美国FDA近日批准了晚期前列腺癌治疗药物——degarelix注射剂。Degarelix属于促性腺激素释放激素(GnRH)受体抑制剂。该药通过抑制睾酮分泌,延缓前列腺癌的生长和发展。 通常激素治疗会引起一过性睾酮分泌增加,可导致瘤体增大,degarelix则不会引起患者睾酮水平一过性升高。 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. 前列腺癌新药degarelix在III期临床中表现良好 有专家表示，III期临床试验结果显示，Ferring公司的新型前列腺癌治疗药degarelix取得了突破性效果。  在该药的III期临床试验中，对比了degarelix（每月用药一次）和标准药物（leuprorelin）的疗效，疗程为期12个月，两组受试者病情情况等同。结果表明，degarelix能更快控制血清睾酮水平和前列腺特异抗原（PSA），并且该药能在12个月的观察期内保持上述疗效。 有负责人称，degarelix临床试验终点数据还未出来，但就该药对PSA水平的快速控制可以延长患者的存活时间。试验也证实，这种新药的耐受性至少与目前标准治疗药物相当。值得指出的是，患者用药后，它未引起严重的全身性不良反应。