Contezolid

Contezolid (MRX-I), 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 (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)^[1][2]. 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^[2].
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%^[2].
Contezolid (MRX-I) exhibits no obvious toxicity^[2].
Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls^[3].