Drug Database
LE

leuprolide (Lutrate)

✓ Approved

GP Pharm · GNRHR · Small Molecule

What is leuprolide?

leuprolide is a small molecule developed by GP Pharm. It is approved for therapeutic indications via injectable (others) or intramuscular (im) injection.

Drug Profile

Brand NamesLutrate
CompanyGP Pharm
Drug ClassSmall Molecule, Polypeptide
Molecular TargetGNRHR
RouteInjectable (Others), Intramuscular (IM) Injection
StatusApproved
Sources: ClinicalTrials.gov, GP Pharm

Mechanism of Action

Molecular Targets

leuprolide acts on 1 molecular target:

GNRHRgonadotropin releasing hormone receptor (HH7, GRHR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

leuprolide is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Prostate cancer✓ Approved

Related Research Articles

PubMedUrologic oncology2026-10-18

Comparison of cardiovascular events in patients with metastatic hormone sensitive prostate cancer treated with LHRH agonists to LHRH antagonists in the US: A retrospective cohort study.

Titus Renil S RS, Velasquez Eusebio Luna EL, Mundra Vatsala V, Riveros Carlos C et al.

Androgen deprivation therapy (ADT) is standard treatment for metastatic hormone-sensitive prostate cancer (mHSCaP). Patients receive LHRH-agonists (LHRH-AG: leuprolide, goserelin or triptorelin) or LHRH-antagonists (LHRH-AN: degarelix or relugolix) with intensification with androgen receptor pathway inhibitors, with or without chemotherapy. Given ongoing concerns about cardiovascular risk, we used real-world data from TriNetX to compare the incidence of major adverse cardiovascular events (MACE) between patients receiving LHRH-AG vs. LHRH-AN. We included adult patients with mHSCaP who received either an LHRH-AG or LHRH-AN. The composite primary outcome was MACE (defined as myocardial infarction (MI), stroke, or all-cause mortality). Secondary outcomes were MI, stroke, and all-cause mortality. Patients were 1:1 propensity-score matched (PSM). Kaplan-Meier analysis reporting hazard ratios (HR) and 95% confidence intervals (CI) for the outcomes was conducted. We conducted a subgroup analysis to assess the effect of intensification of therapy. Exploratory analyses were conducted to assess HR of outcomes and new-onset metabolic comorbidities (diabetes mellitus, insulin use, hypertension, and dyslipidemia) amongst patients without cardiovascular risk factors. Before PSM, there were 27,051 in LHRH-AG and 3,339 in LHRH-AN cohorts. After PSM, 3,329 patients in each cohort were compared. Compared to LHRH-AN, LHRH-AG was associated with a decreased risk of MACE (hazard ratio [HR] = 0.86, 95% CI: 0.79-0.93), MI (HR = 0.80, 95% CI: 0.66-0.97), and any-cause mortality (HR = 0.85, 95% CI: 0.78-0.93). Treatment intensification did not modify the association between MACE outcomes and LHRH-AG vs. LHRH-AN. Using real-world data, LHRH-AG was associated with a decreased risk of experiencing MACE. Among those undergoing intensification of therapy, there was no difference in MACE risk associated with LHRH-AG vs. LHRH-AN.

PMID 42892580
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PubMedCureus2026-10-17

Acute Urinary Retention Leading to Post-renal Acute Kidney Injury Post-radiotherapy: A Case Report.

Bitterman Brayden B, Vaishampayan Nitin N, Hart Kimberly B KB, Boggula Ramesh R et al.

