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leuprolide (Lutrate)

✓ Approved

GP Pharm · GNRHR · 小分子

什么是 leuprolide？

leuprolide 是一种小分子，由GP Pharm研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intramuscular (IM) Injection。

药物档案

商品名Lutrate
公司GP Pharm
药物类别小分子, 多肽类
分子靶点GNRHR
给药途径Injectable (Others), Intramuscular (IM) Injection
状态Approved
来源： ClinicalTrials.gov, GP Pharm

作用机制

分子靶点

leuprolide 作用于 1 个分子靶点：

GNRHRgonadotropin releasing hormone receptor (HH7, GRHR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

leuprolide 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Prostate cancer✓ Approved

相关研究文献

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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PubMedCase reports in psychiatry2026-09-08

Breaking the Cycle: A Case of Delayed Diagnosis and Sustained Remission Following Definitive Surgical Treatment of Premenstrual Dysphoric Disorder (PMDD).

Deaton Daniel J DJ, Deaton Susannah L SL

Premenstrual dysphoric disorder (PMDD) is a hormone-sensitive mood disorder characterized by cyclical psychiatric and physical symptoms that impair functioning. Despite inclusion in DSM-5 and ICD-11, PMDD is frequently misdiagnosed or overlooked due to clinical unfamiliarity, lack of structured assessment, and systemic minimization of hormone-linked distress. Women routinely face delays in diagnosis and often only receive definitive treatment through self-advocacy. This report describes a 35-year-old cisgender female with treatment-resistant PMDD, whose symptoms began after menarche and worsened over two decades. Despite multiple psychiatric and medical encounters, her condition was misattributed to obesity, mood disorders, or trauma. After a diagnostic delay and multiple first and second-line treatment failures, a trial of leuprolide acetate confirmed a hormonal etiology of her symptoms, and she subsequently underwent total hysterectomy with bilateral salpingo-oophorectomy. Although she experienced a severe depressive episode in the immediate postoperative period, she has since remained in sustained symptom remission on an SSRI and estrogen replacement. This case demonstrates the need to recognize cyclic symptom patterns and potential hormonal etiology in treatment-resistant mood disorders.

PMID 42708086
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PubMedThe Canadian journal of urology2026-09-02

Impact of leuprolide and goserelin on androgen suppression and adverse events in patients with prostate cancer.

Freitas Carla Simone Moreira CSM, Rocha-Silva Fabiana F, Marques-Silva Thaís Almeida TA, de Oliveira Ana Carolina Ribeiro ACR et al.

Androgen deprivation therapy (ADT) is widely employed in the management of advanced prostate cancer, with luteinizing hormone-releasing hormone (LHRH) agonists such as leuprolide and goserelin being common options. However, pharmacological and metabolic differences between these agents may affect the efficacy of hormonal suppression and adverse event profiles. This study compared the effects of leuprolide (22.5 and 45 mg) and goserelin (10.8 mg) on prostate-specific antigen (PSA) and testosterone reduction, as well as their metabolic and cardiovascular impacts and the influence of genetic variants on therapeutic response. A prospective, randomized, controlled study was conducted with 174 patients diagnosed with prostate cancer and treated with ADT for 12 months. Serum PSA and testosterone levels, lipid and glycemic profiles, and adverse events were monitored. Genetic analyses were performed to identify mutations in the TP53, BRCA1, BRCA2, and ATM genes. All treatment groups exhibited significant reductions in PSA and testosterone levels. Leuprolide 22.5 mg achieved the most pronounced PSA reduction, whereas goserelin 10.8 mg demonstrated greater variability in testosterone during the early months of therapy. Hot flashes were the most frequent adverse event, reported in 90% of patients treated with leuprolide 22.5 mg, while cardiovascular events were more prevalent in the goserelin 10.8 mg group. The TP53 gene was the most frequently altered (20.4%), followed by BRCA2 (7.4%) and ATM (6.5%), though these mutations did not significantly affect treatment response. ADT effectively achieves hormonal suppression in prostate cancer; however, differences between LHRH agonists influence clinical and metabolic outcomes. Leuprolide 22.5 mg showed superior PSA reduction but higher rates of vasomotor symptoms and weight gain, while goserelin 10.8 mg was associated with hormonal instability and cardiovascular risk. Genetic findings suggest that BRCA2 variants may affect lipid metabolism, reinforcing the need for personalized ADT strategies integrating metabolic and genetic profiles.

PMID 42682049
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PubMedMedwave2026-08-19

Efficacy and safety of goserelin vs. leuprolide in premenopausal breast cancer patients receiving adjuvant endocrine therapy: A retrospective cohort study.

Xu Jiahao J, Tai Yicheng Y, Fang Qi Q, Xue Hui H et al.

