It is an effective antagonist of the LH-RH receptor, which can control the stimulation of the ovaries, prevent premature release of immature follicles, and facilitate conception. Therefore, it is often used as an injectable contraceptive of cyproterone acetate.
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Cetrorelix acetate is a potent synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), specifically engineered as a GnRH antagonist. Its chemical structure features a modified amino acid sequence that allows it to bind competitively and reversibly to GnRH receptors in the anterior pituitary gland without triggering receptor activation or subsequent hormone release. The molecular formula of Cetrorelix acetate is typically represented as C60H83N17O15S·CH3COOH, reflecting the peptide backbone combined with an acetic acid counterion which stabilizes the salt form for pharmaceutical use. The substance is registered under CAS number 141266-89-3.
Clinically, Cetrorelix acetate serves a critical role in assisted reproductive technologies (ART), particularly in controlled ovarian stimulation protocols for in vitro fertilization (IVF) and intracytoplasmic sperm injection (ICSI). During these procedures, patients are often treated with follicle-stimulating hormone (FSH) to induce the growth of multiple ovarian follicles. However, the rising estrogen levels from developing follicles can trigger a premature surge in luteinizing hormone (LH), leading to premature ovulation and potential cycle cancellation. Cetrorelix acetate prevents this by rapidly suppressing LH secretion upon binding to pituitary receptors, thereby maintaining the follicles in a pre-ovulatory state until they reach maturity.
The drug is administered via subcutaneous injection, usually starting on day five or six of the stimulation cycle, depending on individual patient response and serum estradiol levels. Its rapid onset of action distinguishes it from older GnRH agonists, which require a "flare-up" period before downregulation occurs, making Cetrorelix an ideal choice for shortening treatment duration and reducing the risk of OHSS (ovarian hyperstimulation syndrome). Beyond fertility treatments, research continues to explore its potential in managing conditions driven by sex hormones, such as advanced prostate cancer, although its primary indication remains within reproductive medicine. As a generic active pharmaceutical ingredient, it is widely manufactured for global distribution to support millions of ART cycles annually, offering a reliable solution for preventing premature ovulation and optimizing pregnancy outcomes.