Synonyms: PBTZ169
Compound class:
Synthetic organic
Comment: Macozinone (PBTZ169) is the lead from a series of piperazine-containing benzothiazinones [1]. It has potent antimycobacterial activity and is under clinical evaluation as a treatment for tuberculosis (TB). Macozinone is an inhibitor of decaprenylphosphoryl-beta-D-ribose oxidase (DprE1), an essential mycobacterial cell wall biosynthesis enzyme [1].
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No information available. |
Summary of Clinical Use |
Macozinone is under clinical evaluation as a treatment for tuberculosis. Several Phase 1 studies have been completed (NCT03036163, NCT03423030, NCT03776500, NCT04150224) while a Phase 2 trial (NCT03334734) to evaluate early antibacterial activity was terminated (February 2018) due to slow enrollment. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT03334734 | Phase 2a Study of PBTZ169 | Phase 2 Interventional | Nearmedic Plus LLC | Study was terminated due to slow enrollment. | |
NCT03036163 | Phase 1 Study of PBTZ169 | Phase 1 Interventional | Nearmedic Plus LLC | ||
NCT04150224 | Safety, Tolerability, Pharmacokinetics and Food Effects Study of PBTZ169 | Phase 1 Interventional | Nearmedic Plus LLC | ||
NCT03776500 | Study to Evaluate the Safety, Tolerability and Pharmacokinetics of PBTZ169 in Multiple Dosing | Phase 1 Interventional | Innovative Medicines for Tuberculosis | ||
NCT03423030 | Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Ex-vivo Antitubercular Activity of PBTZ169 Formulation | Phase 1 Interventional | Innovative Medicines for Tuberculosis |