Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).
性状
Solid
IC50 & Target[1][2]
Oxazolidinone
体外研究(In Vitro)
Contezolid (MRX-I) is highly potent against all Grampositive clinical isolates of staphylococci, streptococci, and enterococci, including MDR organisms such as MRSA, methicilline-resistant Streptococcus epidermidis (MRSE), penicillin-resistant Streptococci (PRSP), and VRE. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Oral absorption of Contezolid (MRX-I) occurrs rapidly in mouse, rat, and dog, with peak plasma concentrations observed at 0.5?2.6 h postdose. In mouse, rat, and dog, respectively, PK parameters are determined as follows: dose-normalized C max /dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC 0?t /dose was 1654, 3703, and 1664 ng?h/mL/(mg/kg); T 1/2 is 1, 1.5, and 3 h; and the oral bioavailability is 69%, 109%, and 37%.
Contezolid (MRX-I) exhibits no obvious toxicity.
Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-80°C, stored under nitrogen
ClinicalTrial
参考文献
[1]. Junzhen Wu, et al. Evaluation of the Effect of Contezolid (MRX-I) on the Corrected QT Interval in a Randomized, Double-Blind, Placebo- and Positive-Controlled Crossover Study in Healthy Chinese Volunteers. Antimicrob Agents Chemother. 2020 May 21;64(6):e02158-19.[2]. Mikhail F Gordeev, et al. New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile. J Med Chem. 2014 Jun 12;57(11):4487-97.
溶解度数据
In Vitro: DMSO : 180 mg/mL (325.89 mM; Need ultrasonic)配制储备液