Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of leuprorelin acetate injection in China. Welcome to wholesale bulk high quality leuprorelin acetate injection for sale here from our factory. Good service and reasonable price are available.
Leuprorelin acetate injection is an artificially synthesized gonadotropin-releasing hormone (GnRH) analog that achieves precise treatment of hormone dependent diseases by regulating the pituitary gonadal axis function. Its core mechanism of action is "bidirectional regulation": after the first medication, it briefly stimulates the release of gonadotropins (FSH/LH), and then continuously inhibits their secretion through receptor desensitization, ultimately reducing ovarian estrogen or testicular teststerone levels to postmenopausal/castration status. In recent years, genetic testing techniques such as GNRH1 gene polymorphism analysis have provided a basis for personalized medication, and the development of long-acting formulations has significantly improved patient compliance. As a core drug in the field of hormone regulation, this product has become an important tool for multidisciplinary disease management by balancing efficacy and safety.
Additional information of chemical compound:
| Product Name | Leuprorelin Acetate Injection | Leuprorelin Acetate |
| Product Type | Injection | Powder |
| Product Purity | ≥99% | ≥99% |
| Product Specifications | Customizable | Customizable |
| Product Package | Customizable | Customizable |
Our product form
Leuprorelin Acetate COA
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Certificate of Analysis |
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Compound name |
Leuprorelin Acetate | |
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CAS No. |
74381-53-6 | |
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Grade |
Pharmaceutical grade | |
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Quantity |
Customized | |
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Packaging standard |
Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
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Lot No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2029 |
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| TEST STANDARD | GB/T24768-2009 Industry. Stnndard | |
| Sturcture |
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Item |
Enterprise standard |
Analysis result |
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Appearance |
White or almost white powder |
Conformed |
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Water content |
≤4.5% |
0.30% |
| Loss on drying |
≤1.0% |
0.15% |
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Heavy Metals |
Pb≤0.5ppm |
N.D. |
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As≤0.5ppm |
N.D. | |
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Hg≤0.5ppm |
N.D. | |
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Cd≤0.5ppm |
N.D. | |
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Purity (HPLC) |
≥99.0% |
99.5% |
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Single impurity |
<0.8% |
0.48% |
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Residue on ignition |
<0.20% |
0.064% |
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Total microbial count |
≤750cfu/g |
80 |
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E. Coli |
≤2MPN/g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (by GC) |
≤5000ppm |
400ppm |
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Storage |
Store in a sealed, dark and dry place at-20 degrees |
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Leuprorelin acetate injection, as a gonadotropin-releasing hormone (GnRH) analog, achieves precise regulation of hormone dependent diseases by inhibiting the pituitary gonadal axis function. The combination therapy strategy has shown significant advantages in gynecology, oncology, reproductive medicine, and other fields, as it can enhance efficacy and reduce the risk of adverse reactions. The following provides a detailed explanation from three dimensions: disease type, selection of combination drugs, and mechanism of action.
Gynecological diseases: combined treatment of endometriosis and adenomyosis
1. Endometriosis: Relieve soreness and reduce recurrence
Core mechanism: Leuprorelin induces ectopic endometrial atrophy by reducing estradiol levels to postmenopausal status (<50pg/mL). However, long-term use may lead to low estrogen syndrome (hot flashes, vaginal dryness) and osteoporosis.
Joint plan:
Lifumin (black cohosh extract): As a plant estrogen regulator, it can alleviate menopausal symptoms such as hot flashes and insomnia. Clinical studies have shown that the combined use of Levofloxacin can reduce patients' modified Kuperman score by 40% without affecting the anti estrogenic effect of leuprorelin.
Yousiming (Quercetin Ethynylestradiol Tablets): Sequential addition of low-dose estrogen (20 μ g Ethynylestradiol) and progesterone (3mg Quercetin) can maintain BMD and reduce vaginal bleeding. A study involving 60 patients with refractory soreness showed that the combination of Yousiming can increase the soreness relief rate from 73.3% to 96.7%, and reduce the incidence of irregular bleeding from 20% to 3.3%.
Zhibai Dihuang Pill (Traditional Chinese Medicine Compound): By nourishing yin and reducing fire to regulate immune function, combined with leuprorelin, it can reduce serum estradiol levels by 47.3% and relieve dysmenorrhea by 85% in patients with endometriosis, significantly higher than the 70% achieved by monotherapy.
2. Uterine adenomyosis: reducing uterine volume and improving symptoms
Core mechanism: Leuprorelin reduces menstrual flow by inhibiting ovrian function, but may also pose a risk of uterine atrophy and ring dislodgement.
