Identification

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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
  • Leuprorelin
  • Leuprorelina
  • Leuproreline
  • Leuprorelinum
External IDs
CKD-841
Product Ingredients
IngredientUNIICASInChI Key
Leuprolide acetate37JNS02E7V74381-53-6RGLRXNKKBLIBQS-XNHQSDQCSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EligardKit30 mg/0.5mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2003-02-26Not applicableUs
EligardKit30 mg/0.5mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-01-232015-05-08Us
EligardInjection, powder, for suspension, extended release30 mgSubcutaneousSanofi Aventis2004-04-29Not applicableCanada
EligardKit45 mg/0.375mLSubcutaneousSanofi Aventis2002-01-232016-05-31Us
EligardKit22.5 mg/0.375mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-08-26Not applicableUs
EligardKit22.5 mg/0.375mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-01-232015-05-08Us
EligardInjection, powder, for suspension, extended release22.5 mgSubcutaneousSanofi Aventis2003-12-01Not applicableCanada
EligardKit30 mg/0.5mLSubcutaneousSanofi Aventis2002-01-232016-05-31Us
EligardKit7.5 mg/0.25mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-05-15Not applicableUs
EligardKit7.5 mg/0.25mLSubcutaneousTOLMAR PHARMACEUTICALS INC.2002-01-232015-05-08Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Leuprolide AcetateKit1 mg/0.2mLTopicalTeva Parenteral Medicines, Inc.2000-11-062011-03-31Us
Leuprolide AcetateInjection, solution1 mg/.2mLSubcutaneousEon Labs, Inc.1998-08-04Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Leuprolide AcetateLeuprolide acetate + Isopropyl alcoholKitTopicalGenzyme Corporation2006-05-312006-05-31Us
Leuprolide AcetateLeuprolide acetate (5 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL)KitTopicalSun Pharma Global Inc.2014-12-152015-08-31Us
Leuprolide AcetateLeuprolide acetate (1 mg/0.2mL) + Isopropyl alcohol (0.7 mL/1)KitTopicalGenzyme Corporation2001-11-292010-03-31Us
Leuprolide AcetateLeuprolide acetate (1 mg/0.2mL) + Isopropyl alcohol (0.7 mL/1mL)KitTopicalSandoz Inc1998-08-04Not applicableUs
Leuprolide AcetateLeuprolide acetate (5 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL)KitTopicalSun Pharmaceutical Industries, Inc.2014-12-15Not applicableUs
Lupaneta PackLeuprolide acetate (3.75 mg/1mL) + Ethanol (0.7 mL/1mL) + Norethisterone acetate (5 mg/1)KitTopicalAbbVie Inc.2013-07-01Not applicableUs
Lupaneta PackLeuprolide acetate (11.25 mg/1.5mL) + Isopropyl alcohol (0.7 mL/1mL) + Norethisterone acetate (5 mg/1)KitTopicalAbbVie Inc.2013-07-01Not applicableUs
Lupron DepotLeuprolide acetate (11.25 mg/1.5mL) + Isopropyl alcohol (0.7 mL/1mL)KitTopicalAbbVie Inc.2010-11-08Not applicableUs
Lupron DepotLeuprolide acetate (3.75 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL)KitTopicalAbbVie Inc.1990-10-22Not applicableUs
ViadurLeuprolide acetate (72 mg/1) + Lidocaine hydrochloride (20 mg/1mL)KitTopicalBayer Pharmaceuticals Corporation2006-05-10Not applicableUs
International/Other Brands
Leuplin (Takeda) / LeuProMaxx (Baxter/Teva) / Memryte (Curaxis) / Prostap 3 (Takeda UK) / Prostap SR (Takeda UK)
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
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Leuprolide.
AbacavirLeuprolide may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbexinostatThe risk or severity of QTc prolongation can be increased when Leuprolide is combined with Abexinostat.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Leuprolide.
AcebutololThe risk or severity of QTc prolongation can be increased when Leuprolide is combined with Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Leuprolide which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Leuprolide which could result in a higher serum level.
AceprometazineThe risk or severity of QTc prolongation can be increased when Leuprolide is combined with Aceprometazine.
