近日，褪黑激素受体激动剂Tasimelteon（商标名：Hetlioz）最初由百时美施贵宝(Bristol-MyersSquibb，BMS)开发，之后由Vanda研发，于2014年获美国食品药品管理局(FDA)批准上市，后又于2015年7月3日获欧洲药品管理局批准上市，由Vanda在美国及欧盟上市销售。

Tasimelteon是FDA第一个批准的用于治疗非24小时觉醒紊乱(N24HSWD)的药物。其为口服胶囊，每粒含20mg Tasimelteon。推荐剂量为睡前空腹服用20mg。

批准日期：2014年1月31日 公司：百时美施贵宝

HETLIOZ(他司美琼 tasimelteon)胶囊 , 供口服使用

美国初步批准：2014年

作用机理

塔斯美尔顿对非24岁患者的治疗作用的确切机制尚不清楚。Tasimelteon是褪黑激素MT1和MT2受体的激动剂。这些受体被认为参与控制昼夜节律。适应症和使用

Hetlioz是一种褪黑激素受体激动剂，用于治疗非24小时睡眠-觉醒障碍（非24小时）

剂量和给药

睡前20毫克，每晚同一时间

不吃东西吃

剂型及强度

胶囊：20mg

禁忌症

没有

可能导致嗜睡：服用赫托利兹后，患者应将活动限制在准备睡觉，因为赫托利兹会损害需要完全保持精神警觉的活动的表现。

不良反应

最常见的不良反应是头痛、丙氨酸转氨酶升高、噩梦或不寻常的梦境、上呼吸道或尿路感染（Hetlioz组的发病率大于5%，至少是安慰剂组的两倍）。

要报告可疑的不良反应，请联系Vanda Pharmaceuticals Inc.，电话1-844-438-5469或www.hetlioz.com或FDA，电话1-800-FDA-1088或www.fda.gov/medwatch。

药物相互作用

强cyp1a2抑制剂（如氟伏沙明）：由于暴露量增加，避免将hetlioz与强cyp1a2抑制剂结合使用。

强cyp3a4诱导剂（如利福平）：避免与利福平或其他cyp3a4诱导剂联合使用hetlioz，因为减少暴露。

在特定人群中使用

妊娠：根据动物数据，可能导致胎儿伤害

肝功能损害：尚未对严重肝功能损害患者进行Hetlioz研究，这些患者不推荐使用Hetlioz。

包装供应/储存和搬运

Hetlioz 20毫克胶囊有1号，深蓝色不透明，硬凝胶胶囊，印有白色“vanda 20毫克”，每个胶囊含有20毫克的Tasimelteon。

NDC 43068-220-01 30瓶

保管部

在控制的室温（25°C（77°F）下储存20 mg Hetlioz胶囊；允许偏离15°C至30°C（59°F至86°F）【见USP控制的室温】。保护Hetlioz 20毫克胶囊免受光照和湿气的影响。

完整资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ca4a9b63-708e-49e9-8f9b-010625443b90

FDA Accepts HETLIOZ® (tasimelteon) Supplemental New Drug Application for Review in the Treatment of Jet Lag Disorder

Dec. 20, 2018 --  U.S. Food and Drug Administration (FDA) has accepted the filing of Vanda's Supplemental New Drug Application for HETLIOZ® (tasimelteon) for the treatment of jet lag disorder.

About HETLIOZ® (tasimelteon)

HETLIOZ® (tasimelteon) is a melatonin receptor agonist. HETLIOZ® has been granted market authorization by the U.S. Food and Drug Administration and the European Medicines Agency. For full U.S. prescribing information, please visit www.hetlioz.com.

Important Safety Information

The most common adverse reactions (incidence >5% and at least twice as high on HETLIOZ® (tasimelteon) than on placebo) were headache, increased alanine aminotransferase, nightmares or unusual dreams, and upper respiratory or urinary tract infection. The risk of adverse reactions may be greater in elderly (>65 years) patients than younger patients because exposure to HETLIOZ® is increased by approximately 2-fold compared with younger patients.

Indication

HETLIOZ® is indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (Non-24).

Important Safety Information

HETLIOZ® may cause somnolence: After taking HETLIOZ®, patients should limit their activity to preparing for going to bed, because HETLIOZ® can potentially impair the performance of activities requiring complete mental alertness.

The most common adverse reactions (incidence >5% and at least twice as high on HETLIOZ® than on placebo) were headache, increased alanine aminotransferase, nightmares or unusual dreams, and upper respiratory or urinary tract infection. The risk of adverse reactions may be greater in elderly (>65 years) patients than younger patients because exposure to HETLIOZ® is increased by approximately 2-fold compared with younger patients.

Use of HETLIOZ® should be avoided in combination with fluvoxamine or other strong CYP1A2 inhibitors, because of a potentially large increase in exposure of HETLIOZ®, and a greater risk of adverse reactions. HETLIOZ® should be avoided in combination with rifampin or other CYP3A4 inducers, because of a potentially large decrease in exposure of HETLIOZ®, with reduced efficacy.

There are no adequate and well-controlled studies of HETLIOZ® in pregnant women. Based on animal data, HETLIOZ® may cause fetal harm. HETLIOZ® should be used during pregnancy only if the potential benefit justifies the potential risks. Caution should be exercised when HETLIOZ® is administered to a nursing woman.

HETLIOZ® has not been studied in patients with severe hepatic impairment and is not recommended in these patients.