GSK3036656 + BTZ-043

GSK3036656 + BTZ-043 is an investigational oral combination regimen under clinical development for the treatment of drug-sensitive pulmonary tuberculosis. - **GSK3036656** (also called *Ganfeborole*, AN10070, GSK656) is a boron-based small molecule inhibitor of *Leucyl-tRNA synthetase* (LeuRS) that blocks protein synthesis in Mycobacterium tuberculosis[9]. - **BTZ-043** is a novel benzothiazinone antibiotic targeting *Decaprenylphosphoryl-beta-D-ribofuranose 2'-epimerase* (DprE1), interfering with arabinan synthesis required for cell wall formation in M. tuberculosis[2]. - The combination is being tested in early-phase clinical trials for its safety, tolerability, pharmacokinetics, and bactericidal activity in adults with rifampicin-sensitive tuberculosis[1][3][10]. - Both agents are orally administered small molecules targeting different essential bacterial processes for synergistic anti-TB effect. - Development is led by GSK3036656's developer GSK; BTZ-043 is developed by a consortium originally led by Helmholtz Zentrum München and partners.

Other names

Ganfeborole + BTZ-043AN10070 + BTZ-043