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All Leuprolide data. Full access. Full negotiation power €399,-
Distributor CDMO Produced in Asia | Employees: 50+ | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA | CEP All certificates GMP CEP USDMF ISO9001 CoA
Producer CDMO Produced in Asia | Employees: 25+ | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA All certificates MSDS BSE/TSE ISO9001 CoA
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Producer CDMO Produced in Asia | Employees: 10+ | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA All certificates FDA USDMF MSDS BSE/TSE CoA
Producer Produced in Asia | Employees: 1000+ | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA All certificates CoA
Producer Produced in Europe | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA | CEP All certificates GMP FDA CEP USDMF coa
Producer Produced in South America | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA All certificates USDMF CoA
Get full market intelligence report €399,- All Leuprolide data. Full access. Full negotiation power
Producer Produced in Asia | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA | CEP All certificates FDA CEP USDMF CoA WC
Producer Produced in Asia | Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you're interested! Certifications: CoA | CEP All certificates GMP FDA CEP USDMF coa
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A medication that addresses advanced prostate cancer, central precocious puberty, endometriosis symptoms, and preoperative management of anemia in uterine fibroids for diverse therapeutic applications.
Adrenal Cortex Hormones Agents Causing Muscle Toxicity Amino Acids, Peptides, and Proteins Antineoplastic Agents Antineoplastic Agents, Hormonal Antineoplastic and Immunomodulating Agents
Leuprolide (CAS 53714-56-0) is a synthetic nonapeptide analogue of gonadotropin-releasing hormone designed to extend circulating half-life through incorporation of a D-leucyl residue. Its primary clinical indications include advanced prostate cancer, central precocious puberty, endometriosis in combination with norethisterone, and preoperative hematologic optimization in patients with uterine fibroids when used with iron supplementation. The molecule was first approved in 1985 as a daily subcutaneous formulation, with multiple long‑acting intramuscular and subcutaneous depot products later introduced, including six‑month dosing regimens used in global clinical practice.
Pharmacologically, leuprolide functions as a GnRH receptor superagonist. Initial activation of pituitary receptors produces a transient surge in luteinizing hormone, follicle-stimulating hormone, and downstream sex steroids. Continuous receptor stimulation over two to four weeks induces receptor desensitization and suppression of gonadotropin output, resulting in medical castration–level reductions in testosterone or estradiol. These endocrine effects are reversible upon cessation.
Key ADME characteristics reflect its peptide structure. Leuprolide is administered parenterally, displays an extended but still relatively short systemic half-life compared with endogenous GnRH, and undergoes enzymatic degradation to inactive peptide fragments. Renal elimination contributes to clearance, consistent with its designation among drugs primarily excreted renally.
Safety considerations differ across patient groups. In men with prostate cancer, the initial testosterone rise may precipitate tumour flare, bone pain, urinary obstruction, or spinal cord compression, and treatment is associated with risks of hyperglycemia, diabetes, cardiovascular events, QT prolongation, and convulsions. In women, the early estradiol increase may transiently worsen symptoms, and long‑term therapy is linked to bone mineral density loss. Combination therapy with norethisterone may increase risks of thromboembolic and visual events. In pediatric patients with central precocious puberty, transient pubertal progression, psychiatric symptoms, and convulsions have been reported.
For API procurement, sourcing should focus on peptide integrity, consistent impurity control, and validated manufacturing processes to ensure batch-to-batch reliability suitable for long‑acting injectable formulations.
Gonadotropin-releasing hormone (GnRH) is a naturally occurring decapeptide that modulates the hypothalamic-pituitary-gonadal (HPG) axis. GnRH binds to corresponding receptors (GnRHRs) on the anterior pituitary gonadotropes, which in turn release luteinizing hormone (LH) and follicle-stimulating hormone (FSH); these, in turn, affect the downstream synthesis and release of the sex hormones testosterone, dihydrotestosterone, estrone, and estradiol. Despite the variety of conditions indicated for treatment with leuprolide, the mechanism of action underlying efficacy is the same in all cases. As a GnRHR agonist, leuprolide binds to and initially activates downstream LH and FSH release; this initial spike in gonadotropin levels is responsible for some of the adverse effects associated with treatment. After 2-4 weeks of treatment, continuous stimulation of GnRHR results in feedback inhibition and significant downregulation of LH, FSH, and their corresponding downstream effects, producing a therapeutic benefit. These effects are reversible upon treatment discontinuation.
Leuprolide is a gonadotropin-releasing hormone (GnRH) analogue that functions as a GnRH receptor superagonist.After an initial spike in GnRH-mediated steroidal production, including testosterone and estradiol, prolonged use results in a significant drop in circulating steroid levels, in line with those produced through other forms of androgen-deprivation therapy (ADT).The corresponding hormonal/steroidal changes produce specific adverse effects in different patient populations. In women undergoing treatment for endometriosis or uterine leiomyomata, careful consideration regarding pregnancy status is advised. The initial increase in estradiol levels may worsen symptoms such as pain and bleeding. Long-term use of leuprolide is associated with loss of bone mineral density. Patients co-administered with norethisterone may experience sudden vision loss, proptosis, diplopia, migraine, thrombophlebitis, and pulmonary embolism and may also be at higher risk of cardiovascular disease. Patients with a history of depression may experience severe recurrence of depressive symptoms. In men undergoing palliative treatment for advanced/metastatic prostate cancer, short-term spikes in testosterone levels may cause tumour flare and associated symptoms such as bone pain, hematuria, neuropathy, bladder and/or ureteral obstruction, and spinal cord compression. In addition, patients are at increased risk of developing hyperglycemia, diabetes, and cardiovascular disease, which may manifest through myocardial infarction, stroke, cardiac death, or prolonged QT/QTc interval. In addition, Leuprolide may cause convulsions and embryo-fetal toxicity. In pediatric patients undergoing treatment for central precocious puberty (CPP), the initial steroidal spike may be associated with increased clinical signs of puberty within 2-4 weeks of treatment initiation. In addition, leuprolide may cause convulsions and psychiatric symptoms, including irritability, impatience, aggression, anger, and crying.
