Histrelin Acetate,The Chinese name is acetanilide, which is an artificially synthesized peptide drug that belongs to the class of gonadotropin-releasing hormone (GnRH) analogs. It has a wide range of applications in the medical field, especially playing an important role in the treatment of certain hormone dependent diseases. It is a nine peptide analogue of GnRH. GnRH is a peptide hormone secreted by the hypothalamus that plays a crucial role in regulating the reproductive system. Its mechanism of action is mainly based on its excitatory effect on GnRH receptors. GnRH receptors are widely distributed on gonadotropin cells in the anterior pituitary gland. When it enters the bloodstream, it binds to GnRH receptors on these cells, activating intracellular signaling pathways and leading to increased release of luteinizing hormone (LH) and follicle stimulating hormone (FSH).
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Histrelin COA
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| Certificate of Analysis | ||
| Compound name | Histrelin | |
| Grade | Pharmaceutical grade | |
| CAS No. | 76712-82-8 | |
| Quantity | 15g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202501090031 | |
| MFG | Jan 9th 2025 | |
| EXP | Jan 8th 2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.36% |
| Loss on drying | ≤1.0% | 0.27% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.90% |
| Single impurity | <0.8% | 0.48% |
| Total microbial count | ≤750cfu/g | 98 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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| Chemical Formula: | C66H86N18O12 |
| Exact Mass: | 1322.67 |
| Molecular Weight: | 1323.53 |
| m/z: | 1322.67 (100.0%), 1323.67 (71.4%), 1324.67 (25.1%), 1323.66 (6.6%), 1325.68 (5.8%), 1324.67 (4.7%), 1324.67 (2.5%), 1325.67 (1.8%), 1325.67 (1.7%) |
| Elemental Analysis: | C, 59.89; H, 6.55; N, 19.05; O, 14.51 |

Histrelin Acetate,The chemical name acetaminophen is a nine peptide analogue of gonadotropin-releasing hormone (GnRH), belonging to the GnRH receptor agonist. It simulates the action of natural GnRH, binds to GnRH receptors in the anterior pituitary gland, regulates the release of gonadotropins, and thus affects sex hormone levels.
Prostate cancer treatment
Prostate cancer is one of the most common malignant tumors in men. Its incidence rate and mortality rate are among the highest in the world. With the aging of the population and the continuous progress of screening technology, the incidence rate of prostate cancer is increasing year by year. Prostate cancer not only seriously affects the quality of life of patients, but also brings a heavy burden to families and society. Traditional treatment methods include surgery, radiation therapy, chemotherapy, etc., but these methods have certain limitations in the treatment of advanced prostate cancer. Histrelin, as a novel therapeutic drug, has brought new hope for the treatment of prostate cancer.
Basic Information

Chemical Structure and Properties
Histrelin is a nine peptide analogue of gonadotropin-releasing hormone (GnRH) with a molecular weight of 1383.58, a molecular formula of C66H86N18O12 · XC2H4O2, and a CAS number of 220810-26-4. It is a white to off white solid, soluble in water, with a solubility of ≥ 10mg/mL.
Mechanism of Action
Histrelin is a GnRH receptor agonist. Under normal circumstances, the hypothalamus secretes GnRH, which acts on the anterior pituitary gland to promote the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH), thereby regulating the secretion of gonadal hormones. After entering the human body, Histrelin continuously stimulates the release of LH and FSH from the anterior pituitary gland, which initially leads to a brief increase in LH and FSH levels, thereby increasing testosterone levels. However, after continuous use, the GnRH receptors in the anterior pituitary gland are overstimulated, leading to desensitization and inhibition of LH and FSH secretion, resulting in a significant decrease in testosterone levels. Due to the fact that testosterone can promote the growth of prostate cancer cells, reducing testosterone levels can help slow down the growth rate of prostate cancer cells and inhibit tumor spread.

