制造商：
辉凌制药公司
药理分类：
促性腺激素释放激素受体拮抗剂
活性成分（补）：
Degarelix 80mg/vial，120mg/vial;为SC已经来到重组后的密码。
指示（补）：
晚期前列腺癌。
药理作用：
Degarelix可逆性结合垂体促性腺激素释放因子（激素）受体，引起促性腺激素释放和睾丸激素的生产下降。它是在保持低于50ng/dL药物去势水平睾酮抑制。皮下注射后，该产品形成了从哪个degarelix被释放到全身血液循环车厂。它是由肽水解代谢在肝胆系统，并在消除粪便肽片段。
临床试验：
一个为期一年的研究进行了比较degarelix以醋酸亮丙瑞林，在620例前列腺癌患者的治疗。主要目的是要表明，有效地降低睾酮水平，并维持为≤12个月以上50ng/dL去势水平degarelix。测定血清睾酮水平在筛选，并在天0,1,3,7,14和28日在第一个月，然后每月直到研究结束。在所有的中位数血清睾酮水平的治疗武器是400ng/dL。鉴于degarelix将患者分为两组：经过一个初始剂量240mg资深大律师，他们得到要么做一次，每28天或80毫克160mg资深大律师。与亮丙瑞林治疗的患者给予7.5mg聊天室每月一次。
每月给予degarelix 160mg组，药物去势达到98.3％（血清睾酮≤50ng/dL）从28天到364天，而97.2％的degarelix 80mg/month组。给予醋酸亮丙瑞林本集团有96.4％的税率。
睾丸激素的水平抑制≤50ng/dL发生在接受比那些接受leuprolide degarelix患者速度明显加快。第3天，给予96或以下50ng/dL degarelix血清睾酮水平达到％的患者相比，亮丙瑞林者给予0％。第7天，99 degarelix治疗的患者％的人有医疗去势水平，而1％的醋酸亮丙瑞林组。 28天，各组均达到或超过99％。
次要终点，PSA水平，以及进行了监测。血清PSA水平降低64％2周后degarelix管理，85％，后1个月，3个月后及95％，并维持对于今年余下的治疗抑制。
法律分类：
接收
成人：
由资深大律师在给每28天一次腹部损伤;避免腰部和肋骨地区。两个120毫克注射一次，然后一80毫克每28天一次已经来到。
儿童：
不推荐。
禁忌（补）：
妊娠（Cat.X）。
警告/注意事项：
严重肾或肝损害。先天性长QT综合征。电解质不平衡。充血性心力衰竭。监测血清PSA。哺乳母亲：不推荐。
互动（补）：
注意与IA类（如奎尼丁，普鲁卡因胺）或III类（如胺碘酮，索他洛尔）抗心律失常药。
不良反应（补）：
注射液部位反应（如疼痛，红斑，肿胀，硬结），潮热，体重增加，疲劳，转氨酶升高，增加γ-谷氨酰转移; QT间期延长。
如何提供：
开始治疗组（120mg/vial）-2（瓦特用品）
处理维护包（80mg/vial）-1（瓦特用品）
最后更新：
2009年8月4日
FIRMAGON
Manufacturer:
Ferring Pharmaceuticals, Inc.
Pharmacological Class:
GnRH receptor antagonist
Active Ingredient(s):
Degarelix 80mg/vial, 120mg/vial; pwd for SC inj after reconstitution.
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% after 3 months, and remained suppressed for the remainder of the year of treatment.
Legal Classification:
Rx
Adults:
Give by SC inj in abdomen once every 28 days; avoid waist and rib areas. Two 120mg injections once, then one 80mg inj once every 28 days.
Children:
Not recommended.
Contraindication(s):
Pregnancy (Cat.X).
Warnings/Precautions:
Severe renal or hepatic impairment. Congenital long QT syndrome. Electrolyte imbalances. Congestive heart failure. Monitor serum PSA. Nursing mothers: not recommended.
Interaction(s):
Caution with Class IA (eg, quinidine, procainamide) or Class III (eg, amiodarone, sotalol) antiarrhythmics.
Adverse Reaction(s):
Inj site reactions (eg, pain, erythema, swelling, induration), hot flashes, increased weight, fatigue, increased transaminases, increased gamma-glutamyltransferase; QT prolongation.
How Supplied:
Treatment Initiation pack (120mg/vial)—2 (w. supplies)
Treatment Maintenance pack (80mg/vial)—1 (w. supplies)