American University of Beirut Medical Center, Beirut, Lebanon.
Expert Opin Investig Drugs. 2012 Apr;21(4):515-22. doi: 10.1517/13543784.2012.660250. Epub 2012 Feb 13.
Tedizolid phosphate (TR-701) is a new oxazolidinone prodrug that is transformed in the serum into the active drug tedizolid (TR-700). Tedizolid acts by inhibiting protein synthesis and has broad activity against Gram-positive pathogens, including strains that are resistant to linezolid.
This review summarizes the currently available data on this new antimicrobial agent. In vitro activity, pharmacokinetics/pharmacodynamics, clinical efficacy and safety are all addressed.
Tedizolid will provide a useful addition to the antimicrobial armamentarium, particularly in complicated skin and skin structure infections, due to its high oral bioavailability and once-daily dosing. The results of future studies will serve to better position tedizolid among the newly approved agents for infections caused by Gram-positive organisms.
磷酸替唑利（TR-701）是一种新型噁唑烷酮前药，在血清中转化为活性药物替唑利（TR-700）。替唑利通过抑制蛋白质合成发挥作用，对包括耐利奈唑胺的菌株在内的革兰氏阳性病原体具有广泛的活性。
本综述总结了关于这种新型抗菌药物的现有数据。评估了其体外活性、药代动力学/药效学、临床疗效和安全性。
替唑利由于其高口服生物利用度和每日一次的给药方案，将成为抗菌药物治疗手段的有益补充，特别是在治疗复杂的皮肤和皮肤结构感染方面。未来的研究结果将有助于更好地定位替唑利在新批准的用于治疗革兰氏阳性菌感染的药物中的地位。
