Firmagon Company: Ferring Ireland Ltd. Legal category: Prescription. Sport permitted. Active ingredient: Degarelix (as acetate) 80mg, 120mg. Description: Powder and solvent for solution for injection. Presentation: 80mg-1; 120mg-2. Prices available on request. Indication: Treatment of adult male patients with advanced hormone-dependent prostate cancer. Pharmacology: Degarelix is a selective gonadotrophin releasing-hormone(GnRH) antagonist that competitively and reversibly binds to the pituitary GnRH receptors, thereby rapidly reducing the release of the gonadotrophins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), and thereby reducing the secretion of testosterone (T) by the testes. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that removes the source of androgen. Unlike GnRH agonists, GnRH antagonists do not induce a LH surge with subsequent testosterone surge/tumour stimulation and potential symptomatic flare after the initiation of treatment. Dosage: Adult: Initially, 240mg as 2 subcutaneous injections of 120mg each. Monthly maintenance dose: 80mg administered as one subcutaneous injection. First maintenance dose to be given one month after initial dose. Monitor clinical effect by clinical parameters and prostate specific antigen (PSA) serum levels. Elderly: As per adults. Contraindications: Hypersensitivity to the active substance or to any of the excipients. Special precautions: Assess benefit vs risk: History of a corrected QT interval over 450msec, history of or risk factors for torsades de pointes. Caution: Known or suspected hepatic disorder (monitor liver function), severe renal impairment, diabetes. Long-term treatment may affect bone density. Drug interactions: Assess benefit vs risk: Medicinal products known to prolong the QTc interval or medicinal products able to induce torsades de pointes such as class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic medicinal products, methadone, cisapride, moxifloxacine, antipsychotics. Adverse drug reactions: Hot flush, injection site adverse events, insomnia, dizziness, headache, nausea, increased liver transaminases, hyperhidrosis, chills, pyrexia, asthenia, fatigue, influenza-like illness, increased weight. A support service is available to Healthcare Professionals for the administration of the first two doses of Firmagon. 路透社2006年4月10日巴黎讯：根据欧洲泌尿学会协会第21届会议上的一项报告，Degarelix，一种用于前列腺癌激素治疗的新的促性腺激素释放激素（GnRH）阻断剂，可引起睾酮和前列腺特异性抗原(PSA)水平持续降低，而且没有开始的睾酮波动。 比利时Catholic大学的Hein Van Poppel博士及其同事对187例男性进行了为期1年的研究。他们评估了Degarelix 200 mg 和240 mg作为起始剂量进行皮下注射，以及 80, 120 和160 mg 三个维持剂量的治疗作用。 Van Poppel博士说，最重要的结果是，接受240 mg起始剂量的93%的患者在3天内睾酮在去雄水平以下，几乎所有患者在1个月内达到雄激素剥夺，所有患者都未出血睾酮波动。从28天直至1年，每月测量的去雄水平在接受160 mg维持剂量的所有患者、在接受120 mg维持剂量的96%的患者和接受80 mg维持剂量的92%的患者中持续存在。PSA水平在初始治疗后8周降低90%，治疗12周后降低94%，治疗24周后降低96%。 Van Poppel博士说：“这些数据说明我们发现了degarelix的初始和维持剂量。我们目前需要与促黄体生成激素释放激素（LHRH）促效剂进行比较，这是我们所计划的III期研究内容。”