Lanopepden, also known as GSK-1322322 or GSK-322, is a potent and selective peptide deformylase inhibitor with good in vitro activity against bacteria associated with community-acquired pneumonia and skin infections. GSK1322322 had bactericidal activity against S. pneumoniae, H. influenzae, S. pyogenes, and S. aureus, demonstrating a ≥ 3-log(10) decrease in the number of CFU/ml at 4× MIC within 24 h in 29 of the 33 strains tested. GSK1322322 represents a valuable alternative therapy for the treatment of infectious diseases caused by drug-resistant pathogens.