近日，美国食品药品监督管理局（FDA）批准Triptodur（triptorelin）缓释注射悬浮液，用于治疗2岁及以上的中枢性性早熟（CPP）儿科患者。当一个孩子出现比正常青春期提前的征象即为中枢性性早熟（CPP）——一般女孩早于8岁，男孩早于9岁。

Triptodur是一类促性腺激素释放激素（GnRH）激动剂，经肌肉注射（IM）给药，是第一个在美国获得批准每隔半年注射一次的用于治疗中枢性性早熟（CPP）的促性腺激素释放激素（GnRH）激动剂。III期临床试验结果显示，Triptodur™可使93%的中枢性性早熟（CPP）患者的促黄体生成激素（LH）水平回归到青春期前的正常水平，它对98%的中枢性性早熟（CPP）患者青春期前促黄体生成激素（LH）的抑制作用一直持续了12个月之久。Triptodur最常见的不良反应是注射部位反应和月经（阴道）出血。

批准日期：2017年11月12日  公司：Arbor Pharmaceuticals, LLC

TRIPTODUR（曲普瑞林 triptorelin）缓释注射悬浮液，用于肌肉注射

美国最初批准：2000年

作用机制

曲普瑞林是一种GnRH激动剂。

适应症和用法

TRIPTODUR是一种促性腺激素释放激素（GnRH）激动剂，用于治疗2岁及以上患有中枢性性早熟的儿科患者。

剂量和给药

必须在医生的监督下进行。

每24周一次肌肉注射22.5毫克，给予TRIPTODUR。

在治疗开始后1至2个月开始GnRH或GnRH激动剂刺激试验，基础LH或性类固醇水平的血清浓度后监测LH水平的反应，在治疗期间必要时确认功效的维持，以及随后的每个剂量。

每3-6个月测量一次身高，并定期监测骨龄。

有关重建和管理说明，请参阅FPI。

剂量形式和强度

对于延长释放的可注射悬浮液：22.5mg曲普瑞林作为粉末饼，用共同包装的2mL稀释剂无菌注射用水重建。

禁忌症

过敏反应

怀孕

警告和注意事项

促性腺激素和性类固醇水平的初始上升：在治疗的前2-4周期间可以观察到青春期的临床体征和症状的增加，因为促性腺激素和性类固醇由于药物的初始刺激作用而升高到基线以上。

已经报道了服用GnRH激动剂的患者的精神病事件。事件包括情绪不稳定，如哭泣，烦躁，急躁，愤怒和侵略。监测精神症状的发展或恶化。

在有或没有癫痫发作，癫痫，脑血管疾病，中枢神经系统异常或肿瘤史的患者以及与惊厥相关的伴随药物治疗的患者中观察到惊厥。

不良反应

在TRIPTODUR的临床试验中，最常见的不良反应（≥4.5％）是注射部位反应，月经（阴道）出血，热潮红，头痛，咳嗽和感染（支气管炎，肠胃炎，流行性感冒，鼻咽炎，外耳炎，咽炎，鼻窦炎和上呼吸道感染）。

如何提供/存储和处理

每个TRIPTODUR 22.5mg一次性试剂盒（NDC 24338-150-20）包含：

一个单剂量的TRIPTODUR 22.5毫克（NDC 24338-150-01），带有翻转密封，含有无菌冻干白色至微黄色粉末饼

一个带Luer Lock的无菌玻璃注射器预先注入2 mL无菌注射用水（NDC 24338-150-02）

两个无菌21规格，1½“针（薄壁）带安全盖

一个包插入

储存温度为20-25°C（68-77°F）[见USP Controlled Room Temperature]。 不要冻结。

完整资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f41380e7-b830-432d-a5f5-a872932f107e

Arbor Pharmaceuticals, LLC and Debiopharm International SA Announce U.S. FDA Approval for Triptodur™, Triptorelin 6-month Formulation, in the Treatment of Central Precocious Puberty (CPP) 

Triptodur™, (triptorelin) for extended release injectable suspension, has been shown to arrest or reverse the clinical signs of puberty with once every six-month intramuscular injection (IM) dosing for children with CPP.

U.S.-based specialty pharmaceutical company, and Debiopharm International SA, part of Debiopharm Group™, a Swiss-based global biopharmaceutical company, today announced that the U.S. Food and Drug Administration (FDA) has approved Triptodur™ for the treatment of pediatric patients 2 years and older with central precocious puberty (CPP). CPP occurs when a child shows signs of puberty sooner than normal - before age 8 in girls and 9 nine in boys. 

"We are excited to be bringing Triptodur™, a new treatment option for children impacted by the disruptive effects of CPP, to the U.S. market," said Ed Schutter, President and CEO of Arbor.  "Triptodur™ adds to our growing portfolio of approved medications that may help to improve the lives of our patients." 

Triptodur™, a gonadotropin-releasing hormone (GnRH) agonist administered through intramuscular injection (IM), is the first GnRH agonist to offer once-every six-month dosing approved for the treatment of CPP in the U.S. In a phase III clinical trial, Triptodur™ demonstrated a return to pre-pubertal luteinizing hormone (LH) levels in 93 percent of patients, with pre-pubertal LH suppression maintained at 12 months by 98 percent of patients.1  The most common adverse reactions are injection site reactions and menstrual (vaginal) bleeding.

"Early puberty in a child can pose significant physical and emotional challenges throughout their life, including shorter adult stature, social, psychological and emotional effects," said Karen Klein, M.D., Pediatric Endocrinologist, University of California San Diego and Rady Children's Hospital. "With treatment, hormone levels in children with CPP are returned to a normal level, slowing the clinical signs of puberty until an age appropriate time."

"We are extremely pleased to provide this pediatric population with the option of the triptorelin six-month formulation," said Eija Lundstrom, Medical Director, Debiopharm International SA. "This will allow children to benefit from an effective and well tolerated treatment with only two injections per year."

Triptorelin was developed by Debiopharm and will be manufactured in Switzerland by Debiopharm Research & Manufacturing SA. Arbor acquired exclusive U.S. commercial rights to Triptorelin 6-month for CPP in November 2015. Triptodur™ is expected to be available in the fourth quarter of 2017.