A man in his 70s with high-risk localized prostate adenocarcinoma underwent definitive external beam radiotherapy (EBRT) to the prostate and pelvis with concurrent androgen deprivation therapy using leuprolide. Eight days after completion of radiotherapy, he developed acute urinary retention (AUR) with overflow incontinence, constipation, and post-renal acute kidney injury (AKI), requiring hospitalization and bladder decompression with Foley catheter placement. Initial urine output was approximately 1 liter, and creatinine improved from 4.89 mg/dL to 1.46 mg/dL after decompression. Imaging demonstrated mild left hydronephrosis and chronic renal disease without an obstructing calculus. He was discharged home on tamsulosin and a bowel regimen with a Foley catheter in place. Persistent catheter dependence subsequently required transurethral resection of the prostate (TURP) with improvement in symptoms. This case report describes a case of severe acute urinary retention with post-renal acute kidney injury occurring shortly after prostate and pelvic radiotherapy. The obstruction was likely multifactorial, with radiation-associated inflammation or edema potentially aggravating the underlying outlet issues and constipation. Prompt recognition and bladder decompression may permit rapid renal recovery and are important in patients with reduced renal reserves.

PMID 42889864
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PubMedGynecologic oncology reports2026-10-13

Persistently elevated estradiol after bilateral salpingo-oophorectomy in recurrent low-grade endometrial stromal sarcoma: a case report.

Moghaddam Ali Sanjari AS, Pastore Benjamin B, Turzio Maria Fernandez MF, McCash Samuel S et al.

Low-grade endometrial stromal sarcoma (LGESS) is a rare uterine mesenchymal neoplasm that frequently expresses estrogen and progesterone receptors. Endocrine therapy is a cornerstone of treatment for recurrent or metastatic LGESS. In premenopausal patients, bilateral salpingo-oophorectomy (BSO) is commonly performed to reduce endogenous estrogen production and would be expected to result in a postmenopausal hormonal profile. We report the case of a patient with recurrent, metastatic estrogen receptor (ER)/progesterone receptor (PR)-positive LGESS who had previously undergone BSO. Her disease initially responded to aromatase inhibitor therapy; however, she subsequently experienced pulmonary progression, including a large endobronchial metastasis requiring bronchoscopic cytoreduction. Despite pathologically confirmed BSO, further evaluation revealed a hormone profile more consistent with persistent premenopausal estrogen exposure. Given concern that ongoing estrogen exposure may have been contributing to progression of this hormone-sensitive malignancy, treatment was changed to combined leuprolide and letrozole. Three months after initiation of combined endocrine therapy, imaging demonstrated a partial response, which was confirmed at 6 months, accompanied by estradiol levels in the postmenopausal range. This case raises the possibility that surgical menopause may not always result in complete estrogen deprivation in LGESS. Potential explanations include assay limitations, undetectable residual gonadotropin-responsive steroidogenic tissue, peripheral aromatization, and tumor-associated estrogenic activity. Biochemical evaluation of estrogen status may be informative in select patients whose disease behavior appears discordant with presumed post-oophorectomy menopausal status.

PMID 42866660
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PubMedIJU case reports2026-10-06

Prostatic Adenosquamous Carcinoma With a Minute Squamous Component in the Initial Biopsy and Early Liver Metastasis: A Case Report.

Tsubouchi Yohei Y, Naiki Taku T, Naiki-Ito Aya A, Unno Rei R et al.

We report a case of de novo prostatic adenosquamous carcinoma with a minute squamous component in the initial biopsy and early liver metastasis despite a marked prostate-specific antigen response. A 72-year-old man was diagnosed with locally advanced prostate cancer with nodal and multiple bone metastases. Prostate biopsy initially showed adenocarcinoma with a Gleason score of 4 + 5. After leuprolide and abiraterone plus radiotherapy, prostate-specific antigen decreased from 13.0 to 0.22 ng/mL; however, a liver metastasis developed. Re-evaluation of the prostate biopsy revealed minute squamous differentiation, and liver biopsy showed metastatic squamous cell carcinoma. Immunohistochemistry showed retained MLH1 and PMS2 expression with loss of MSH2 and MSH6 in both specimens. Genomic profiling showed microsatellite instability-high status. Repeat biopsy and molecular-pathological reassessment may be important when radiographic progression is discordant with prostate-specific antigen kinetics.

PMID 42835373
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PubMedFrontiers in cell and developmental biology2026-09-15

Long-term testicular changes caused by the temporary suspension of puberty initiated at different stages of development.

