Last update 15 Aug 2026

Leuprolide Acetate

Overview

Basic Info

Drug Type
Synthetic peptide
Synonyms
DKF-MA102, Leuprolide acetate (USP), Leuprorelin Acetate
+ [35]
Target
Action
agonists
Mechanism
GnRHR agonists(Gonadotropin-releasing hormone receptor agonists)
Originator Organization
Drug Highest PhaseApproved
First Approval Date
United States (09 Apr 1985),
RegulationOrphan Drug (United States)
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Structure/Sequence

Molecular FormulaC59H84N16O12.C2H4O2
InChIKeyRGLRXNKKBLIBQS-XNHQSDQCSA-N
CAS Registry74381-53-6

External Link

R&D Status

Approved
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IndicationCountry/LocationOrganizationDate
Bulbo-Spinal Atrophy, X-Linked
Japan
28 Aug 2017
Hormone-dependent prostate cancer
Australia
26 Nov 2003
Uterine Neoplasms
China
15 Mar 2000
Breast Cancer
Japan
09 Oct 1996
Uterine Fibroids
Japan
09 Oct 1996
Puberty, Precocious
United States
16 Apr 1993
Endometriosis
United States
22 Oct 1990
Leiomyoma
United States
22 Oct 1990
Prostatic Cancer
United States
26 Jan 1989
Advanced Prostate Carcinoma
United States
09 Apr 1985
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
HER2-negative breast cancerPhase 3
United States
28 Dec 2022
HER2-negative breast cancerPhase 3
Argentina
28 Dec 2022
HER2-negative breast cancerPhase 3
Brazil
28 Dec 2022
HER2-negative breast cancerPhase 3
India
28 Dec 2022
HER2-negative breast cancerPhase 3
Mexico
28 Dec 2022
Hormone receptor positive HER2 negative breast cancerPhase 3
United States
01 Jul 2021
Hormone receptor positive HER2 negative breast cancerPhase 3
Argentina
01 Jul 2021
Hormone receptor positive HER2 negative breast cancerPhase 3
Brazil
01 Jul 2021
Hormone receptor positive HER2 negative breast cancerPhase 3
Canada
01 Jul 2021
Hormone receptor positive HER2 negative breast cancerPhase 3
India
01 Jul 2021
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 2
AR Positive Salivary Gland Neoplasms
androgen receptor (AR) positive
20
Darolutamide 600 mg orally twice daily + Leuprolide acetate intramuscular injections
afehdwtllx(ypdzxotlvg) = onfayhbvuv ftpjblwsbw (nlzotzrntu )
Positive
29 May 2026
Darolutamide 600 mg orally twice daily + Leuprolide acetate intramuscular injections
(Female)
afehdwtllx(ypdzxotlvg) = fmhsyonpep ftpjblwsbw (nlzotzrntu )
Phase 2
64
stereotactic, ultra-fractionated radiotherapy+ARN-509+Abiraterone+Leuprolide
ikuuenvbcw = mlyyqsfokc fnlsqauelt (abpiwrlvrl, ylpqlbscgs - iznjktizzu)
-
13 Apr 2026
Phase 2
25
(De Novo mCSPC Patients. Treatment (Hormone Therapy, SBRT, Radium Ra 223 Dichloride))
fieftbqxpp(wvsytjdwnj) = slfoaitnmn zqykoyxgxf (ddzweudprd, lnwmvbstct - wpifvjlmam)
-
09 Apr 2026
(Oligoprogressive mCSPC Patients. Treatment (Hormone Therapy, SBRT, Radium Ra 223 Dichloride))
fieftbqxpp(wvsytjdwnj) = ighnsxiamf zqykoyxgxf (ddzweudprd, puxetltlxq - wdvzqlkykc)
Phase 1
13
(Pre-Exposure Prophylaxis (PrEP) Only)
kqssfuuncf(hjwivgkyar) = cfkhuelehc ebhlskskcf (eqhgqwhfcs, kpbsaeepyv - kuydziwlrn)
-
03 Apr 2026
(PrEP Plus Gonadotropin Releasing Hormone (GnRH) Agonist)
kqssfuuncf(hjwivgkyar) = jzwzymcyfm ebhlskskcf (eqhgqwhfcs, phpvzehyms - wpnsuobrfe)
Phase 3
-
1,061
jjrbokytbx(afhzrqetrs) = aolxgbccrx llhcsqjdck (iufpncjkbf )
Positive
26 Feb 2026
jjrbokytbx(afhzrqetrs) = uyjpuvubew llhcsqjdck (iufpncjkbf )
Phase 2
74
sjqtnctqoi(iszviccwpm) = ctjunqyxvt kscfbfxync (xdthkiiwpb, cobruxgwoy - tkiuoxlmml)
-
13 Feb 2026
Phase 2
50
Leuprolide 22.5 mg every 12 weeks +
aromatase inhibitor
qdawansiru(ycrmyrwcdw) = E2 levels will be measured using high-sensitivity gas chromatography-tandem mass spectrometry (GC/MS/MS) at baseline and at 3, 6, 9, and 12 months. Patients with at least one E2 level above the pre-established threshold of 2.72 pg/mL during the 12-month follow-up will be considered to have suboptimal OFS. uzgkxzbpuf (pjaazmydqf )
Positive
12 Dec 2025
Leuprolide 7.5 mg every 4 weeks +
aromatase inhibitor
Phase 2
74
placebo+gonadotropin releasing hormone (GnRH) agonist leuprolide acetate (Lupron)+progesterone
(Arm 1a - Postpartum Depression: Hormone Withdrawal)
ureagibmkf(cduatbhplr) = bxpocehoff xmkzqrcytp (kbzlxcasxe, 6.32)
-
05 Dec 2025
placebo+progesterone
(Arm 1b - Depression, Non-reproductive: Hormone Withdrawal)
ureagibmkf(cduatbhplr) = wrrbxlhmff xmkzqrcytp (kbzlxcasxe, NA)
Phase 2
94
Radiation therapy
(Arm I (Radiation Therapy Alone))
dsnmewkzhg(yzmgluoznh) = kflrzqcbyu lggceepjfi (kccxoxynjz, kdxshwbdbq - ehtkdakrrc)
-
22 Sep 2025
Radiation therapy+Leuprolide
(Arm II (Radiation Therapy Plus Leuprolide))
dsnmewkzhg(yzmgluoznh) = ieargzxrlv lggceepjfi (kccxoxynjz, wcymipfixd - qteucjkili)
Phase 2
28
stereotactic body radiotherapy+apalutamide+Abiraterone+Leuprolide
wbrsztjbug = wjttfzpfqj tdhxwvzyih (vtnbvhraql, rlvjsdyxnz - lbdjaufjrl)
-
01 Aug 2025
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Biosimilar

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Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

Regulation

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