OPC-167832

Description: OPC-167832 is a novel carbostyril derivative developed by Otsuka with potent antituberculosis activity, acting as a DprE1 (decaprenylphosphoryl-beta-d-ribose 2?-oxidase) Inhibitor. In a mouse model of chronic TB, OPC-167832 showed potent bactericidal activities starting at a dose of 0.625?mg/kg of body weight. Further, it exhibited significant combination effects in 2-drug combinations with delamanid, bedaquiline, or levofloxacin. Finally, 3- or 4-drug regimens comprised of delamanid and OPC-167832 as the core along with bedaquiline, moxifloxacin, or linezolid showed efficacy in reducing the bacterial burden and preventing relapse superior to that of the standard treatment regimen.

References: Chem Rev. 2018 Feb 28; 118(4): 1887–1916.