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
EligardKit7.5 mg/0.25mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-05-15Not applicableUs
EligardKit22.5 mg/0.375mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-08-26Not applicableUs
EligardKit22.5 mg/0.375mLSanofi Aventis2002-01-232016-05-31Us
EligardKit30 mg/0.5mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2003-02-26Not applicableUs
EligardKit45 mg/0.375mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2005-01-07Not applicableUs
EligardKit45 mg/0.375mLSanofi Aventis2002-01-232016-05-31Us
EligardKit7.5 mg/0.25mLSanofi Aventis2002-01-232016-05-31Us
EligardKit7.5 mg/0.25mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-05-15Not applicableUs
EligardKit22.5 mg/0.375mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-08-26Not applicableUs
EligardKit30 mg/0.5mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2003-02-26Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Leuprolide AcetateInjection, solution1 mg/.2mLSubcutaneousEon Labs, Inc.1998-08-04Not applicableUs
Leuprolide AcetateKit1 mg/0.2mLTeva Parenteral Medicines, Inc.2000-11-062011-03-31Us
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Leuprolide AcetateLeuprolide acetate (1 mg/0.2mL) + Isopropyl Alcohol (0.7 mL/1mL)KitSandoz1998-08-04Not applicableUs
Leuprolide AcetateLeuprolide acetate (5 mg/1mL) + Isopropyl Alcohol (0.7 mL/1mL)KitSun Pharmaceutical Industries, Inc.2014-12-15Not applicableUs
Leuprolide AcetateLeuprolide acetate (5 mg/1mL) + Isopropyl Alcohol (0.7 mL/1mL)KitSun Pharma Global Inc.2014-12-152015-08-31Us
Leuprolide AcetateLeuprolide acetate + Isopropyl AlcoholKitGenzyme Corporation2006-05-312006-05-31Us
Leuprolide AcetateLeuprolide acetate (1 mg/0.2mL) + Isopropyl Alcohol (0.7 mL/1)KitGenzyme Corporation2001-11-292010-03-31Us
Lupaneta PackLeuprolide acetate (11.25 mg/1.5mL) + Isopropyl Alcohol (0.7 mL/1mL) + Norethisterone acetate (5 mg/1)KitAbbvie2013-07-01Not applicableUs
Lupaneta PackLeuprolide acetate (3.75 mg/1mL) + Ethanol (0.7 mL/1mL) + Norethisterone acetate (5 mg/1)KitAbbvie2013-07-01Not applicableUs
Lupron DepotLeuprolide acetate (3.75 mg/1mL) + Isopropyl Alcohol (0.7 mL/1mL)KitAbbvie1990-10-22Not applicableUs
ViadurLeuprolide acetate (72 mg/1) + Lidocaine hydrochloride (20 mg/1mL)KitBayer Pharmaceuticals Corporation2006-05-10Not 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)
Categories
UNII
EFY6W0M8TG
CAS number
53714-56-0

