Cetrorelix Acetate CAS 120287-85-6

In the treatment of prostate cancer, it is usually combined with other treatment methods such as surgery, radiotherapy, and chemotherapy to provide a more comprehensive treatment plan.

This mechanism has significant implications for improving the success rate of in vitro fertilization (IVF).
Specifically, ovurelix downregulates the sensitivity of the pituitary gland to GnRH by binding to the gonadotropin-releasing hormone (GnRH) receptor in the anterior pituitary gland, thereby reducing the release of gonadotropins. This inhibitory effect enables multiple follicles in the ovary to develop in a relatively synchronized state, avoiding asynchronous follicular development and thus improving the quantity and quality of mature eggs obtained.

In the practical operation of assisted reproductive therapy, the use of cetrorelix acetate is usually after gonadotropin-releasing hormone analogs (GnRHa). GnRHa, as a regulator, can initially reduce the sensitivity of the pituitary gland to GnRH, laying the foundation for subsequent treatment with ovurelix. By combining GnRHa with ovurelix, doctors can more accurately control the process of superovulation, ensuring that follicles develop and mature under ideal time and conditions.

(2) Reproductive medicine research: It also has important applications in reproductive medicine research. It can be used to study the secretion and regulatory mechanisms of gonadotropins, as well as to explore the etiology and treatment methods of infertility. Studying the mechanism of action and therapeutic effect of this substance helps to gain a deeper understanding of the physiological and pathological status of the reproductive system, providing new ideas and methods for improving reproductive health and fertility.

(3) Pharmacological research: It is also used in pharmacological research to explore the pharmacological effects and mechanisms of GnRH receptor antagonists.

Through pharmacological research, we can further understand the characteristics of action and potential therapeutic targets of GnRH receptor antagonists in vivo, providing useful information and guidance for drug design and development.

In addition to the above purposes, there may also be some other applications. For example, it can be used for the establishment and research of animal models to understand the pharmacological and physiological mechanisms of GnRH receptor antagonists in animals. In addition, Cetrorelixacetate may also be used in some clinical trials and studies to evaluate its efficacy and safety in specific diseases or situations.

Application in Polycystic Ovary Syndrome (PCOS)

Polycystic ovary syndrome (PCOS) is a highly prevalent endocrine and metabolic disorder in women of reproductive age. It is typically characterized by hyperandrogenemia and dysfunction of the hypothalamic-pituitary-ovarian axis, commonly manifested as excessive follicle recruitment, uneven follicle size, and asynchronous follicular development. During ovulation induction, an early LH surge and premature luteinization of follicles are highly prone to occur, which not only reduces the conception rate but also greatly increases the risk of Ovarian Hyperstimulation Syndrome (OHSS).

Cetrorelix acetate is a third-generation GnRH antagonist. It binds competitively to pituitary GnRH receptors with high selectivity, rapidly inhibits the abnormal secretion of endogenous luteinizing hormone, and stably suppresses aberrant endocrine fluctuations. In assisted reproduction and ovulation induction cycles for PCOS patients, this drug can effectively regularize the rhythm of follicular development, improve asynchronous follicle growth, facilitate the preferential maturation of dominant follicles, and avoid spontaneous premature ovulation and Luteinized Unruptured Follicle Syndrome (LUFS).

Meanwhile, it can effectively control excessive ovarian response, reduce synchronous over-proliferation of multiple follicles, and significantly lower the risk of mild, moderate and severe OHSS. It is especially suitable for PCOS patients with high ovarian response constitution, obese phenotype and refractory conditions. Compared with the GnRH agonist protocol, the cetrorelix regimen features a shorter cycle, rapid onset of hormonal suppression, and no drug-induced flare-up effect. Endocrine and ovarian functions can recover quickly after drug discontinuation, offering better clinical tolerability and applicability.

Application in Benign Prostatic Hyperplasia (BPH) (Clinical Research Stage)

The onset and progression of Benign Prostatic Hyperplasia (BPH) are highly dependent on the persistent stimulation of testosterone and dihydrotestosterone. Long-term androgen action promotes hyperplasia of the prostatic glands and stroma, compresses the urethra, and induces lower urinary tract symptoms such as frequent urination, nocturia, straining to urinate, thin urinary stream, and increased residual urine volume.

Unlike GnRH agonists, it does not cause an initial testosterone flare effect, so it will not aggravate dysuria and prostate symptoms in the short term, with a stable and safe pharmacological profile. Although it has not been officially approved for the BPH indication and remains in the clinical research stage, multiple clinical trials have confirmed that it can significantly increase maximum urinary flow rate, reduce post-void residual urine volume, relieve nocturia and frequent urination, and delay the pathological progression of prostatic hyperplasia. For middle-aged and elderly BPH patients who are intolerant to α-blockers and 5α-reductase inhibitors, or unwilling to undergo surgical treatment, ovurelix possesses important value in clinical research and potential clinical application.

Application in Ovarian Cancer (Clinical Exploration Stage)

Most ovarian cancers are hormone-dependent malignant tumors. Gonadotropins and estrogen can regulate the proliferation, invasion, migration and angiogenesis of ovarian cancer cells. Advanced ovarian cancer is characterized by high chemotherapy drug resistance and high recurrence rate, with limited clinical treatment options.

Through endocrine regulation, ovurelix inhibits the secretion of LH, FSH and estrogen, blocks the hormone microenvironment required for tumor growth, directly suppresses the proliferative activity of ovarian cancer cells, and weakens their invasion and metastasis capabilities.

At present, it is mainly in the stage of clinical exploration and clinical trials, and is mostly combined with platinum-based, taxane-standard chemotherapy drugs and anti-angiogenic targeted agents. Combined medication exerts a synergistic effect, enhances the sensitivity of tumor cells to chemotherapy, reverses drug resistance, shrinks solid tumor lesions, controls malignant ascites formation, and prolongs progression-free survival in patients with advanced and recurrent ovarian cancer. In addition, it can regulate the body's inflammatory and immune microenvironment, inhibit tumor angiogenesis, and reduce the risk of distant metastasis, providing a novel adjuvant therapeutic strategy and research direction for the comprehensive treatment of drug-resistant and recurrent ovarian cancer.