AcetaminophenLeuprolide may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Leuprolide.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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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
L02AE51 — Leuprorelin and bicalutamideL02AE02 — Leuprorelin
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
  • 68:18.08 — Gonadotropins
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 RecruitingTreatmentMetastatic Hormone Refractory Prostate Cancer / Metastatic Prostatic Adenocarcinoma / Prostate Carcinoma Metastatic to the Bone1
1Active Not RecruitingTreatmentProstate Cancer1
1CompletedBasic ScienceBMI >30 kg/m21
1CompletedBasic ScienceThere Are no Conditions Under Study. Healthy Volunteers1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentPostmenopausal Disorder1
1CompletedTreatmentProstate Cancer3
1Not Yet RecruitingTreatmentProstate Cancer1
1TerminatedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer1
1WithdrawnTreatmentProstatic Neoplasms1
1, 2CompletedTreatmentProstate Cancer4
1, 2CompletedTreatmentProstatic Neoplasms1
1, 2CompletedTreatmentUterine Leiomyomata1
1, 2RecruitingTreatmentAdenocarcinoma, Prostate / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
1, 2RecruitingTreatmentPremenopausal Breast 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 RecruitingSupportive CareAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
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)2
2Active Not RecruitingTreatmentNeoplasms, Breast2
2Active Not RecruitingTreatmentProstate Cancer / PSA Level Greater Than Two / Stage IV Prostate Adenocarcinoma AJCC v71
2Active Not RecruitingTreatmentPelvic Nodal / Prostatic Neoplasms1
2Active Not RecruitingTreatmentProstate Cancer6
2CompletedNot AvailableEndometriosis1
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
2CompletedTreatmentBreast Cancer1
2CompletedTreatmentContraception / Hypogonadism1
2CompletedTreatmentEndometriosis6
2CompletedTreatmentHormonal Cycling / Malignancies / Prostate1
2CompletedTreatmentHyperandrogenism1
2CompletedTreatmentInsulin Resistance / One to five years postmenopausal1
2CompletedTreatmentMalignancies / Prostate Neoplasms1
2CompletedTreatmentMetastatic Cancers / Prostate Cancer1
2CompletedTreatmentProstate Cancer23
2CompletedTreatmentProstate Cancer / Prostatic Adenocarcinoma / Prostatic Neoplasms1
2CompletedTreatmentProstatic Neoplasms2
2CompletedTreatmentRecurrent Prostate Cancer2
2CompletedTreatmentUterine Leiomyomas1
2Not Yet RecruitingBasic ScienceDepression / Perinatal Depression / Post Partum Depression / Postpartum Depression1
2Not Yet RecruitingTreatmentAdenocarcinoma, Prostate / Hormone Sensitive Prostate Cancer / Metastasis Prostate Adenocarcinoma1
2Not Yet RecruitingTreatmentAlzheimer's Disease (AD)1
2Not Yet RecruitingTreatmentBreast Cancer1
2Not Yet RecruitingTreatmentMetastatic Prostate Adenocarcinoma / Prostate Adenocarcinoma With Focal Neuroendocrine Differentiation / Recurrent Prostate Carcinoma / Stage IVB Prostate Cancer AJCC v81
2Not Yet RecruitingTreatmentProstate Cancer3
2RecruitingOtherBreast Cancer1
2RecruitingTreatmentAdenocarcinoma, Prostate1
2RecruitingTreatmentBreast Cancer1
2RecruitingTreatmentBreast Cancer / Breast Cancer Invasive Nos1
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)1
2RecruitingTreatmentMetastatic Hormone Refractory Prostate Cancer1
2RecruitingTreatmentNewly Diagnosed Oligometastatic Prostate Cancer1
2RecruitingTreatmentProstate Cancer6
2RecruitingTreatmentProstate Cancer / Prostate Neoplasms / Prostatic Neoplasms1
