BTZ-043

BTZ‑043 is a first-in-class benzothiazinone small molecule antibiotic developed for the treatment of tuberculosis (TB), including multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains. It acts by selectively and irreversibly inhibiting the enzyme decaprenyl-phosphoribose 2′‑epimerase (DprE1), which is essential for the synthesis of D-arabinofuranose—a key component of mycobacterial cell wall arabinogalactan and arabinomannan. This mechanism is highly selective for Mycobacterium species and does not affect gut flora[2][3][6][7][8]. BTZ‑043 has demonstrated potent bactericidal activity in preclinical models and early clinical trials; it shows efficacy against all tested Mtb strains with low minimum inhibitory concentrations. Clinical studies have shown good tolerability and safety in humans up to phase IIa trials[3][5][6]. The drug was discovered at Leibniz Institute for Natural Product Research and Infection Biology – Hans Knöll Institute (Leibniz-HKI), with further development by a consortium including DZIF (German Center for Infection Research), LMU Munich’s Tropical Institute, InfectControl, UNITE4TB consortium partners[3].

Other names

2-((2s)-2-methyl-1,4-dioxa-8-azaspiro(4.5)decan-8-yl)-8-nitro-6-trifluoromethyl-4h-1,3-benzothiazin-4-one4h-1,3-benzothiazin-4-one, 2-((2s)-2-methyl-1,4-dioxa-8azaspiro(4.5)dec8yl)-8-nitro6-(trifluoromethyl)