MmpL3 Inhibitors
Background
MmpL3 is responsible for the transport of mycolic acids in the form of trehalose monomycolate (TMM), the precursor of trehalose dimycolate (TDM) and mycolates bound to arabinogalactan that together forms the mycomembrane. Inhibition of the transporter activity of MmpL3 has showed potent anti-M. tb activity in vitro and in animal models. Two compounds from indolcarboxamide are under safety evaluation for selecting one preclinical candidate. Backup series have also demonstrated potent in vitro efficacy and are under optimization for ADME/Tox properties.