Cetrorelix Acetate 0.25 Mg

Ovarian cancer is a highly estrogen-dependent malignant tumor. GnRH antagonists can suppress the hypothalamic-pituitary-ovarian axis, reduce circulating estrogen levels, and block proliferative signaling in tumor cells.Cetrorelix acetate 0.25 mg administered subcutaneously once daily rapidly inhibits LH secretion, markedly reducing ovarian estrogen synthesis. Deprived of hormonal stimulation, tumor cells undergo growth arrest and apoptosis.

Clinically, it is mainly used as second-line endocrine therapy for advanced epithelial ovarian cancer, or in combination with chemotherapy and targeted agents for maintenance treatment in patients with platinum-resistant recurrent disease. It can reduce the tumor marker CA125 level and delay disease progression, especially suitable for elderly or frail patients who cannot tolerate intensive chemotherapy.Compared with GnRH agonists, the 0.25 mg formulation has no initial flare effect, takes effect within 4–12 hours after administration, avoids the risk of transient tumor proliferation, and offers better safety.

Prostate cancer growth relies on testosterone, and androgen deprivation is the core treatment for locally advanced and metastatic prostate cancer.It administered subcutaneously once daily inhibits pituitary LH secretion, blocks testicular testosterone synthesis, and rapidly reduces serum testosterone to castrate levels (< 50 ng/dL).

Its mechanism is direct and reversible, without the drawback of initial testosterone elevation seen with agonists. Rapid castration is achieved within 3–5 days of treatment, significantly lowering prostate-specific antigen (PSA) levels, shrinking tumor volume, and relieving symptoms such as bone pain and dysuria.The daily 0.25 mg dose maintains stable hormonal suppression, avoiding fluctuations caused by high-dose intermittent administration. It is indicated for primary castration therapy in advanced prostate cancer, second-line endocrine therapy for castration-resistant prostate cancer, and preoperative tumor shrinkage to reduce surgical risk.

Uterine fibroids are estrogen-dependent benign tumors, in which a high-estrogen environment promotes fibroid cell proliferation and angiogenesis.Cetrorelix acetate 0.25 mg administered subcutaneously once daily, or a single 3 mg dose every 28 days combined with 0.25 mg maintenance therapy, rapidly suppresses estrogen secretion, placing fibroids in a low-hormone state and reducing volume by 30%–50%.

Clinically, it is mainly used for preoperative preparation, especially in patients with large fibroids (> 5 cm in diameter) accompanied by menorrhagia, anemia, or compressive symptoms. After 3–6 months of treatment, intraoperative blood loss is reduced and surgical difficulty is lowered; after fibroid shrinkage, minimally invasive surgery can be selected, shortening hospital stay.For perimenopausal patients, the 0.25 mg formulation can be used for long-term low-dose maintenance to relieve symptoms such as prolonged menstruation, heavy menstrual bleeding, and abdominal pain, delay fibroid progression, and avoid surgical trauma.

The development and progression of endometriosis are closely related to estrogen, as ectopic endometrial tissue depends on estrogen for proliferation and invasion.The product administered subcutaneously once daily rapidly lowers estrogen levels, causing atrophy and necrosis of ectopic endometrial lesions, and significantly relieving core symptoms including dysmenorrhea, chronic pelvic pain, and dyspareunia.

Compared with traditional GnRH agonists, the 0.25 mg daily dose acts faster (estrogen inhibition within 24 hours of administration), has no flare effect, and causes milder hypoestrogenic symptoms (hot flashes, night sweats). It is suitable for short-term preoperative treatment (3 months) or long-term intermittent therapy.For patients with recurrent endometriosis, those intolerant to surgery, or for postoperative recurrence prevention, the 0.25 mg formulation can serve as a long-term management strategy, combined with add-back therapy (low-dose estrogen-progestin) to reduce side effects such as bone loss.

Benign prostatic hyperplasia is a common disease in middle-aged and elderly men. Its progression is closely associated with dihydrotestosterone (DHT), which is converted from testosterone by 5α-reductase. Chronic stimulation by DHT leads to prostatic cell hyperplasia, resulting in urethral compression and voiding dysfunction.

Cetrorelix acetate 0.25 mg administered subcutaneously once daily inhibits pituitary LH secretion, reduces testicular testosterone production, lowers DHT synthesis at the source, and causes atrophy and volume reduction of hyperplastic prostatic tissue.

Clinically, the 0.25 mg formulation is mainly used as adjuvant therapy for patients with moderate to severe BPH, especially those with elevated PSA and suspected prostate cancer risk, or those intolerant to 5α-reductase inhibitors (e.g., finasteride).

After 3–6 months of treatment, the International Prostate Symptom Score (IPSS) is significantly improved, relieving symptoms such as urinary frequency, urgency, dysuria, and nocturia, increasing maximum urinary flow rate, and reducing the risk of acute urinary retention.When combined with α-blockers, 0.25 mg provides long-term stable hormonal suppression, preventing symptom rebound and supporting long-term conservative management of BPH.The daily 0.25 mg dose delivers steady hormonal control with no significant side effects such as sexual dysfunction or breast tenderness, resulting in better patient compliance than high-dose GnRH antagonists.