Goserelin and leuprolide are gonadotropin-releasing hormone (GnRH) agonists used for ovarian function suppression in premenopausal breast cancer patients. Whether their different molecular structures lead to clinically meaningful differences in efficacy and safety remains unclear. To compare the efficacy and safety of goserelin versus leuprolide as adjuvant endocrine therapy (combined with tamoxifen) in premenopausal women with hormone receptor-positive breast cancer after curative surgery. This retrospective cohort study initially recruited 215 young cancer patients receiving adjuvant chemotherapy with tamoxifen combined with a gonadotropin-releasing hormone agonist. After applying inclusion and exclusion criteria, 187 patients were included and divided into two groups according to the gonadotropin-releasing hormone agonist they actually received: leuprolide (n=90) or goserelin (n=97). The primary efficacy outcome was the proportion of patients achieving substantial estrogen reduction (estradiol ≤30 pg/mL or falling into the pre-specified laboratory range) after 6 months. Secondary outcomes included liver function parameters and thyroid function parameters. Exploratory outcomes included changes from baseline to six months in testosterone, luteinizing hormone (LH), follicle-stimulating hormone (FSH), and prolactin levels, as well as descriptive assessment of the tumor marker carcinoembryonic antigen (CEA). Between-group differences were expressed as risk differences (RDs) with 95% confidence intervals (CIs). Baseline demographic and cancer-related characteristics were balanced between the two groups. After six months of adjuvant therapy, the two groups showed similar primary efficacy: the proportion of patients with substantial estrogen reduction was 88.89% in the leuprolide group and 92.78% in the goserelin group (RD = -3.89%, 95% CI: -12.18% to 4.40%; p = 0.354). Regarding safety, the leuprolide group had a significantly higher rate of liver function abnormalities (30.00% vs. 13.40%; RD = 16.60%, 95% CI: 4.96% to 28.24%; p = 0.012), driven mainly by a lower rate of normal aspartate aminotransferase (AST) levels (85.56% vs. 96.91%; RD = -11.35%, 95% CI: -19.39% to -3.31%; p < 0.05). In contrast, the leuprolide group had a higher rate of normal thyroid function (88.89% vs. 76.29%; RD = 12.60%, 95% CI: 1.94% to 23.26%; p = 0.018), mainly due to a higher normal thyroid-stimulating hormone rate (93.33% vs. 83.51%; RD = 9.82%, 95% CI: 0.82% to 18.82%; p < 0.05). Carcinoembryonic antigen normalization rates were also comparable (93.33% vs. 92.78%; RD = 0.55%, 95% CI: -6.74% to 7.84%; p = 0.549). Leuprolide and goserelin demonstrate similar efficacy when used as adjuvant therapy in combination with tamoxifen for young women with breast cancer. However, leuprolide may pose a potential risk of hepatic impairment, whereas goserelin appears to be associated with a higher incidence of thyroid injury. These findings provide a theoretical basis for personalized clinical management in this patient population.

PMID 42617170
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PubMedJACC. CardioOncology2026-08-19

Divergent Effects of GnRH Agonist and GnRH Antagonist Treatment on Platelet Activity and Transcriptome.

Beitzen-Heineke Antonia A, Siskin Matthew M, Muller Matthew M, Bhatt Anshini A et al.

Prostate cancer is associated with increased cardiovascular risk. Among androgen deprivation therapy (ADT) modalities, the gonadotropin-releasing hormone (GnRH) antagonist relugolix appears to confer a lower risk for cardiovascular events than the GnRH agonist leuprolide. The aim of this prospective study was to investigate the impact of relugolix and leuprolide on platelet phenotype. Patients with prostate cancer initiating first-line ADT were prospectively enrolled. Blood samples were collected at baseline and 8 ± 4 weeks after treatment initiation. Platelet activation was assessed using flow cytometry (P-selectin, PAC-1, CD40, CD40L, and monocyte-platelet aggregates). Platelet RNA sequencing was performed to characterize treatment-associated transcriptomic changes. Compared with healthy control subjects, patients (n = 69) exhibited elevated P-selectin expression and enrichment of thromboinflammatory pathways. During leuprolide treatment (n = 40), PAC-1 expression increased compared with baseline in response to epinephrine, thrombin, adenosine diphosphate (ADP) and arachidonic acid (AA), while P-selectin increased in response to epinephrine and was higher with ADP and AA, though not statistically different. In contrast, during relugolix treatment (n = 29), AA-induced P-selectin expression and CD40 decreased. Platelet RNA sequencing in relugolix-treated patients demonstrated down-regulation of pathways associated with platelet activation and aggregation. Finally, leuprolide-treated patients on aspirin (n = 6) did not exhibit increased AA-induced platelet activation and in vitro P2Y12 inhibition of patient-derived platelets attenuated activation induced by epinephrine, ADP, and AA. Prostate cancer is associated with heightened platelet activation and thromboinflammatory signaling. Treatment with leuprolide, but not relugolix, was associated with further augmented platelet activity. These findings support further studies to clarify links with platelet-mediated cardiovascular risk and the potential role of platelet-targeted strategies.

PMID 42615451
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PubMedJACC. CardioOncology2026-08-19

Statin Use Attenuates Leuprolide-Associated Coronary Atherosclerosis Progression: A Secondary Analysis of the REVELUTION Trial.

Yadalam Adithya K AK, Liu Chang C, van Assen Marly M, Sebastian Nikhil T NT et al.

PMID 42615454
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