Pharmacology

Indication

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

Associated Conditions
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
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Leuprolide.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Leuprolide.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Leuprolide.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Leuprolide.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Leuprolide.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Leuprolide.
6-Deoxyerythronolide BThe metabolism of Leuprolide can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Leuprolide.
AbacavirLeuprolide may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Leuprolide.
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 ScienceBMI >30 kg/m2 / Hyperandrogenemia / Polycystic Ovaries Syndrome1
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 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, 2TerminatedTreatmentAdenocarcinoma, Prostate / Stage IIA Prostate Cancer / Stage IIA Prostate Cancer AJCC v7 / Stage IIB Prostate Cancer / Stage IIB Prostate Cancer AJCC v71
1, 2TerminatedTreatmentProstate Cancer1
1, 2TerminatedTreatmentProstate Cancer / Prostatic Neoplasms1
2Active Not RecruitingNot AvailableEndometriosis1
2Active Not RecruitingTreatmentAcute Lymphocytic Leukemia (ALL) / Acute Myelogenous Leukaemia (AML) / Myelodysplastic Syndrome RAEB 1 / Myelodysplastic Syndrome RAEB 21
2Active Not RecruitingTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
2Active Not RecruitingTreatmentAdenocarcinoma, Prostate / High Risk Prostate Cancer / Prostate Cancer1
2Active Not RecruitingTreatmentAdenocarcinoma, Prostate / Prostate Cancer / PSA Level Greater Than or Equal to 0.2 / PSA Progression / Recurrent Prostate Carcinoma1
2Active Not RecruitingTreatmentFibrolamellar Carcinoma / Fibrolamellar Liver Cancer1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2Active Not RecruitingTreatmentPelvic Nodal / Prostatic Neoplasms1
2Active Not RecruitingTreatmentProstate Cancer8
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 / Recurrent Prostate Carcinoma / 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
2CompletedTreatmentContraception / Hypogonadism1
2CompletedTreatmentEndometriosis5
2CompletedTreatmentHormonal Cycling / Malignancies / Prostate1
2CompletedTreatmentHyperandrogenism1
2CompletedTreatmentInsulin Resistance / One to five years postmenopausal1
2CompletedTreatmentMetastatic Cancers / Prostate Cancer1
2CompletedTreatmentProstate Cancer19
2CompletedTreatmentProstate Cancer / Prostatic Adenocarcinoma / Prostatic Neoplasms1
2CompletedTreatmentProstatic Neoplasms1
2CompletedTreatmentRecurrent Prostate Cancer2
2CompletedTreatmentUterine Leiomyomas1
2Not Yet RecruitingTreatmentAlzheimer's Disease (AD)1
2Not Yet RecruitingTreatmentProstate Cancer2
2RecruitingSupportive CareAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2RecruitingTreatmentAdenocarcinoma, Prostate1
2RecruitingTreatmentBreast Cancer Invasive Nos / Cancer, Breast1
2RecruitingTreatmentCastration-Resistant Prostate Cancer (CRPC) / Prostate Cancer1
2RecruitingTreatmentHigh-risk Prostate Cancer / Prostate Cancer1
2RecruitingTreatmentLeukemias / Multiple Myeloma (MM) / Myelodysplastic Syndrome / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2RecruitingTreatmentNeoplasms, Breast1
2RecruitingTreatmentNewly Diagnosed Oligometastatic Prostate Cancer1
2RecruitingTreatmentProstate Cancer7
2RecruitingTreatmentProstate Cancer / Prostate Neoplasms / Prostatic Neoplasms1
2RecruitingTreatmentProstatic Neoplasms1
2SuspendedSupportive CareAdenocarcinoma, Prostate / Malignancies / Prostate Cancer1
2TerminatedPreventionUterine Leiomyomas1
2TerminatedSupportive CareHodgkins Disease (HD) / Leukemia Acute Myeloid Leukemia (AML) / Multiple Myeloma (MM) / Myeloproliferative Disorders / Non-Hodgkin's Lymphoma (NHL)1
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 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 StatusTreatmentPedophilia1
3Active Not RecruitingTreatmentCancer of the Prostate / Hormone Sensitive Prostate Cancer / Prostate Cancer1
3Active Not RecruitingTreatmentGastrointestinal Complications / Prostate Cancer / Sexual Dysfunctions / Urinary Complications1
3Active Not RecruitingTreatmentMetastases1
3Active Not RecruitingTreatmentProstate Cancer4
3Active Not RecruitingTreatmentUterine Leiomyomas1
3CompletedTreatmentAdenocarcinoma, Prostate1
3CompletedTreatmentBMI >30 kg/m21
3CompletedTreatmentCancer, Breast2
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
3CompletedTreatmentFertility Preservation / Malignancies1
3CompletedTreatmentIdiopathic Short Stature (ISS)1
