Nafarelin Acetate

2.1 Benign Prostatic Hyperplasia (BPH)

Benign prostatic hyperplasia is a common urological disorder in middle-aged and elderly males. Its pathogenesis is closely associated with serum testosterone levels. After testosterone is converted into dihydrotestosterone (DHT), it stimulates hyperplasia of the prostatic stroma and glands, leading to prostate enlargement, urethral compression, and lower urinary tract symptoms such as frequent urination, nocturia, dysuria, and thin urinary stream. Severe cases may develop complications including urinary retention and urinary tract infections.

As a LHRH agonist, nafarelin acetate acts on the pituitary gland long-term to inhibit gonadotropin secretion, thereby reducing testosterone synthesis and lowering circulating testosterone and dihydrotestosterone levels.

This suppresses the growth of hyperplastic prostatic tissue, shrinks prostate volume, and relieves lower urinary tract obstruction symptoms.

Compared with 5α-reductase inhibitors such as Finasteride, it exerts a faster onset of action in reducing prostate volume. Symptomatic improvement is usually observed within 4–6 weeks of administration, with optimal therapeutic effects achieved at approximately 3 months, reducing prostate volume by 15%–20%.

It also significantly decreases the International Prostate Symptom Score, increases maximum urinary flow rate, and reduces residual urine volume. Clinically, the product is mostly used for short-term intervention in patients with moderate to severe benign prostatic hyperplasia, especially those with severe symptoms requiring rapid relief of obstruction, who are temporarily unsuitable for surgical treatment or intolerant to long-term oral medications - such as elderly patients complicated with cardiovascular diseases or hepatorenal insufficiency.

It should be noted that the treatment course of the product for benign prostatic hyperplasia must be strictly controlled, generally not exceeding 6 months. Long-term use may cause adverse reactions including decreased libido, osteoporosis, and hot flashes. Symptom recurrence may occur in some patients after drug withdrawal. Therefore, an individualized treatment regimen should be formulated based on the patient's specific condition, combined with lifestyle interventions such as avoiding prolonged sitting and reducing spicy and irritating diets to enhance therapeutic efficacy.

2.2 Endocrine Therapy for Advanced Prostate Cancer

Prostate cancer is a common malignant tumor of the male reproductive system, and its growth is highly androgen-dependent. Accordingly, androgen deprivation therapy (ADT) serves as the core treatment for advanced prostate cancer. The therapeutic goal is to reduce serum testosterone to castration level (<50 ng/dL), thereby inhibiting tumor cell growth and metastasis, prolonging patient survival, and alleviating clinical symptoms.

As a pivotal agent in ADT regimens, the product specifically binds to pituitary LHRH receptors to chronically inhibit the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It blocks testicular testosterone synthesis and rapidly reduces testosterone to castration levels, achieving pharmacological castration.

3.1 Puberty Blockade Therapy (Transgender Medicine)

In international clinical practice, one of the key applications of the product is as a puberty blocker for interventional treatment in transgender adolescents. Transgender adolescents refer to those whose gender identity is inconsistent with their biological sex. Upon the onset of puberty, the development of secondary sexual characteristics corresponding to their natal sex - such as Adam's apple prominence and voice deepening in natal males, and breast development and menarche in natal females - causes severe psychological distress, even triggering anxiety, depression and other mental disorders, and impairing physical and mental health as well as social adaptation.

By inhibiting pituitary gonadotropin secretion, the product blocks the synthesis of sex hormones related to natal sex, thereby suppressing the development of secondary sexual characteristics. It reserves sufficient time for transgender adolescents to undergo psychological assessment, gender identity confirmation and subsequent hormone therapy.

Clinical studies have demonstrated that nafarelin acetate features high safety in puberty blockade for transgender adolescents and can effectively delay the development of secondary sexual characteristics.

Sex hormone secretion can gradually recover after drug withdrawal without causing irreversible damage to reproductive function. This therapeutic regimen must be implemented under the joint guidance of professional endocrinologists and psychologists. A comprehensive assessment of the adolescent's gender identity is conducted first; treatment with the product is initiated only after meeting the therapeutic indications. During treatment, regular monitoring of sex hormone levels, bone age and psychological status is required, with dosage and treatment duration adjusted according to individual conditions.

At present, the product has been recommended as a first-line agent for puberty blockade by transgender medical guidelines in multiple countries and regions, including the Endocrine Society and the European Society of Endocrinology. Its application provides a milder and more targeted intervention for transgender adolescents, helping them better cope with physical and psychological challenges during puberty and laying a foundation for subsequent gender transition therapy.

3.2 Benign Hormone-Dependent Breast Diseases

Benign hormone-dependent breast diseases mainly include hormone-sensitive mammary hyperplasia and recurrent breast nodules. Their pathogenesis is closely linked to excessive estrogen levels or estrogen-progesterone imbalance in the body, clinically manifested as breast distending pain and breast lumps. Symptoms in some patients fluctuate with the menstrual cycle and may severely impair quality of life in severe cases.