IMPDH Inosine monophosphate dehydrogenase inhibitors

Submitted by barbara on

Phenotypic screening with a biased target-specific screen. The inosine monophosphate dehydrogenase (IMPDH) protein GuaB2 has been identified as a drugable target in Mycobacterium tuberculosis, however previously identified compounds lack the desired characteristics necessary for further development into lead-like molecules. This study has identified 7 new chemical series from a high-throughput resistance based phenotypic screen using Mycobacterium bovis BCG over-expressing GuaB2.

Pretomanid - Moxifloxacin - Pyrazinamide Regimen

Submitted by zaidtanvir on

PaMZ was the first novel multi-drug TB treatment to undergo clinical testing in the new regimen development paradigm. PaMZ was tested in the Phase 2a NC-001 trial, in which it killed TB bacteria faster when compared with the current TB regimen, as well as other experimental regimens over the first two weeks of treatment. It was subsequently tested in NC-002, in which it met its primary endpoint after eight weeks treatment.

Pyrazinamide

Submitted by zaidtanvir on

Pyrazinamide (PZA) is one of the drugs used in standard, first-line TB therapy for drug-sensitive patients. It was discovered in 1954, though it wasn’t until approximately 30 years later that it became part of the standard TB treatment. Adding it to TB treatment enabled the shortening of treatment from 9 to 6 months. PZA is unique among current TB drugs in that it demonstrates impressive sterilizing activity and synergy with other drugs in animal models of TB but its activity itself is not potent against M.tb in a test tube.

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