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Goserelin acetate is a hormone based drug that is a white to grayish white powder, odorless, and tasteless. Its molecular formula is C61H88N18O16, CAS 145781-92-6, and molecular weight is 1329.49. The solubility in water is 20 mg/mL, and it is clear and colorless. In addition, it is also soluble in organic solvents such as methanol, ethanol, acetone, etc. It is a synthetic decapeptide compound with a complex chemical structure. Its molecule contains multiple functional groups such as amino acid residues and ester groups, which have a certain impact on its stability, solubility, and other properties. It is a hormone drug with multiple uses, and is widely used in the treatment of prostate cancer, endometriosis, breast cancer and other fields.
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Customized Bottle Caps And Corks:
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Chemical Formula |
C61H88N18O16 |
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Exact Mass |
1329 |
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Molecular Weight |
1329 |
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m/z |
1329 (100.0%), 1330 (66.0%), 1331 (21.4%), 1270 (6.6%), 1271 (4.0%), 1272 (3.3%), 1271 (2.9%), 1272 (1.8%), 1272 (1.3%) |
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Elemental Analysis |
C, 55.11; H, 6.67; N, 18.96; O, 19.25 |
In the field of chemistry, it has some specific uses. The following is a detailed description of its application in the field of chemistry:
Synthetic research&Drug research and development
- it is an important compound in drug research and development, which is used to develop drugs to treat endocrine factor dependent diseases such as prostate cancer, endometriosis and breast cancer. Studying its mechanism of action and efficacy can help discover new therapeutic targets and methods, and promote the progress of drug research and development.
- It is a gonadotropin-releasing endocrine factor(GnRH) antagonist that can be used to study the mechanism of action and signal transduction pathways of GnRH receptors. By using Goserelin acetate, the regulatory effect of GnRH on gonadal endocrine factorsecretion can be studied, further understanding the endocrine factor regulatory mechanisms in the reproductive system.
Chemical synthesis&Biological analysis
- Synthesis involves multiple chemical reactions and steps, requiring carefully designed synthesis routes and precise operations. By studying and improving its synthesis methods, it is helpful to improve synthesis efficiency and yield, providing support for the development of chemical synthesis technology.
- Used in biological analysis to detect the expression and function of gonadotropin-releasing endocrine factor receptors. By using this substance as a probe, biological behaviors such as the localization, expression levels, and signal transduction of GnRH receptors in cells can be studied.
Pharmacological research
Used in pharmacological research to study the effects and effects of drugs on the reproductive system. By using this substance, the effects of the drug on gonadal endocrine factor secretion and reproductive organ function can be observed, thereby evaluating the efficacy and safety of the drug.
(1) Pharmacological research mainly focuses on the following aspects:
Hormone regulation: It is an antagonist of gonadotropin-releasing endocrine factor(GnRH) that can inhibit the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). By regulating the levels of these hormones, it is possible to affect the function of the reproductive system, such as inhibiting ovulation and testosterone synthesis.
(2) Tumor treatment: in terms of tumor treatment, it is mainly used for endocrine factor dependent diseases such as prostate cancer, endometriosis and breast cancer. By inhibiting the release of LH and FSH, serum testosterone or estradiol levels can be reduced, thereby reducing tumor volume, improving symptoms.
(3) Assisted reproductive technology: In assisted reproductive technology, it is used to control the release of gonadotropins to help infertile couples achieve fertility. By regulating the levels of LH and FSH, ovulation can be promoted and the success rate of assisted reproductive technologies.
(4) Endometriosis and uterine fibroids: Endometriosis and uterine fibroids are common gynecological diseases. By inhibiting the release of LH and reducing serum estradiol levels, symptoms of endometriosis and uterine fibroids can be alleviated.
(5) Infertility treatment: In the treatment of female infertility, it can be used to control the release of gonadotropins, thereby promoting ovulation. By regulating the levels of gonadotropins, it can help improve fertility and increase the chances of successful pregnancy.
Explain the principle of action
The principle of action of Goserelin acetate mainly involves the regulation of endocrine factor. It is a synthetic analogue of luteinizing hormone releasing hormone (GnRH) that, when used for a long time, can inhibit the secretion of luteinizing hormone in the pituitary gland, leading to a decrease in male serum testosterone and female serum estradiol. This inhibitory effect can cause most prostate tumors to regress and improve symptoms. For female patients, it reduces serum estradiol levels by inhibiting LH release, thereby alleviating symptoms of endometriosis and uterine fibroids.
The mechanism of action mainly involves the following aspects:
1. Hormone regulation
By simulating the endocrine factor regulatory system in the body, a chemical substance similar to gonadotropin-releasing hormone (GnRH) is continuously released. This can lead to sustained stimulation of the GnRH receptors in the pituitary gland, thereby reducing the secretion of gonadotropins (LH and FSH). By regulating the levels of these endocrine factor, they can affect the function of the reproductive system and can be used to treat endocrine factor related diseases.
2. Tumor treatment
In the treatment of hormone dependent diseases such as prostate cancer, the therapeutic effect is achieved by reducing serum testosterone levels. By inhibiting the release of LH and reducing the production of testosterone, it helps to reduce tumor volume and improve symptoms. For other hormone dependent diseases such as breast cancer, the mechanism of action also involves the regulation of related hormones, thus inhibiting the growth and spread of tumors.