Joint plan:
Manyue Le (levonorgestrel intrauterine sustained-release system): Local release of progesterone (52 μ g/d) can induce endometrial atrophy and works synergistically with leuprorelin. Clinical observations have shown that the combined treatment group showed a 25% increase in uterine volume reduction rate compared to the monotherapy group, a 60% decrease in dysmenorrhea score, and a decrease in the rate of Manyue Le detachment from 15% to 5%.
Reverse addition therapy (calcium+vitamin D): In response to the decrease in BMD caused by leuprorelin, the combination of calcium supplementation (1200mg/d) and vitamin D supplementation (800IU/d) can increase the maintenance rate of lumbar spine BMD by 30% and reduce the risk of fractures by 50%.
Malignant tumor: endocrine combined therapy for prostate carcinoma and breast carcinoma
1. Prostate carcinoma: Combination of drug castration and anti androgen therapy
Core mechanism: Leuprorelin blocks carcinoma cell growth by inhibiting teststerone secretion to castration levels (<50ng/dL), but some patients may develop resistance due to androgen receptor mutations.
Joint plan:
Abiraterone (CYP17 inhibitor): Blocking the teststerone synthesis pathway, combined with leuprorelin, can prolong PSA progression time to 18.2 months and increase overall survival by 4.2 months.
Methylteststerone (a synthetic metabolic steroid): For bone metastasis soreness, short-term combination with methylteststerone (10mg/d) can alleviate soreness scores of 30% -50%, but liver enzymes and blood potassium concentrations need to be monitored.
2. breast carcinoma: inhibiting estrogen signaling pathway
Core mechanism: Leuprorelin blocks ER+carcinoma cell proliferation by reducing estradiol levels to<20pg/mL, but the 5-year recurrence rate of monotherapy still reaches 30%.
Joint plan:
Aromatase inhibitors (letrozole/anastrozole): block peripheral estrogen synthesis, combined with leuprorelin, can extend disease-free survival from 36 months to 48 months in premenopausal patients, and increase overall survival rate from 75% to 90%.
Tamoxifen (selective estrogen receptor modulator): for low-risk patients, combined treatment can reduce the risk of contralateral breast carcinoma by 40%, but it is necessary to be alert to endometrial thickening (incidence 5% -8%).
Reproductive Medicine: Precise Regulation of Controlled Ovulation
Core mechanism: During in vitro fertilization (IVF) cycles, leuprorelin prevents premature luteinization of follicles by inhibiting endogenous LH peaks, but may trigger ovrian hyperstimulation syndrome (OHSS).
Joint plan:
FSH (follicle stimulating hormone): Combined with leuprorelin (0.5-1mg/d), it can achieve synchronous follicular development, increase the number of retrieved eggs by 20% -30%, and reduce the incidence of OHSS from 15% to 5%.
Livmin: For young patients, combining Livmin can alleviate anxiety (reduce HAMA score by 25%) and improve treatment compliance.
Pediatric diseases: Delayed intervention for central precocious puberty
Core mechanism: Leuprorelin delays epiphyseal closure by inhibiting GnRH secretion, but may affect growth hormone axis function.
Joint plan:
Growth hormone: For patients with growth retardation, the combination of growth hormone (0.05-0.1IU/kg/d) can increase adult height by 3-5cm without affecting sexual development.
Calcium supplements+vitamin D: Regular monitoring of BMD (once every 6 months), combined supplementation can slow down bone age progression by 60% and predict a 10% increase in adult height.
Leuprorelin acetate injection, as a gonadotropin-releasing hormone (GnRH) agonist, achieves precise regulation of estrogen levels by inhibiting the pituitary gonadal axis function, and has become an important tool for the treatment of gynecological diseases. Its mechanism of action includes inhibiting the secretion of gonadotropins, inducing temporary inhibition of ovrian function, and endometrial atrophy. It has shown significant therapeutic effects in diseases such as endometriosis, uterine fibroids, adenomyosis, and central precocious puberty. The following provides a detailed discussion from three dimensions: disease type, combination therapy strategy, and safety management.
Endometriosis: Relieve soreness and reduce recurrence
Leuprorelin inhibits pituitary secretion of gonadotropins (LH and FSH), reducing ovrian estrogen levels to postmenopausal status (<50pg/mL) and inducing ectopic endometrial atrophy. Clinical studies have shown that continuous medication for 3-6 months can alleviate dysmenorrhea with a relief rate of 70% -85% and reduce the volume of ectopic lesions by 40% -60%. For patients with ovrian chocolate cysts after surgery, leuprorelin can reduce the risk of recurrence to less than 15%, significantly better than the simple surgery group (recurrence rate of 35%).
