MC-207110 Daiichi Seiyaku/Microcide Pharmaceuticals

Microcide and Daiichi are collaborating on the discovery of new bacterial efflux pump inhibitorsfor the treatment of drug-resistant Pseudomonas aeruginosa and other bacterial infections. The bacterial efflux pump technology program focuses on Gram-negative bacteria that have developed antibiotic resistance by means of the efflux pump [192681], [341408]. MC-207110 was the initial screening hitfrom Microcide's library and is a low molecular weight dipeptide amide, which shows minimal antibacterial activity but potentiated the activity of levofloxacin by 8-fold at 10 microg/ml. This lead is being optimized to improve on its biological and pharmacological profile [341183]. Optimization studies have been conducted on MC-207110, yielding a class of broad-spectrum efflux pump inhibitors for P aeruginosa. A member of this class has demonstrated in vivo activity against P aeruginosa in a murine neutropenic thigh model [351686].