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

Author:

Sarathy Jickky Palmae,Zimmerman Matthew D.,Gengenbacher MartinORCID,Dartois VéroniqueORCID,Dick ThomasORCID

Abstract

ABSTRACTThe 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.

Publisher

Cold Spring Harbor Laboratory

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