近日，美国食品和药物管理局（FDA）已批准XERAVA(eravacycline) 治疗18岁以上成年人的复杂腹腔内感染（complicated intra-abdominal infections，cIAIs）。
Eravacycline是一种可注射的、全合成的氟化四环素类抗菌药物。对临床常见革兰阳性、阴性需氧及兼性厌氧菌，大多数厌氧菌以及对头孢菌素、大环内酯类、β内酰胺类/β内酰胺酶抑制剂多重耐药菌均有较强体外抗菌活性。
批准日期：2018年8月30日 公司：TetraphasePharmaceuticals Inc
XERAVA（eravacycline）注射用，用于静脉注射
美国最初批准：2018年
作用机制
Eravacycline是一种抗菌药物[见微生物学]。
适应症和用法
XERAVA是一种四环素类抗菌药，适用于治疗18岁及以上患者的并发腹腔感染。
使用限制
XERAVA不适用于治疗复杂性尿路感染（cUTI）。
为了减少抗药性细菌的发展并保持XERAVA和其他抗菌药物的有效性，XERAVA应仅用于治疗或预防已被证实或强烈怀疑由易感细菌引起的感染。
剂量和给药
•通过静脉内输注给予XERAVA注射1mg/kg，每12小时注射约60分钟，总持续时间为4至14天。
•严重肝功能损害（Child Pugh C）：第1天每12小时1次/kg XERAVA，第2天开始每24小时1 mg/kg总持续时间为4至14天。
•伴随使用强细胞色素P450同工酶（CYP）3A诱导剂：每12小时1.5mg/kg XERAVA，总持续时间为4至14天。
•查看XERAVA准备的完整处方信息。
剂量形式和强度
•用于注射：50mgeravacycline（相当于63.5mg eravacyclinedihydrochloride）作为单剂量小瓶中的冻干粉末，用于重构和进一步稀释。
禁忌症
•已知对甲基环素，四环素类抗菌药物或XERAVA中任何赋形剂的超敏反应。
警告和注意事项
•超敏反应：四环素抗菌药物，包括XERAVA，已报道危及生命的超敏反应（过敏性）反应。避免用于已知对四环素过敏的患者。
•牙齿变色和牙釉质发育不全：XERAVA在牙齿发育期间（怀孕的后半段，婴儿期和儿童期至8岁）可能导致牙齿永久性变色（黄灰棕色）和牙釉质发育不全。
•抑制骨骼生长：在怀孕的第二和第三个三个月，婴儿和儿童直至8岁时使用XERAVA可能会导致骨骼生长的可逆抑制。
•艰难梭菌相关性腹泻：评估腹泻是否发生。
不良反应
最常见的不良反应（发生率≥3％）是输液部位反应，恶心和呕吐。
要报告疑似不良反应，请致电1-833-7-XERAVA（1-833-793-7282）或FDA 1-800--FDA-1088或www.fda.gov/medwatch联系TetraphasePharmaceuticals Inc.
药物相互作用
•伴随使用强CYP3A诱导剂可减少乙酰环素的暴露。增加XERAVA剂量同时使用强效剂量CYP3A诱导剂。
•接受抗凝治疗的患者可能需要向下调整抗凝剂剂量。
用于特定人群
哺乳期：在使用XERAVA治疗期间不建议母乳喂养。
包装提供/存储和处理
提供
注射用XERAVA，50毫克/瓶，是一种黄色至橙色，无菌，无防腐剂的粉末，用于单剂量10mL透明玻璃瓶中，配有橡胶塞和铝质外壳。 每个小瓶含有50mg的eravacycline（相当于63.5mg的eravacyclinedihydrochloride）。 XERAVA提供两种包装配置：
单瓶小瓶包含一个50mg单剂量小瓶：NDC 71773-050-05。
12小瓶装有12个50毫克单剂量小瓶的纸盒：NDC 71773-050-12。
存储和处理
在重建之前，XERAVA应储存在2°C至8°C（36°F至46°F）[见剂量和管理]。 将小瓶装入纸箱直至使用。
完整资料附件：https://www.xerava.com/assets/pdf/Xerava-Approved%20PI_27AUG2018.pdf

TETRAPHASE PHARMACEUTICALS ANNOUNCES FDA APPROVAL OF XERAVA™ (ERAVACYCLINE) FOR COMPLICATED INTRA-ABDOMINAL INFECTIONS (CIAI)
U.S. Food and Drug Administration (FDA) has granted approval of XERAVA™ (eravacycline) for the treatment of complicated intra-abdominal infections (cIAI). In clinical trials, XERAVA was well-tolerated and achieved high clinical cure rates in patients with cIAI, demonstrating statistical non-inferiority to two widely used comparators – ertapenem and meropenem.
