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bioRxiv · 10.1101/2022.09.14.508059

Mycobacterium tuberculosis DprE1 inhibitor OPC-167832 is active against Mycobacterium abscessus in vitro

Sarathy, J. P.·Zimmerman, M.·Gengenbacher, M.·Dartois, V. A.·Dick, T.
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Abstract

The anti-tuberculosis candidate OPC-167832, an inhibitor of DprE1, was active against Mycobacterium abscessus. Resistance mapped to M. abscessus dprE1, suggesting target retention. OPC-167832 was bactericidal and did not antagonize activity of clinical anti-M. abscessus antibiotics. Due to its moderate potency compared to Mycobacterium tuberculosis, the compound lacked efficacy in a mouse model and is thus not a repurposing candidate. These results identify OPC-167832 - DprE1 as a lead-target couple for a M. abscessus-specific optimization program.

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Sarathy, J. P., Zimmerman, M., Gengenbacher, M., Dartois, V. A., Dick, T.. 2022-09-15. Mycobacterium tuberculosis DprE1 inhibitor OPC-167832 is active against Mycobacterium abscessus in vitro. https://doi.org/10.1101/2022.09.14.508059

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