tcsc0018175 Delpazolid

Delpazolid is a novel oxazolidinone antibiotic agent which can inhibit the growth of MSSA and MRSA with a MIC₉₀ of 2 μg/mL for both of them.

IC50 & Target: MIC90: 2 μg/mL (MSSA), 2 μg/mL (MRSA)^[1]

In Vitro: Delpazolid (LCB01-0371), at concentrations of 1×MIC and 2×MIC, has bacteriostatic activity against MSSA and MRSA after 24 h. At concentrations of 4×MIC and 8×MIC, Delpazolid shows bacteriostatic activity, but there is no regrowth at concentrations of 4×MIC and 8×MIC after 24 h of incubation^[1]. The survival of M. abscessus is greatly decreased in the presence of Delpazolid (LCB-0371) (MIC₅₀=1.2 μg/mL). Delpazolid dramatically decreases the number of intracellular mycobacteria present at 2 days after infection at concentrations of 0.1, 1, and 10 μg/mL^[2].

In Vivo: When administered orally, Delpazolid (LCB01-0371) shows potent protective effects against systemic infections caused by Gram-positive and Gram-negative bacteria. Against infection caused by S. aureus Giorgio (MSSA), the ED₅₀ of Delpazolid is 4.53 mg/kg of body weight. Against S. aureus p125 (MRSA), the ED₅₀ of Delpazolid is 2.96 mg/kg^[1]. When Delpazolid (LCB-0371) is administered at 100 mg/kg daily (by gavage), the colony-forming unit (CFU) counts tend to be decreased in the lungs of mice at 7 days after infection^[2].