3CompletedTreatmentMalignant Neoplasm of Female Breast1
3CompletedTreatmentPrecocious Puberty, Central1
3CompletedTreatmentProstate Cancer15
3CompletedTreatmentPuberty, Precocious2
3CompletedTreatmentUterine Leiomyomas1
3Not Yet RecruitingTreatmentInfertilities / Infertility, Female / Male Infertility1
3RecruitingTreatmentCancer, Breast1
3RecruitingTreatmentCastration Levels of Testosterone / Metastatic Prostatic Adenocarcinoma / Stage IV Prostate Cancer AJCC v8 / Stage IVA Prostate Cancer AJCC v8 / Stage IVB Prostate Cancer AJCC v81
3RecruitingTreatmentCentral Precocious Puberty (CPP)1
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
3WithdrawnTreatmentUterine Leiomyomas1
4Active Not RecruitingTreatmentProstate Cancer1
4Active Not RecruitingTreatmentPuberty, Precocious1
4CompletedNot AvailableEffect of Two Protocols of Ovarian Stimulation on Oocyte Quality1
4CompletedNot AvailableEndometriosis1
4CompletedNot AvailableProstate Cancer1
4CompletedBasic ScienceContraception / Fertility1
4CompletedBasic ScienceDepression / Menopausal Hot Flushes / Menopause1
4CompletedBasic ScienceMenopausal Hot Flushes1
4CompletedPreventionOvarian Hyperstimulation Syndrome1
4CompletedTreatmentCentral Precocious Puberty (CPP)2
4CompletedTreatmentEgg Donation1
4CompletedTreatmentEndometriosis / Infertilities1
4CompletedTreatmentInfertilities / Polycystic Ovarian Syndrome1
4CompletedTreatmentProstate Cancer3
4Not Yet RecruitingTreatmentAmenorrhea / Endometriosis / Quality of Life1
4Not Yet RecruitingTreatmentInvitro Fertilization1
4RecruitingBasic ScienceMenopause1
4RecruitingTreatmentAbortions spontaneous / Egg Retrieval / IVF Cycle / Ovarian Hyperstimulation / Ovarian Stimulation / Pregnancy1
4RecruitingTreatmentLeiomyomas3
4RecruitingTreatmentPrecocious Puberty, Central1
4TerminatedOtherMetastatic Hormone Refractory Prostate Cancer1
4TerminatedTreatmentObstructive Sleep Apnea (OSA) / Polycystic Ovaries Syndrome1
4TerminatedTreatmentProstate Cancer1
4Unknown StatusPreventionCentral Precocious Puberty (CPP)1
4WithdrawnTreatmentInfertilities1
Not AvailableCompletedNot AvailableAdvanced Prostate Carcinoma1
Not AvailableCompletedNot AvailableBMI >30 kg/m21
Not AvailableCompletedNot AvailableCancer, Breast2
Not AvailableCompletedNot AvailablePremenopausal Breast Cancer1
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 AvailableCompletedTreatmentProstate Cancer1
Not AvailableCompletedTreatmentProstatic Neoplasms1
Not AvailableNot Yet RecruitingNot AvailableProstate Cancer1
Not AvailableRecruitingNot AvailableProstate Cancer2
Not AvailableRecruitingNot AvailablePuberty, Precocious1
Not AvailableRecruitingNot AvailableSpinal and Bulbar Muscular Atrophy1
Not AvailableRecruitingBasic ScienceBMI >30 kg/m2 / Menopause1
Not AvailableRecruitingTreatmentAdenocarcinoma of the Prostate1
Not AvailableRecruitingTreatmentProstate Cancer1
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
  • Abbott Laboratories Ltd.
  • Cardinal Health
  • Eon Labs
  • Hospira Inc.
  • Oso Biopharmaceuticals Manufacturing LLC
  • Physicians Total Care Inc.
  • Sanofi-Aventis Inc.
  • Sun Pharmaceutical Industries Ltd.
  • Takeda Pharmaceutical Co. Ltd.
  • Teva Pharmaceutical Industries Ltd.
  • Tolmar Inc.
Dosage forms
FormRouteStrength
Kit22.5 mg/0.375mL
Kit30 mg/0.5mL
Kit45 mg/0.375mL
Kit7.5 mg/0.25mL
KitSubcutaneous22.5 mg/0.375mL
KitSubcutaneous30 mg/0.5mL
KitSubcutaneous45 mg/0.375mL
KitSubcutaneous7.5 mg/0.25mL
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
Kit1 mg/0.2mL
LiquidSubcutaneous5 mg
Injection, solutionSubcutaneous5 mg/1mL
Kit5 mg/1mL
SolutionSubcutaneous5 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, lyophilized, for suspensionIntramuscular3.75 mg/1mL
Injection, powder, lyophilized, for suspensionIntramuscular30 mg/1.5mL
Kit22.5 mg/1.5mL
Kit3.75 mg/1mL
Kit30 mg/1.5mL
Kit45 mg/1.5mL
Kit7.5 mg/1mL
Injection, powder, lyophilized, for suspensionIntramuscular11.25 mg/1mL
Injection, powder, lyophilized, for suspensionIntramuscular15 mg/1mL
Injection, powder, lyophilized, for suspensionIntramuscular7.5 mg/1mL
Kit11.25 mg/1.5mL
Kit11.25 mg/1mL
Kit15 mg/1mL
Kit
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
US9914802No2000-11-132020-11-13Us

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]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Hutson PR, Oettel K, Douglas J, Ritter M, Messing E, Staab MJ, Alberti D, Horvath D, Wilding G: Effect of medical castration on CYP3A4 enzyme activity using the erythromycin breath test. Cancer Chemother Pharmacol. 2008 Aug;62(3):373-7. doi: 10.1007/s00280-007-0613-6. Epub 2007 Oct 9. [PubMed:17922273]

Drug created on June 13, 2005 07:24 / Updated on November 12, 2018 07:11