Compound ID | 643
Pretomanid
Synonym(s): PA-824 | PA 824 | PA824
Class: Nitroimidazole
| Agent Type: | Synthetic; Small molecule; Direct acting; |
| Spectrum of activity: | Antimycobacterial |
| Mechanism of action: | Mycolic acid synthesis inhibitor. Additionally inhibits protein synthesis |
| Target Pathogen: | Active against Mycobacterium tuberculosis |
| Description: | A nitroimidazopyran derivative; 1. Bake WR, Keeler EL, Cai S, et al. Identification of PA-834, a novel 6-nitroimidazopyran antitubercular agent, using high throughput synthesis and screening methodology. 36th-Intersci-Conf-Antimicrobial-Agents-Chemother 1996; 137. 2. Ritchie HD, Orta GJ, Harris LM, et al. Toxicology and toxicokinetics of PA-824 and PA 1297, two nitroimidazopyran antitubercular agents in mice. 37th-Intersci-Conf-Antimicrobial-Agents-Chemother 1997; 150. |
| Institute where first reported: | Pathogenesis Corp. (Chiron Corp., USA) |
| Year first mentioned: | 1997 |
| Highest development stage: | Phase 2 and Phase 3 |
| Development status: | Active |
| Reason dropped: | Poor oral bioavailability which although can be improved through use of lipid coated cyclodextrin formulations would increase cost a lot.; previous Clinical Phase Trial terminated due to failure to achieve the trial objective of identifying a new regimen to treat tuberculosis in 3 months or less |
| External links: | |
| PubChem link: | https://pubchem.ncbi.nlm.nih.gov/compound/456199 |
| Citations: |
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