Using a set of in-licensed macrolide
chemistry technologies, Cempra Pharmaceuticals Inc. is developing a pipeline
of macrolide antibiotics that it hopes will be effective against resistant bacteria
but have safety profiles similar to marketed macrolides. The company began Phase
I studies of CEM-101 in healthy volunteers this month.
Macrolides inhibit bacterial
protein synthesis by binding reversibly to a peptide tunnel on the 50S subunit
of the bacterial ribosome, thereby inhibiting translocation of peptidyl-tRNA.
This action is mainly bacteriostatic, but can also be bactericidal at high drug
concentrations.