Adis, a Wolters Kluwer Business, Auckland, New Zealand.
Drugs. 2010 Feb 12;70(3):347-53. doi: 10.2165/11202230-000000000-00000.
A 6-month formulation of the gonadotropin-releasing hormone agonist triptorelin embonate (designed to deliver 22.5 mg of triptorelin over a 6-month period) has been developed for use in the treatment of advanced prostate cancer. Following intramuscular administration of the 6-month formulation of triptorelin embonate 22.5 mg to men with advanced prostate cancer (subset of 15 patients from the pivotal clinical trial), serum testosterone levels initially increased, followed by a rapid, sustained decrease. Castrate serum testosterone levels (i.e. < or =1.735 nmol/L) were achieved in a geometric mean time of 18.8 days. The 6-month formulation of triptorelin embonate achieved and maintained castrate serum testosterone levels in patients with advanced prostate cancer (n = 120), according to the results of the pivotal, noncomparative, multicentre trial (patients received intramuscular triptorelin embonate 22.5 mg on day 1 and at month 6 [week 24]). By day 29, 97.5% of patients had castrate serum testosterone levels. Castrate serum testosterone levels were maintained from months 2 to 12 in 93.0% of patients. Prior to the second injection at month 6, 98.3% of patients had castrate serum testosterone levels, and 98.3% of patients had castrate serum testosterone levels at study completion. The 6-month formulation of triptorelin embonate 22.5 mg was generally well tolerated in patients with advanced prostate cancer; adverse events were of mild severity in the majority of patients. Drug-related adverse events (e.g. hot flushes) were consistent with the pharmacological action of triptorelin. Injection-site reactions occurred in 6.7% of triptorelin embonate recipients.
一种戈那瑞林激动剂醋酸曲普瑞林 6 个月制剂（设计用于在 6 个月内递送 22.5 毫克曲普瑞林）已被开发用于治疗晚期前列腺癌。在向患有晚期前列腺癌的男性（关键性临床试验的 15 名患者亚组）肌内注射醋酸曲普瑞林 6 个月制剂 22.5 毫克后，血清睾酮水平最初升高，随后迅速持续下降。在 18.8 天的时间内，95%的患者达到去势血清睾酮水平（即 <或=1.735 nmol/L）。在关键性、非对照、多中心试验中（患者在第 1 天和第 6 个月[第 24 周]接受肌内注射醋酸曲普瑞林 22.5 毫克），120 例晚期前列腺癌患者中，醋酸曲普瑞林 6 个月制剂达到并维持了去势血清睾酮水平。第 29 天，97.5%的患者达到去势血清睾酮水平。93.0%的患者在第 2 至 12 个月时维持去势血清睾酮水平。在第 6 个月进行第二次注射前，98.3%的患者达到去势血清睾酮水平，98.3%的患者在研究结束时达到去势血清睾酮水平。醋酸曲普瑞林 6 个月制剂 22.5 毫克在晚期前列腺癌患者中一般耐受性良好；大多数患者的不良事件为轻度。与药物相关的不良事件（如热潮红）与曲普瑞林的药理作用一致。注射部位反应发生在 6.7%的醋酸曲普瑞林接受者中。
