近日，美国FDA批准TPOXX（tecovirimat）上市新药，治疗天花（smallpox）。这也是首款获批治疗天花的新药。
批准日期：2018年7月16日 公司：SIGA Technologies
TPOXX（tecovirimat）胶囊,用于口服
美国最初批准：2018年
作用机制
Tecovirimat是一种抗天花病毒（天花）的抗病毒药物[见微生物学]
适应症和用法
TPOXX是正痘病毒VP37包膜蛋白的抑制剂，适用于治疗体重至少13kg的成人和百分比患者的人类天花病。
使用限制：
TPOXX治疗天花病的有效性尚未在人体中确定，因为充分且控制良好的田间植物不可行，并且在人类中诱导天花病以研究药物的疗效并不符合道德规范。
TPOXX的疗效可能会降低免疫功能低下的患者基础，从而降低免疫功能低下的动物模型的疗效。
剂量和给药
TPOXX应在中度或高脂肪的全餐后30分钟内服用。
成人：600毫克，每日两次，共14天
体重13公斤或以上的儿科患者：
13kg至小于25 kg：200mg TPOXX每日两次，共14天25 kg至小于40 kg：400mg TPOXX每日两次，共14天40kg或更多：600mg TPOXX每日两次，持续14天
剂量形式和强度
胶囊：200毫克。
禁忌症
没有
警告和注意事项
低血糖：与瑞格列奈共同给药可能引起低血糖。
监测血糖并监测共同给药期间的低血糖症状。
不良反应
健康成人受试者（≥2％）的常见不良反应是头痛，恶心，腹痛和呕吐。
药物相互作用
在治疗前和治疗期间查阅完整的处方信息以获得潜在的药物相互作用。
包装提供/存储和处理
每个TPOXX胶囊含有200毫克的tecovirimat。 TPOXX胶囊是硬明胶，其中印有白色墨水的不透明橙色主体带有“SIGA”，随后是SIGA标志，随后是带有“ST-246®”白色墨水的不透明黑色盖子，含有白色的白色粉末。
每瓶含有42粒胶囊（NDC 50072-200-42），带有感应密封和儿童防护帽。
将胶囊储存在20°C至25°C（68°F至77°F）的原瓶中; 允许偏移15°C至30°C（59°F至86°F）[见USP受控室温]。

https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf
TPOXX Approved for the Treatment of Human Smallpox Disease
SIGA Technologies announced that the Food and Drug Administration (FDA) has approved TPOXX (tecovirimat) for the treatment of human smallpox disease in adults and pediatric patients weighing at least 13kg.
TPOXX is the first small-molecule oral antiviral agent to be specifically approved for this indication. It targets and inhibits the activity of the orthopoxvirus VP37 protein and blocks its interaction with cellular Rab9 GTPase and TIP47, which prevents the formation of egress-competent enveloped virions necessary for cell-to-cell and long-range dissemination of virus.
The approval was supported by findings from 12 clinical trials of TPOXX with more than 700 healthy human volunteers that showed no drug-related serious adverse events. The most commonly reported adverse effects were headache, nausea, and abdominal pain. In addition, significant reductions in mortality and viral load were seen in non-human primates infected with monkeypox virus and in rabbits infected with rabbitpox virus in 4 trials. Overall, treatment with TPOXX for 14 days led to a statistically significant improvement in survival vs placebo, except when given to cynomolgus macaques on day 6 post-challenge.
“The FDA approval of TPOXX achieves an important objective for both SIGA and our lead partner in the U.S. Government, the Biomedical Advanced Research and Development Authority (BARDA). The approval validates this novel smallpox therapy as an important medical countermeasure in response to a potential smallpox outbreak," stated Dr. Phil Gomez, CEO of SIGA Technologies, Inc.
For now, TPOXX will be available only through the US government's Strategic National Response Stockpile (SNS) and is supplied as 200mg strength capsules. The Company plans to evaluate the potential expansion of the TPOXX indication to include prophylactic use in those exposed to smallpox and other orthopoxviruses (eg, monkeypox).