2RecruitingTreatmentProstatic Neoplasms1
2TerminatedPreventionUterine Leiomyomas1
2TerminatedSupportive CareAdenocarcinoma, Prostate / Malignancies / Prostate Cancer1
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
2TerminatedTreatmentBreast Cancer1
2TerminatedTreatmentHodgkins Disease (HD) / Mantle Cell Lymphoma (MCL) / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2TerminatedTreatmentProstate Cancer4
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, 3TerminatedTreatmentProstate Cancer1
2, 3Unknown StatusTreatmentPedophilia1
3Active Not RecruitingTreatmentBreast Cancer2
3Active Not RecruitingTreatmentGastrointestinal Complications / Prostate Cancer / Sexual Dysfunctions / Urinary Complications1
3Active Not RecruitingTreatmentHormone Sensitive Prostate Cancer / Prostate Cancer1
3Active Not RecruitingTreatmentMetastases1
3Active Not RecruitingTreatmentProstate Cancer6
3CompletedTreatmentAdenocarcinoma, Prostate1
3CompletedTreatmentBMI >30 kg/m21
3CompletedTreatmentBreast Cancer2
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
3CompletedTreatmentEndometriosis / Pelvic Pain1
3CompletedTreatmentFertility Preservation / Malignancies1
3CompletedTreatmentIdiopathic Short Stature (ISS)1
3CompletedTreatmentMalignant Neoplasm of Female Breast1
3CompletedTreatmentPrecocious Puberty, Central1
3CompletedTreatmentProstate Cancer17
3CompletedTreatmentProstatic Neoplasms1
3CompletedTreatmentProstatic Neoplasms, Locally Advanced1
3CompletedTreatmentPuberty, Precocious2
3CompletedTreatmentUterine Leiomyomas2
3RecruitingTreatmentBreast Cancer Invasive1
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
3RecruitingTreatmentEndometriosis1
3RecruitingTreatmentMetastatic Breast Cancer (MBC)1
3RecruitingTreatmentProstate Cancer4
3TerminatedSupportive CareProstate Cancer1
3TerminatedTreatmentIsolated Angiitis of Central Nervous System / Lung Disease Interstitial Diffuse / Lung Disease With Systemic Sclerosis / Systemic Lupus Erythematosus (SLE) / Systemic Vasculitis1
3TerminatedTreatmentPedophilia1
3TerminatedTreatmentProstate Cancer4
3TerminatedTreatmentProstatic Neoplasms1
3Unknown StatusTreatmentEndometriosis / Menstrual Cramps / Painful Intercourse1
3Unknown StatusTreatmentInfertilities1
3Unknown StatusTreatmentProstate Cancer1
3WithdrawnTreatmentInfertilities / Infertility, Female / Male Infertility1
3WithdrawnTreatmentUterine Leiomyomas1
4Active Not RecruitingTreatmentProstate Cancer1
4CompletedNot AvailableEffect of Two Protocols of Ovarian Stimulation on Oocyte Quality1
4CompletedNot AvailableEndometriosis1
4CompletedNot AvailableProstate Cancer1
4CompletedBasic ScienceContraception / Fertility1
4CompletedBasic ScienceDepression / Hot Flushes / Menopause1
4CompletedBasic ScienceHot Flushes1
4CompletedPreventionOvarian Hyperstimulation Syndrome1
4CompletedTreatmentCentral Precocious Puberty (CPP)2
4CompletedTreatmentEgg Donation1
4CompletedTreatmentEndometriosis / Infertilities1
4CompletedTreatmentInfertilities1
4CompletedTreatmentInfertilities / Polycystic Ovarian Syndrome1
4CompletedTreatmentProstate Cancer3
4CompletedTreatmentPuberty, Precocious1
4Not Yet RecruitingTreatmentAmenorrhea / Endometriosis / Quality of Life1
4Not Yet RecruitingTreatmentIdiopathic Precocious Puberty1
4Not Yet RecruitingTreatmentInvitro Fertilization1
4Not Yet RecruitingTreatmentPolycystic Ovaries Syndrome1
4RecruitingBasic ScienceMenopause1
4RecruitingTreatmentAbortions spontaneous / Egg Retrieval / IVF Cycle / Ovarian Hyperstimulation / Ovarian Stimulation / Pregnancy1
4RecruitingTreatmentCentral Precocious Puberty (CPP)1
4RecruitingTreatmentLeiomyomas3
