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近日，新型抗菌药物的静脉注射和口服片剂Sivextro(tedizolid phosphate)获美国FDA批准用于治疗皮肤感染成人患者（如金黄色葡萄球菌[包括耐甲氧西林菌株和甲氧西林敏感菌株]、各种链球菌和粪肠球菌引起的急性细菌性皮肤及皮肤组织感染 (ABSSSI)）。
FDA药品评价和研究中心的抗微生物产品室主任Edward Cox，M.D.，M.P.H说：“今天的批准提供医生和患者对严重有皮肤感染一种新治疗选择，”被指定为一种合格的传染病产品(QIDP)和接受一种加快审评。QIDP指定还使它合格对另外五年专卖权。
原研上市时间：2014年6月20日[FDA批准]，2015年6月[欧盟上市] 公司：Cubist Pharmaceuticals，Inc.
SIVEXTRO (磷酸泰地唑胺[tedizolid phosphate])为注射，为静脉使用
SIVEXTRO (磷酸泰地唑胺[tedizolid phosphate])片，为口服使用
美国初次批准：2014
作用机制:Tedizolid磷酸酯是tedizolid的前药，一种抗细菌药[见药代动力学；微生物学].
适应证和用途
SIVEXTRO是一种恶唑烷酮类抗细菌药适用在成年为治疗由指定易感细菌所致急性细菌性皮肤和皮肤结构感染(ABSSSI)。
为减低耐药细菌的发生和维持SIVEXTRO和其他抗细菌药的有效性，SIVEXTRO只应用于治疗或预防被证明或强烈怀疑是被细菌所致感染。
剂量和给药方法
200 mg每天1次口服或作为静脉(IV)历时1小时输注给予共6天。
剂型和规格
⑴为注射：200mg，无菌，冻干粉在为静脉输注重建单次使用小瓶；
⑵片：200mg.
禁忌证
无。
警告和注意事项
⑴患者有粒细胞减少：尚未曾适当地在有粒细胞减少(中性粒细胞计数<1000细胞/mm3)患者中评价SIVEXTRO的安全性和疗效。在一个感染的动物模型，SIVEXTRO的抗细菌活性在缺乏粒细胞时减低。中性粒细胞减少患者考虑替代疗法。
⑵难辨梭状芽孢杆菌[Clostridium difficile]-伴随腹泻：如发生腹泻评价。
不良反应
最常见不良反应(>2%)是恶心，头痛，腹泻，呕吐，和眩晕。
包装供应/贮存和处置
片剂
SIVEXTRO片是黄色薄膜衣椭圆片含200 mg的Tedizolid磷酸酯；每片一侧凹陷有“TZD”和另侧“200“。
供应如下：
高密度聚乙烯[HDPE]30片瓶有防儿童打开的密盖(NDC 67919-041-01)
6片剂量单位泡罩包装(NDC 67919-041-02)
注射剂
SIVEXTRO是以无菌，冻干粉为注射在单次使用200mg小瓶供应。每个200mg小瓶必须用注射用无菌水重建和随后只用0.9%氯化钠注射液，USP稀释。
200mg单剂量小瓶10个包装(NDC 67919-040-01)
贮存和处置
SIVEXTRO片和SIVEXTRO为注射应贮存在20°C至25°C (68°F至77°F)；外出允许至15°C至30°C (59°F至86°F) [见USP控制室温].
产品特点；
抗生素的广泛使用使得细菌的耐药性问题日益严重，新型抗耐药菌药物的研究已成为抗菌药物研究的主要方向。其中，全合成的恶唑烷酮类抗菌药物利奈唑胺已成功上市，并取得了良好的临床治疗效果。Sivextro(通用名：tedizolid磷酸盐，曾用名：TR-701)由Cubist制药公司开发，是一种恶唑烷酮类抗生素，口服和注射均为每日一次，每次200mg，连续使用6日。Sivextro是一种前药，在体内可被磷酸酶迅速转化为具有生物活性的tedizolid。后者能够和细菌的核糖体50S亚基结合，从而抑制蛋白质的合成。。
产品国外上市情况：
磷酸特地唑胺，是由CUBIST PHARMS公司研发的新型抗细菌感染用药。2014年6月20日，美国FDA批准磷酸特地唑胺上市，用于特定的敏感细菌引起的成人急性细菌性皮肤和皮肤结构感染(ABSSSI)，商品名为SIVEXTRO，规格200mg。目前在欧洲和加拿大已提交上市申请。
完整说明资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=75672079-589f-451a-bdbf-eaebcfcc80a9
Sivextro (tedizolid phosphate) is an antibacterial agent of the oxazolidinone class.
Sivextro is specifically indicated for the treatment of adults with acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of the following Gram-positive microorganisms: Staphylococcus aureus (including methicillin-resistant [MRSA] and methicillin-susceptible [MSSA] isolates), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus Group (including Streptococcus inosus, Streptocccus intermedius, and Streptococcus constellatus), and Enterococcus faecalis.
Sivextro is supplied as a tablet or solution, for oral and/or intravenous administration. The recommended dosage of Sivextro is 200 mg administered once daily for six (6) days either orally (with or without food) or as an intravenous (IV) infusion.
A short course in ABSSSI
Once-daily IV/oral SIVEXTRO® (tedizolid phosphate) offers a short, 6-day course for the treatment of acute bacterial skin and skin structure infections (ABSSSI), including MRSA
Indication:
SIVEXTRO is an oxazolidinone-class antibacterial indicated for the treatment of adults with acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of the following Gram-positive microorganisms: Staphylococcus aureus (including methicillin-resistant [MRSA] and methicillin-susceptible [MSSA] isolates), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus group (including Streptococcus anginosus, Streptococcus intermedius and Streptococcus constellatus), and Enterococcus faecalis.
Usage:
To reduce the development of drug-resistant bacteria and maintain the effectiveness of SIVEXTRO and other antibacterial drugs, SIVEXTRO should be used only to treat ABSSSI that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
Selected Important Safety Information
Patients with neutropenia: The safety and efficacy of SIVEXTRO® (tedizolid phosphate) in patients with neutropenia (neutrophil counts <1000 cells/mm3) have not been adequately evaluated. In an animal model of infection, the antibacterial activity of SIVEXTRO was reduced in the absence of granulocytes. Alternative therapies should be considered when treating patients with neutropenia.
Clostridium difficile–associated diarrhea (CDAD), ranging from mild diarrhea to fatal colitis, has been reported with nearly all systemic antibacterial agents, including SIVEXTRO. Evaluate all patients who present with diarrhea following antibiotic use. Careful medical history is necessary because CDAD has been reported to occur more than two months after the administration of antibacterial agents. If CDAD is suspected or confirmed, antibacterial use not directed against C. difficile should be discontinued, if possible.
Development of drug-resistant bacteria: Prescribing SIVEXTRO in the absence of a proven or strongly suspected bacterial infection or prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Adverse Reactions: The most common adverse reactions for SIVEXTRO are nausea (8%), headache (6%), diarrhea (4%), vomiting (3%), and dizziness (2%).
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