美国FDA批准Ferring Pharmaceuticals公司degarelix粉针剂（Tradename/Firmagon）上市，用于治疗晚期前列腺癌。本品剂量规格：degarelix 80 mg、120 mg/瓶。80 mg瓶含甘露醇 200 mg，120 mg瓶含甘露醇 150 mg。

    本品系一促性腺激素释放激素（GnRH）受体抑制剂类药物，可逆性抑制垂体GnRH受体来减少促性腺激素释放继而抑制睾酮的释放。本品通过抑制对前列腺癌持续生长至关重要的睾酮来延缓前列腺癌的生长和恶化。以激素治疗前列腺癌来降低睾酮浓度的初期却造成睾酮浓度激增，此初始刺激该激素受体可暂时性促进肿瘤生长而不是抑制它。而地degarelix则不会。

    Ⅲ期临床研究显示，本品降低睾酮浓度的效果至少可与亮丙瑞林储库型控释注射剂（Lupron Depot）相媲美，而且降低睾酮浓度在统计学上显著快。在治疗的第3日，本品组96％达到去生殖腺的睾酮浓度，亮丙瑞林组效果为0％。第14日，本品组99％达到去生殖腺的睾酮浓度，亮丙瑞林组为18％。

    在临床研究中，前列腺特异抗原（PSA）浓度可作为监测的第2个疗效判断终点。使用degarelix2周后降低PSA 64％，1月后85％，3月后95％，在治疗的整个1年中始终抑制PSA。

    本品在临床研究中报道的最常见的不良反应是注射部位反应（疼痛，红肿和肿胀），热潮红，体重增加，乏力和某些肝酶浓度升高。

Manufacturer:
Ferring Pharmaceuticals, Inc.

Pharmacological Class:
GnRH receptor antagonist

Active Ingredient(s):
Degarelix 80mg/vial, 120mg/vial; pwd for SC inj after reconstitution.

Manufacturer:
Ferring Pharmaceuticals, Inc.

Pharmacological Class:
GnRH receptor antagonist

Active Ingredient(s):
Degarelix 80mg/vial, 120mg/vial; pwd for SC inj after reconstitution.
治疗前列腺癌新药Degarelix上市

Indication(s):
Advanced prostate cancer.

Pharmacology:
Degarelix binds reversibly to pituitary gonadotropin releasing factor (GnRH) receptors, causing a decrease in the release of gonadotropins and in the production of testosterone. It is effective in maintaining the suppression of testosterone below the medical castration level of 50ng/dL. Upon subcutaneous injection, this product forms a depot from which degarelix is released to the systemic circulation. It is metabolized by peptide hydrolysis in the hepatobiliary system and is eliminated as peptide fragments in the feces.

Clinical Trials:
A one-year study was conducted to compare degarelix to leuprolide in the treatment of 620 patients with prostate cancer. The primary objective was to demonstrate that degarelix effectively lowered and maintained testosterone levels to castration levels of ≤50ng/dL over 12 months. Serum testosterone levels were measured at screening, and on days 0,1,3,7,14, and 28 in the first month, then monthly until the end of the study. The median serum testosterone levels across all treatment arms was 400ng/dL. The patients given degarelix were divided into two groups: after an initial dose of 240mg SC, they were given either 160mg or 80mg SC once every 28 days. The patients treated with leuprolide were given 7.5mg IM once monthly.

Of the group given degarelix 160mg monthly, 98.3% achieved medical castration (serum testosterone ≤50ng/dL) from day 28 to day 364, compared to 97.2% for the degarelix 80mg/month group. The group given leuprolide had a rate of 96.4%.

The suppression of testosterone levels ≤50ng/dL occurred significantly faster in patients receiving degarelix than in those receiving leuprolide. By day 3, 96% of the patients given degarelix attained serum testosterone levels at or below 50ng/dL, compared to 0% for those given leuprolide. By day 7, 99% of the degarelix-treated patients were at the medical castration level, compared to 1% for the leuprolide group. At day 28, all groups were at or above 99%.

A secondary endpoint, PSA level, was monitored as well. Serum PSA levels were lowered by 64% 2 weeks after the administration of degarelix, 85% after 1 month, and 95% a