Clinical application in the treatment of prostate cancer
Indications
Histrelin is mainly used for palliative treatment of advanced prostate cancer. Late stage "refers to cancer that has spread to other parts of the body. As a palliative therapy, it helps alleviate symptoms such as difficulty urinating and bone pain, improving the quality of life for patients with advanced prostate cancer. Although it cannot cure this disease, it can effectively control the development of the condition and alleviate the patient's pain.
Usage and Dosage
Histrelin is used in the form of an implant, directly inserted under the skin (subcutaneous), and healthcare workers typically place it between the biceps and triceps muscles in the inner area of the upper arm. A Histrelin Acetate implant typically lasts for 12 months, after which it must be removed before inserting other implants. This long-term administration method reduces the number of times patients take medication and improves their medication compliance.
Combined application with other treatment methods

Combination with radiotherapy
Radiotherapy is one of the commonly used treatment methods for prostate cancer, which kills cancer cells through high-energy radiation. The combination of Histrelin and radiotherapy can enhance the therapeutic effect. Radiotherapy can directly act on local tumors, killing cancer cells, while Histrelin controls the condition from a systemic perspective by reducing testosterone levels, inhibiting the growth and spread of tumor cells. The combination of the two can have a synergistic effect, improving the local control rate of tumors and the survival rate of patients.
Combination with chemotherapy
Chemotherapy is a treatment method that uses chemical drugs to kill cancer cells. Although chemotherapy has relatively limited efficacy in treating prostate cancer, its combination with Histrelin can have a certain synergistic effect. Histrelin reduces testosterone levels, putting tumor cells in a relatively sensitive state, making it easier for chemotherapy drugs to work and improving the efficacy of chemotherapy. Meanwhile, Histrelin can also alleviate some of the side effects of chemotherapy, such as improving patients' physical condition and enhancing their tolerance to chemotherapy.


Combination with Immunotherapy
Immunotherapy has been a hot topic in the field of cancer treatment in recent years, which recognizes and kills cancer cells by activating the body's immune system. The immunosuppressive tumor microenvironment of prostate cancer limits the effectiveness of immunotherapy. Histrelin can reduce testosterone levels, regulate the tumor microenvironment, alleviate immune suppression, and enhance the effectiveness of immunotherapy. For example, when used in combination with prostate cancer vaccines, Histrelin can improve the tumor microenvironment, making it easier for the vaccine to activate the body's immune response and enhance its ability to kill tumor cells.
The advantages of Histrelin in treating prostate cancer

Efficiency
Clinical studies have shown that Histrelin can rapidly and effectively reduce testosterone levels, achieving chemical castration. Reduce the patient's testosterone levels to extremely low levels in a short period of time, effectively inhibiting the growth and spread of prostate cancer cells. Compared with traditional castration surgery, Histrelin does not require surgery, avoiding the trauma and complications caused by surgery, while also achieving similar therapeutic effects.
Long term effectiveness
The Histrelin implant has a duration of action of up to 12 months, and patients only need to replace the implant once a year to maintain the treatment effect. This long-term administration method reduces the number of times patients take medication and improves medication compliance, especially suitable for patients with poor memory or limited self-care ability. At the same time, long-term effectiveness also reduces the trouble of frequent medical treatment for patients and lowers medical costs.


Security
Compared with traditional treatment methods, Histrelin has higher safety. It avoids the risks of surgery and the serious side effects of chemotherapy and radiation therapy. Although there may be some local reactions during use, such as redness, swelling, and pain at the implantation site, these reactions are usually mild and can be relieved through appropriate treatment. In addition, Histrelin has minimal impact on important organs such as the cardiovascular system, liver, and kidneys, making it suitable for most patients to use.
Improving Quality of Life
Patients with advanced prostate cancer often have symptoms such as difficulty urinating and bone pain, which seriously affect their quality of life. Histrelin acetate can effectively alleviate these symptoms and alleviate the pain of patients. At the same time, it can also improve the physical, mental, and sexual function of patients, enhance their quality of life, and enable them to better enjoy life.

Frequently Asked Questions
What is histrelin acetate used for?
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A drug used under the brand name Vantas as palliative therapy for advanced prostate cancer. Histrelin acetate initially causes the pituitary gland to make more luteinizing hormone (LH) and follicle-stimulating hormone (FSH), temporarily increasing testosterone levels in men.
Is histrelin a puberty blocker?
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The histrelin subdermal implant is FDA-approved for treatment of precocious puberty for 1 year. These implants are used off-label in transgender youth, and the effective duration of treatment has not been studied.
What is the generic for histrelin implant?
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Supprelin LA. Supprelin LA (histrelin) helps prevent early puberty in children 2 years of age and older. The medication works well to delay puberty, but it's an implant that is placed under your skin during a minor surgical procedure.
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