2-[4-(CYCLOHEXYLMETHYL)-1-PIPERAZINYL]-8-NITRO-6-(TRIFLUOROMETHYL)-4H-1,3-BENZOTHIAZIN-4-ONE (Macozinone, PBTZ169) is a piperazinobenzothiazinone derivative optimized by medicinal chemistry from the lead BTZ043. Macozinone is a tuberculosis (TB) drug candidate that specifically targets the essential flavoenzyme DprE1, thereby blocking synthesis of the cell wall precursor decaprenyl phosphoarabinose (DPA) and provoking lysis of Mycobacterium tuberculosis. The company Nearmedic Plus leads PBTZ169 development for the Russian market and associated countries and has completed an open-labelled, dose-escalation phase I study in healthy male volunteers followed by a Multiple Ascending Dose in 2016. In 2017, a phase IIa EBA study (monotherapy during 14 days) was initiated in DS-TB patients in Russia and Belarus. It was completed in February 2018 with 16 patients enrolled. Nearmedic Plus indicated it confirmed the good safety in DS-TB patients and the statistically significant EBA after 14 days monotherapy in the group of 7 patients treated with 640 mg of PBTZ169. The EPFL-based non-profit Innovative Medicines for Tuberculosis (iM4TB) foundation (Lausanne, Switzerland) is leading PBTZ169 development in the rest of the world.