Mancilla-Martínez Christian C, Contreras-García Itzel Jatziri IJ, Rojas-Castañeda Julio César JC, Landero-Huerta Daniel Adrian DA et al.

During puberty, secondary sexual characteristics develop alongside processes of testicular cell differentiation and maturation. Puberty suppression has been introduced to prevent the development of these physical changes in some individuals who request it, as is the case with gender dysphoria. However, not everyone continues with the treatment. Therefore, the objective of this study was to determine the testicular changes caused by the temporary suppression of puberty, initiated at different stages of development, in an experimental model. A total of 56 male rats were used, distributed equally into four study groups. A Control group, which received saline, and three experimental groups that received the GnRH analog (GnRHa), leuprolide acetate at 25 μg/kg/day. In the first of these groups, administration of the analog began during early puberty (LeuEP) on day postpartum (dpp) 25, equivalent to Tanner stages II-III in humans; in the second group, administration began during advanced puberty (LeuAP) at 35 dpp, equivalent to Tanner stages IV-V; and in the postpubertal group (LeuPP), administration began at 60 dpp. Half of the number of animals in each group were euthanized at 90 dpp, while the remaining animals had the GnRHa removed to allow recovery and were euthanized at 190 dpp. Testicular tissue was collected to assess histological and ultrastructural changes, as well as proteins that regulate the functional activity of Sertoli and Leydig cells. The LeuEP and LeuAP groups exhibited seminiferous tubules atrophy with peritubular cell hyperplasia, resulting in thickened tubular walls. They also showed Leydig cell hyperplasia with low immunoreactivity to the HSD17B3 enzyme, reduced immunoreactivity to androgen receptor proteins, and vimentin disorganization. These same groups showed partial recovery at 190 dpp, without reaching the values of the Control group. This may have been due to the persistence of thick tubular walls, possibly resulting from the dysfunction of Leydig cells and peritubular cells, which impeded the paracrine action of molecules necessary to maintain spermatogenesis. Furthermore, this was compounded by Sertoli cell dysfunction. Therefore, the temporary arrest of puberty initiated during puberty resulted in permanent testicular alterations, unlike in animals where GnRHa administration began postpubertally.

PMID 42741146
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PubMedFrontiers in pharmacology2026-09-09

Comparison of Beiyi® and its reference product Enantone® as agonists of luteinizing hormone-releasing hormone against prostate cancer: a multicenter, randomized single-dose study.

Yi Yuyao Y, Shen Pengfei P, Zheng Tongsen T, Hou Ruigang R et al.

Leuprolide acetate is a potent agonist of luteinizing hormone-releasing hormone that has been licensed to treat prostate cancer. The microsphere formulation of leuprolide acetate called Beiyi®, developed in China, has shown favorable pharmacokinetics, pharmacodynamics and safety similar to those of the reference drug Enantone® in healthy individuals. The present study examined whether the two formulations are bioequivalent in men with prostate cancer. This multicenter, open-label study randomized 120 Chinese men with prostate cancer 1:1 to receive a single subcutaneous injection of Beiyi® or Enantone® (3.75 mg). The two groups were compared in terms of pharmacokinetics and safety. The ratio of the geometric means of the maximum serum concentration (Cmax) of Beiyi® and Enantone® was 98.34% (91.88%-105.25%); the ratio of the geometric means of the concentration-time curve from 7 to 28 days (AUC7-28) was 100.52% (88.17%-114.60%); and the ratio of the geometric means of the concentration-time curve from 0 to 28 days (AUC0-28) was 109.07% (98.54%-120.73%). The three 90% confidence intervals fell within the range of 80.00%-125.00%, indicating similar pharmacokinetics. The two drugs showed similar safety profiles, with no treatment-emergent adverse events leading to withdrawal or death. The two formulations of leuprolide acetate microspheres Beiyi® and Enantone® show similar pharmacokinetics and safety in Chinese men with prostate cancer. These results support the further clinical development of Beiyi® as a generic formulation of Enantone®. CTR20222654 on http://www.chinadrugtrials.org.cn/index.html.

PMID 42713047
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