Degarelix Injection 80mg

The clinical application of Degarelix Injection 80mg is mainly focused on the treatment of prostate cancer. Relying on its advantages of rapid testosterone reduction and no initial flare effect, it covers different treatment stages of advanced, locally advanced, and recurrent prostate cancer, and can be used in combination with other therapeutic modalities according to patient conditions. Specific clinical applications are as follows:

The core therapeutic goal for advanced or metastatic prostate cancer (including bone metastasis, lymph node metastasis, etc.) is to rapidly reduce testosterone levels to the castrate level (<50ng/dL), block the nutrient supply of androgens to cancer cells, thereby controlling tumor progression and relieving clinical symptoms. As a first-line castration therapy, the product has become one of the preferred options for such patients due to the highly efficient absorption of the injectable formulation.

Unlike traditional GnRH agonists, this injection does not require an initial stimulation phase followed by suppression. After subcutaneous injection, it directly and competitively binds to pituitary GnRH receptors, rapidly inhibiting the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and subsequently quickly reducing the synthesis and release of testicular testosterone. Testosterone levels are usually reduced to the castrate level within 24–48 hours after administration, with no transient testosterone elevation (flare effect). This feature is particularly critical for advanced patients at risk of bone metastasis and spinal cord compression, as it effectively avoids adverse events such as accelerated tumor progression and aggravated bone pain caused by testosterone flare, significantly improving treatment safety.

In clinical practice, for patients with advanced prostate cancer who cannot tolerate or refuse surgical castration, or who have comorbidities (e.g., cardiovascular disease, diabetes, etc.), it can serve as a long-term maintenance treatment. Regular subcutaneous injections sustainably control testosterone levels, delay tumor progression, prolong patient survival, improve quality of life, and alleviate tumor-related symptoms such as bone pain, frequent urination, and urgency.

The treatment of locally advanced prostate cancer (tumor invasion beyond the prostatic capsule, seminal vesicles, and other surrounding tissues without distant metastasis) usually involves comprehensive therapy including surgery and radiotherapy. Degarelix Injection 80mg can be used as an adjuvant treatment in combination with surgery or radiotherapy to enhance efficacy.

For locally advanced patients who are unsuitable for surgical resection (e.g., large tumor volume, extensive invasion) or refuse surgery, the product can be used alone as long-term androgen deprivation therapy. The 80mg maintenance dose via subcutaneous injection continuously suppresses testosterone levels, shrinks the tumor, stabilizes the disease, prevents further invasion of surrounding tissues, and creates opportunities for subsequent treatment. For patients undergoing radiotherapy, combination with this injection significantly improves radiotherapy efficacy, as androgens reduce the sensitivity of prostate cancer cells to radiation. By rapidly and sustainably lowering testosterone, the product enhances the response of cancer cells to radiotherapy, reduces radiotherapy resistance, and lowers the risk of local recurrence.

In addition, neoadjuvant therapy with the product before surgery for some locally advanced prostate cancer patients can rapidly reduce testosterone levels via injection, leading to tumor shrinkage and downstaging, improving surgical resection rates, reducing the risk of tumor spread during surgery, and improving postoperative prognosis.

After radical prostatectomy or radiotherapy, some patients experience elevated prostate-specific antigen (PSA), indicating tumor recurrence, requiring re-initiation of endocrine therapy. It is an important option for second-line endocrine therapy.
For patients with PSA recurrence after surgery or radiotherapy without distant metastasis, the 80mg maintenance dose via subcutaneous injection effectively suppresses testosterone and PSA levels, delays tumor progression, and prevents progression to metastatic prostate cancer. For recurrent patients with distant metastasis, this injection can be combined with novel endocrine agents (e.g., enzalutamide, abiraterone, etc.) to further enhance efficacy and prolong progression-free survival.

Furthermore, for recurrent patients who developed resistance to previous GnRH agonist therapy or could not tolerate agonist-related adverse reactions, switching to Degarelix Injection 80mg effectively improves treatment outcomes. Its mechanism of action differs from agonists, with no receptor desensitization, allowing sustained testosterone inhibition and providing a new therapeutic direction for drug-resistant patients.

The active ingredient of the product, degarelix, is a highly selective GnRH receptor antagonist, which is fundamentally different in mechanism from traditional GnRH agonists (e.g., leuprorelin, goserelin). Agonists first stimulate pituitary GnRH receptors, causing transient elevations in LH and FSH, followed by a temporary increase in testosterone (flare effect), and only then does receptor desensitization occur to suppress testosterone secretion. In contrast, degarelix directly and competitively binds to pituitary GnRH receptors without an initial stimulatory phase, immediately blocking the stimulatory effect of GnRH on the pituitary gland, rapidly inhibiting LH and FSH secretion, and thereby quickly reducing testosterone levels.

This unique mechanism leads to an extremely rapid onset of action after subcutaneous administration of it. Testosterone is typically reduced to castrate levels within 24 hours of dosing, with stable castration achieved within 48 hours, and no testosterone flare occurs throughout treatment. This feature not only rapidly relieves tumor-related symptoms but also effectively prevents serious adverse events such as tumor progression, aggravated bone pain, and spinal cord compression caused by testosterone flare. It is especially suitable for prostate cancer patients at risk of bone metastasis, significantly improving the safety and efficacy of treatment.

The product is administered via subcutaneous injection, which causes less trauma and pain than intramuscular injection, resulting in better patient tolerance. The product is packaged in a prefilled syringe with an accurate dose (80mg per syringe) and requires no additional dilution. Medical staff can complete administration quickly, and patients may self-administer at home under professional guidance, greatly improving convenience and reducing hospital visits-particularly beneficial for long-term maintenance therapy.

In addition, it has a rational dosing schedule: a loading dose is given in the initial 28‑day phase, followed by one 80mg maintenance dose subcutaneously every 28 days. The low frequency avoids missed or interrupted doses from frequent administration, markedly improving treatment compliance. Subcutaneous injection also avoids gastrointestinal absorption interference seen with oral drugs, providing more stable absorption and ensuring sustained efficacy to maintain testosterone within the castrate range.

Other common adverse reactions include hot flashes, night sweats, decreased libido, and fatigue, all of which are normal physiological responses to testosterone reduction. Patients generally adapt over the course of treatment, and symptoms gradually diminish.
Unlike traditional GnRH agonists, it has no testosterone flare, thus avoiding serious complications such as exacerbated bone pain and urinary tract obstruction. It also has minimal impact on the cardiovascular system, liver, and renal function, so routine monitoring of liver and kidney function is unnecessary. Only regular monitoring of testosterone and PSA levels is required to ensure therapeutic effect.