英文药名: Firmagon (Degarelix) 中文药名: 地加瑞克, 地盖瑞利注射剂 生产品牌药厂家: Ferring Pharmaceuticals Inc 药品简介 Generic Name for FIRMAGON Degarelix 80mg/vial, 120mg/vial; pwd for SC inj after reconstitution. Legal Classification: Rx Pharmacological Class for FIRMAGON GnRH receptor antagonist. Manufacturer of FIRMAGON Ferring Pharmaceuticals, Inc. Indications for FIRMAGON Advanced prostate cancer. Adult dose for FIRMAGON 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's dosing for FIRMAGON Not recommended. Contraindications for FIRMAGON Pregnancy (Cat.X). Warnings/Precautions for FIRMAGON Severe renal or hepatic impairment. Congenital long QT syndrome. Electrolyte imbalances. Congestive heart failure. Monitor serum PSA. Nursing mothers: not recommended. Interactions for FIRMAGON Caution with Class IA (eg, quinidine, procainamide) or Class III (eg, amiodarone, sotalol) antiarrhythmics. Adverse Reactions for FIRMAGON Inj site reactions (eg, pain, erythema, swelling, induration), hot flashes, increased weight, fatigue, increased transaminases, increased gamma-glutamyltransferase; QT prolongation. How is FIRMAGON supplied? Treatment Initiation pack (120mg/vial)—2 (w. supplies) Treatment Maintenance pack (80mg/vial)—1 (w. supplies) 地盖瑞利能可逆性抑制垂体GnRH受体来减少促性腺激素释放继而抑制睾酮的释放，治疗前列腺癌的效果与亮丙瑞林储库型控释注射剂相当，但见效更快且更持久，用药3天可使96％达到去生殖腺的睾酮浓度。 随着医药技术的快速发展，越来越多的新型抗癌药物进入临床，日前，Ferring（辉凌）公司的新型抗癌药物-地盖瑞利注射剂Firmagon(Degarelix)获美国批准用于治疗晚期前列腺癌。 睾酮是前列腺癌持续生长至关重要的物质。目前，临床主要采用激素降低睾酮浓度来治疗前列腺癌，但初期往往造成睾酮浓度激增，因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，但地盖瑞利却不会出现此种情况，它主要通过持续抑制睾酮来延缓前列腺癌的生长和恶化。 地盖瑞利是一种新型促性腺激素释放激素（GnRH）受体抑制剂类药物，能可逆性抑制垂体GnRH受体来减少促性腺激素释放继而抑制睾酮的释放。研究证明，地盖瑞利1年的治疗可快速有效且持续抑制睾酮和前列腺特异抗原（PSA），耐受性良好，且未见睾酮快速升高。 Ⅲ期临床研究显示，地盖瑞利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（LupronDepot）相媲美，而且降低睾酮浓度兼相爱哦更快。研究发现，在治疗的第3日，地盖瑞利组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。结果显示，使用地盖瑞利2周后降低PSA64％，1月后85％，3月后95％，在治疗的整个1年中始终抑制PSA。临床研究中，地盖瑞利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。 【原产地英文商品名】Firmagon Injection Solution 120mg/vial 【原产地英文药品名】degarelix 【中文参考商品译名】 注：以下产品不同规格和不同价格，购买时请以电话咨询为准！ ·Firmagon注射液 80毫克/瓶 ·Firmagon注射液 120毫克/瓶 ·Firmagon 120毫克/瓶*2+6毫升/瓶溶剂*2 ·Firmagon ps.注射液 80毫克/瓶+6毫升/瓶溶剂+1注射器 【中文参考药品译名】地加瑞克 【生产厂家中文参考译名】辉凌制药 【生产厂家英文名】FERRING Ferring Pharmaceuticals Announces Immediate Availability of Degarelix for the Treatment of Advanced Prostate Cancer Ferring Pharmaceuticals, USA today announced the U.S. commercial availability of degarelix for injection (trade name pending), a new injectable gonadotropin-releasing hormone (GnRH) receptor antagonist approved by the U.S. Food and Drug Administration (FDA) for the treatment of hormone sensitive advanced prostate cancer. Degarelix is available for order through traditional and specialty pharmacy distributors. advertisement Degarelix provides fast, long-term suppression of testosterone, a hormone that stimulates prostate cancer growth.(1-3) Clinical trials demonstrated that degarelix is effective in quickly reducing and sustaining castrate levels of testosterone.(2,3) Degarelix works differently than a luteinizing hormone-releasing hormone (LHRH) agonist bybinding immediately and reversibly to GnRH receptors in the pituitary gland, quickly reducing the release of gonadotropins and consequently testosterone. In the Phase III study vs. leuprolide, the degarelix group achieved a 90 percent decrease in median testosterone levels at Day 3 of treatment, compared with the leuprolide group, which experienced a 65 percent increase in median testosterone levels. By Day 3, 96 percent of degarelix patients achieved castrate levels of testosterone, compared with zero percent receiving leuprolide. In addition, degarelix was as effective as leuprolide in suppressing testosterone levels from Day 28 to the end of the study (Day 364), with 97.2 percent of the degarelix patients maintaining medical castrate levels compared with 96.4 percent for leuprolide. Study findings also showed that prostate specific antigen (PSA) levels were lowered by 64 percent two weeks after administration of degarelix, 85 percent after one month, 95 percent after three months, and remained suppressed throughout the one year of treatment.