XERAVA is indicated for the treatment of complicated intra-abdominal infections in patients 18 years of age and older. To reduce the development of drug-resistant bacteria and maintain the effectiveness of XERAVA and other antibacterial drugs, XERAVA should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria.
Important Safety Information
XERAVA is a tetracycline class antibacterial indicated for the treatment of complicated intra‑abdominal infections in patients 18 years of age and older.
XERAVA is not indicated for the treatment of complicated urinary tract infections.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of XERAVA and other antibacterial drugs, XERAVA should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria.
XERAVA is contraindicated for use in patients with known hypersensitivity to eravacycline or to tetracycline-class antibacterial drugs. Life-threatening hypersensitivity (anaphylactic) reactions have been reported with XERAVA.
The use of XERAVA during tooth development (last half of pregnancy, infancy and childhood to the age of 8 years) may cause permanent discoloration of the teeth (yellow-gray-brown) and enamel hypoplasia.
The use of XERAVA during the second and third trimester of pregnancy, infancy and childhood up to the age of 8 years may cause reversible inhibition of bone growth.
Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents and may range in severity from mild diarrhea to fatal colitis.
The most common adverse reactions observed in clinical trials (incidence ≥ 3%) were infusion site reactions, nausea, and vomiting.
XERAVA is structurally similar to tetracycline-class antibacterial drugs and may have similar adverse reactions.  Adverse reactions including photosensitivity, pseudotumor cerebri, and anti‑anabolic action which has led to increased BUN, azotemia, acidosis, hyperphosphatemia, pancreatitis, and abnormal liver function tests, have been reported for other tetracycline-class antibacterial drugs, and may occur with XERAVA.  Discontinue XERAVA if any of these adverse reactions are suspected.
About XERAVA™
XERAVA (eravacycline for injection) is a novel, fully-synthetic fluorocycline, FDA-approved antibiotic for the treatment of cIAI. XERAVA has demonstrated potent activity against MDR pathogens.
XERAVA was investigated for the treatment of cIAI as part of the Company's IGNITE (Investigating Gram-Negative Infections Treated with Eravacycline) phase 3 programs. In the first pivotal phase 3 trial in patients with cIAI, twice-daily intravenous (IV) eravacycline met the primary endpoint by demonstrating statistical non-inferiority of clinical response compared to ertapenem and was well-tolerated. In the second phase 3 clinical trial in patients with cIAI, twice-daily IV eravacycline met the primary endpoint by demonstrating statistical non-inferiority of clinical response compared to meropenem and was well-tolerated. In both trials, XERAVA achieved high cure rates in patients with Gram-negative pathogens, including resistant isolates.
About Tetraphase Pharmaceuticals, Inc.
Tetraphase is a biopharmaceutical company using its proprietary chemistry technology to create novel antibiotics for serious and life-threatening bacterial infections, including those caused by many of the MDR bacteria highlighted as urgent public health threats by the WHO and CDC. The Company has created more than 3,000 novel tetracycline compounds using its proprietary technology platform. Tetraphase's lead product, XERAVA™ (eravacycline) is FDA-approved for the treatment of complicated intra-abdominal infections (cIAI), has received a positive opinion from the CHMP for cIAI, and is under consideration for potential marketing approval by the European Commission for cIAI.