2. Combination therapy strategy
Reverse addition therapy:
For low estrogen syndrome (hot flashes, vaginal dryness), the combination of pregnancy induced estrone (0.625mg/d) and medroxyprogesterone (2mg/d) can maintain BMD and alleviate symptoms. A randomized controlled trial involving 200 patients showed that the incidence of hot flashes in the combination group decreased from 85% to 30%, and the rate of BMD loss decreased by 50%.
Lifumin (black cohosh extract):
As a plant estrogen regulator, Lifumin can alleviate menopausal symptoms without affecting the anti estrogenic effect of leuprorelin. Clinical observations have shown that the modified Kuperman score in the combination therapy group decreased by 40%, and patient treatment compliance increased by 25%.
Yousiming (Quercetin Ethynylestradiol Tablets):
Sequential addition of low-dose estrogen (20 μ g Ethynylestradiol) and progesterone (3mg Quercetin) can reduce irregular vaginal bleeding while maintaining BMD. Research shows that the combined group had a 20% increase in uterine volume reduction rate compared to the monotherapy group, and the incidence of irregular bleeding decreased from 20% to 5%.
Uterine fibroids: reducing tumor size and improving symptoms
Leuprorelin inhibits the proliferation of uterine smooth muscle cells and induces fibroid atrophy by reducing estrogen levels to<50pg/mL. Clinical data shows that continuous medication for 3 months can reduce the volume of fibroids by 30% -50%, decrease menstrual flow by 50% -70%, and increase hemoglobin levels by 10-20 g/L. For preoperative adjuvant therapy, leuprorelin can reduce the volume of fibroids, lower surgical difficulty, and reduce intraoperative bleeding (average reduction of 200-300mL).
2. Combination therapy strategy
Reverse addition of calcium and vitamin D:
In response to the decrease in BMD caused by leuprorelin, combined supplementation of calcium (1200mg/d) and vitamin D (800IU/d) can increase the maintenance rate of lumbar spine BMD by 30% and reduce the risk of fractures by 50%. A long-term follow-up study showed that the bone loss rate in the combination group was reduced by 40% compared to the monotherapy group, and it did not affect the reduction of fibroids.
Manyue Le (levonorgestrel intrauterine sustained-release system):
Local release of progesterone (52 μ g/d) can synergistically induce endometrial atrophy. Combined with leuprorelin, it can increase the uterine volume reduction rate to 60% and relieve dysmenorrhea by 90%. For patients with submucosal fibroids and excessive menstruation, combination therapy can significantly reduce the emergency curettage rate (from 30% to 5%).
Uterine adenomyosis: relieving soreness and improving fertility function
Leuprorelin reduces menstrual flow and alleviates dysmenorrhea and chronic pelvic soreness caused by adenomyosis by inhibiting ovarian function. Clinical observations have shown that continuous medication for 6 months can reduce the VAS score of dysmenorrhea from 8 points to 3 points and reduce uterine volume by 20% -30%. For patients with combined infertility, leuprorelin can improve the pelvic environment and increase the natural pregnancy rate (from 10% to 25%).
2. Combination therapy strategy
Manyue Le combination therapy:
Placing Manyue Le after induction of amenorrhea by leuprorelin can maintain long-term low estrogen status and reduce drug withdrawal bleeding. Research shows that the 5-year cumulative recurrence rate of the combination group is 40% lower than that of the monotherapy group, and the quality of life score of patients is improved by 30%.
Reverse addition of Levofloxacin:
For young patients, combining Levofloxacin can alleviate anxiety (reduce HAMA score by 25%) and improve treatment compliance. A multicenter study showed that the interruption rate of combined treatment decreased from 20% to 5%, without affecting the reduction of adenomyosis lesions.
FAQ
1. Does it have a unique drug delivery system?
It has a long-acting sustained-release injection formulation, which can continuously release the drug for 1 to 6 months after a single injection, improving medication compliance and stability.
2. What are the unique features of its mechanism of action?
It belongs to the "GnRH agonist" category. By first providing a brief stimulation and then subsequently maintaining a continuous inhibition of the pituitary-gonadal axis, it achieves the "down-regulation" effect. This biphasic action mechanism is quite distinctive among similar drugs.
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