(1,2) These PSA results should be interpreted with caution because of the heterogeneity of the patient population studied. No evidence has shown that the rapidity of PSA decline is related to aclinicalbenefit."Degarelix, the lead product in our urology portfolio,demonstrated both a rapid onset of action and a profound long-term suppression of testosterone," said Wayne Anderson, President and CEO Ferring Pharmaceuticals Inc., USA. "Now, advanced prostate cancer can be treated with a direct-acting GnRH receptor antagonist inducing rapid reduction of testosterone and sustaining those levels over time, meeting the goals of systemic therapy. We are excited to provide this effective new treatment option for men fighting advanced prostate cancer."Approved by the FDA on December 24, 2008, degarelix represents Ferring Pharmaceuticals' first global launch and the second urology product launch for Ferring Pharmaceuticals, USA. The European Commission granted marketing authorization for degarelix on February 19, 2009. Degarelix is awaiting approval in other key global markets. Phase III Study Results The 12-month, randomized, open-label, parallel-group Phase III study evaluated the efficacy and safety of degarelixcompared with leuprolide administered monthly over one year of prostate cancer treatment. Patients with histologically confirmed prostate cancer were randomized to either degarelix or leuprolide: a degarelix subcutaneous (under the skin) injection of 240 mg for one month with monthly maintenance doses of 80 mg (n=207) or monthly intramuscular (into the muscle) injections of leuprolide depot 7.5 mg (n=201). The primary endpoint was testosterone suppression to less than or equal to 50 ng/dL during monthly measurements from Day 28 to Day 364. Degarelix was at least as effective as leuprolide in achieving and maintaining castrate levels of testosterone.                                N          Patients with         % (95% CI)                                        treatment response Degarelix                 207               202                97.2 240/80 mg Leuprolide 7.5 mg         201               194                96.4 Suppression of testosterone levels to less than or equal to 50 ng/dL occurred significantly faster in patients receiving degarelix than in those receiving leuprolide. At Day 3 of treatment, the degarelix group achieved a 90 percent decrease in median testosterone levels, compared to the leuprolide group which experienced a 65 percent increase in median testosterone levels. The most commonly observed adverse reactions during degarelix therapy included injection site reactions (e.g. pain, erythema, swelling or induration), hot flashes, increased weight, fatigue, and increases in serum levels of transaminases and gamma-glutamyltransferase (GGT). Ninety-nine percent of these observed adverse reactions were Grade 1 or 2 (mild to moderate). Specifically relating to the injection site adverse reactions, most were transient, of mild to moderate intensity, occurred primarily with the starting dose and led to few discontinuations (<1%). Grade 3 (severe) injection site reactions occurred in two percent or less of patients receiving degarelix. Degarelix is contraindicated in patients with known hypersensitivity to degarelix or to any of the product components. Degarelix is not indicated in women or pediatric patients. Long-term androgen deprivation therapy prolongs the QT interval. Physicians should consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, or congestive heart failure and in patients taking Class IA (e.g. quinidine, procainamide) or Class III (e.g. amiodarone, sotalol) antiarrhythmic medications. About Degarelix Degarelix is an injectable gonadotropin-releasing hormone (GnRH) receptor antagonist approved by the U.S. Food and Drug Administration (FDA) for the treatment of hormone sensitive advanced prostate cancer. As a receptor antagonist, degarelix reversibly binds to the GnRH receptors in the pituitary gland, immediately suppressing the secretion of theluteinizinghormone (LH), follicle-stimulating hormone (FSH), and subsequently, testosterone levels.(4) Degarelix also reduces levels ofprostate-specific antigen (PSA). Unlike LHRH agonists, such as leuprolide, an established treatment for prostate cancer, degarelix does not induce an initial testosterone surge. Degarelix is administered monthly by subcutaneous injection. The starting dose is 240 mg, followed by monthly maintenance doses of 80 mg. Degarelix is available for order through traditional and specialty pharmacy distributors. The average monthly cost of one year of degarelix treatment is comparable to other hormone treatments for prostate cancer. About Prostate CancerProstate cancer is the most common cancer, excluding skin cancers, and the second leading cause of cancer death in American men. About one man in six will be diagnosed with prostate cancer during his lifetime, and one in 35 will die of this disease.(5) Prostate cancer develops from cells in the prostate gland that begin to grow out of control. In most cases, prostate cancer grows slowly and can remain undetected throughout a man's life, although it can grow and spread quickly.(6) The four types of standard treatment are: watchful waiting, surgery, radiation therapy, and hormone therapy, also called androgen deprivation therapy (ADT). 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。  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。