3. The treatment of endometriosis and uterine fibroids
Endometriosis and uterine fibroids are common gynecological diseases. By inhibiting the release of LH and reducing serum estradiol levels, symptoms of endometriosis and uterine fibroids can be alleviated. This mechanism of action helps to improve the pain and discomfort symptoms of patients and improve their quality of life.
4. Pregnancy treatment and assisted reproductive technology
In the treatment of female infertility and assisted reproductive technology, the mechanism of action involves controlling the release of gonadotropins, thereby promoting ovulation. By regulating the levels of gonadotropins, it can help improve fertility and increase the chances of successful pregnancy.
toxicological effects
In a 1-year and 23 week recovery period rat animal study, subcutaneous implantation of approximately 80mcg/kg/day and 150mcg/kg/day (male rats) or 50mcg/kg/day and 100mcg/kg/day (female rats) every 4 weeks resulted in an increased incidence of adenomas in the body. In a study of male rats at 72 weeks or male rats at 101 weeks, subcutaneous implantation of similar doses of this product also resulted in an increased incidence of pituitary adenomas. The correlation between rat pituitary adenoma and human body is not yet clear.
In mouse studies, subcutaneous implantation of this product (dosage: 2400mcg/kg/day, once every 3 weeks for 2 years) can lead to an increase in the incidence of spinal and femoral tissue cells. It is not yet possible to calculate the multiple of human dose exposure based on the obtained animal research data. In mice, long-term repeated use of doses several times higher than those used by humans resulted in changes in tissue structure in the digestive tract, manifested as benign proliferation of the pyloric region of the stomach and proliferation of insulin cells (also reported as spontaneous injury). The relationship between these phenomen.
A real case about the use of this acetate in the treatment of breast cancer
Medical History and Diagnosis:
Ms. Zhang was diagnosed with ductal invasive carcinoma of the right breast in 2015 and underwent modified radical surgery. Postoperative pathology results showed pT4N2M1 with lymph node metastasis. After chemotherapy and radiotherapy, Ms. Wang has been taking oral tamoxifen for adjuvant therapy. However, in 2018, she found a mass with swelling on the right chest wall, and swelling and limited movement of the right upper limb. After further examination, she was diagnosed with postoperative local recurrence of right breast cancer with bone metastasis.
Initial chemotherapy:
Ms. Wang was first treated with chemotherapy regimen (epirubicin hydrochloride + cyclophosphamide + paclitaxel liposome) + tamoxifen + zoledronic acid. After three cycles of chemotherapy, the condition remained stable, but breast ultrasound still showed a tumorigenic lesion.
Adjustment of chemotherapy regimen:
Subsequently, her treatment regimen was adjusted to chemotherapy (paclitaxel liposome + lopressor) + letrozole + this acetate + zoledronic acid. At the end of the 6th cycle of chemotherapy,She developed fever and other adverse reactions. After anti-infection, leukocyte, platelet and hemoglobin boosting treatments, the blood routine indexes returned to normal.
Follow-up chemotherapy and maintenance therapy:
The next chemotherapy regimen was chemotherapy (paclitaxel) + trastuzumab + letrozole + this acetate + zoledronic acid. After completing chemotherapy, Ms. Zhang received maintenance therapy based on trastuzumab (intravenous) + capecitabine tablets (oral) + letrozole + acetate + zoledronic acid.
This acetate was applied:
This acetate was used in her treatment regimen as an important endocrine therapy drug. It acts to inhibit the growth of breast cancer by inhibiting the release of gonadotropins from the hypothalamus and reducing the ovaries' production of estrogen. It was administered subcutaneously every 28 days in the form of 3.6 mg of injectable implants.
Therapeutic Efficacy Evaluation:
After the implementation of the above treatment program, Ms. Zhang's condition was significantly relieved. Breast ultrasound results showed that the hypoechoic area on the right chest wall gradually decreased and eventually no definite abnormal echoes were seen. This indicates that goserelin acetate has significant efficacy in the treatment of breast cancer.
This case demonstrates the effective use of this med in the treatment of breast cancer. By combining with other chemotherapeutic drugs and endocrine therapeutic drugs, this med can significantly reduce the patient's estrogen level and inhibit the growth and spread of breast cancer cells, thus improving the therapeutic efficacy and prolonging the patient's survival.
Please note that the above cases are only examples and do not mean that all breast cancer patients can obtain the same treatment effect. The treatment plan should be personalized according to the patient's specific situation and under the guidance of the doctor.
FAQ
What is goserelin acetate used for?
This is approved to treat: Breast cancer that is advanced. It is used as palliative treatment in premenopausal and perimenopausal women. Prostate cancer.
Is it a chemotherapy?
No, goserelin (brand name Zoladex) is not chemotherapy; it is a type of hormone therapy (endocrine therapy). It works as a luteinizing hormone-releasing hormone (LHRH) agonist, reducing estrogen in women or testosterone in men to slow cancer growth. It is often used to treat breast and prostate cancer.
What are the side effects of this?
Goserelin (Zoladex) is a hormone therapy that causes temporary menopause in women or lowers testosterone in men, commonly causing hot flashes, fatigue, weight gain, joint pain, decreased libido, and injection site reactions. Serious but rare side effects include bone density loss, depression, and blood pressure changes.
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