4RecruitingTreatmentPrecocious Puberty, Central1
4TerminatedDiagnosticEndometrial Receptivity / Ovarian Hyperstimulation Syndrome1
4TerminatedOtherMetastatic Hormone Refractory Prostate Cancer1
4TerminatedTreatmentInfertilities1
4TerminatedTreatmentOSAS (Obstructive Sleep Apneas Syndrome) / Polycystic Ovaries Syndrome1
4TerminatedTreatmentProstate Cancer1
4Unknown StatusPreventionCentral Precocious Puberty (CPP)1
4WithdrawnTreatmentInfertilities1
Not AvailableCompletedNot AvailableAdvanced Prostate Cancer / Lower Urinary Tract Symptoms (LUTS)1
Not AvailableCompletedNot AvailableAdvanced Prostate Carcinoma1
Not AvailableCompletedNot AvailableBMI >30 kg/m21
Not AvailableCompletedNot AvailableBreast Cancer2
Not AvailableCompletedNot AvailableEndometriosis / Endometriosis of Uterus1
Not AvailableCompletedNot AvailablePremenopausal Breast Cancer1
Not AvailableCompletedNot AvailableProstate Cancer3
Not AvailableCompletedNot AvailableProstatic Neoplasms1
Not AvailableCompletedNot AvailablePuberty, Central Precocious / Puberty, Precocious1
Not AvailableCompletedBasic ScienceBMI >30 kg/m21
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Menopausal Syndromes1
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 Cancer2
Not AvailableRecruitingNot AvailableAdenocarcinoma, Prostate / Prostate Cancer1
Not AvailableRecruitingNot AvailableProstate Cancer2
Not AvailableRecruitingNot AvailableSpinal and Bulbar Muscular Atrophy1
Not AvailableRecruitingBasic ScienceBMI >30 kg/m2 / Menopause1
Not AvailableRecruitingTreatmentAdenocarcinoma of the Prostate1
Not AvailableTerminatedNot AvailableGender Dysphoria1
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
Injection, powder, for suspension, extended releaseSubcutaneous22.5 mg
Injection, powder, for suspension, extended releaseSubcutaneous30 mg
Injection, powder, for suspension, extended releaseSubcutaneous45 mg
Injection, powder, for suspension, extended releaseSubcutaneous7.5 mg
KitSubcutaneous22.5 mg/0.375mL
KitSubcutaneous30 mg/0.5mL
KitSubcutaneous45 mg/0.375mL
KitSubcutaneous7.5 mg/0.25mL
Injection, solutionSubcutaneous1 mg/.2mL
KitTopical1 mg/0.2mL
LiquidSubcutaneous
KitTopical5 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
KitTopical22.5 mg/1.5mL
KitTopical3.75 mg/1mL
KitTopical30 mg/1.5mL
KitTopical45 mg/1.5mL
KitTopical7.5 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
KitTopical11.25 mg/1mL
KitTopical
Injection, powder, for suspension, extended release; kitIntramuscular
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)
US6036976No2000-03-142016-12-13Us
US8921326No2014-12-302031-02-05Us
US7429559No2008-09-302019-01-13Us
US8815801No2014-08-262022-06-28Us
US5728396No1998-03-172017-01-30Us
US6156331No2000-12-052017-01-30Us
US6375978No2002-04-232018-12-17Us
US6235712No2001-05-222017-06-13Us
US6113938No2000-09-052018-07-24Us
US6124261No2000-09-262017-06-13Us
US6395292No2002-05-282017-01-30Us
US6132420No2000-10-172017-01-30Us
US5985305No1999-11-162017-01-30Us
US5932547No1999-08-032017-06-13Us
US6565874No2003-05-202018-10-28Us
US6773714No2004-08-102018-10-28Us
US6626870No2003-09-302020-03-27Us
US9283282No2016-03-152018-10-28Us
US9254307No2016-02-092018-10-28Us
US8486455No2013-07-162018-10-28Us
US8840916No2014-09-232020-11-13Us
US8470359No2013-06-252023-10-15Us
US9539333No2017-01-102020-11-13Us
US9914802No2018-03-132020-11-13Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

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
Humans
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
Humans
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 16, 2019 10:17