprot Name
Gonadotropin-releasing hormone receptor
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]

Drug created on June 13, 2005 07:24 / Updated on December 04, 2017 13:13