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. Author manuscript; available in PMC: 2013 Sep 1.
Published in final edited form as: Expert Opin Drug Discov. 2013 Jul 6;8(9):1095–1116. doi: 10.1517/17460441.2013.807246

Table 1.

Antibacterial agents and non-antibiotic therapeutics in clinical trials for MRSA and other related bacterial infections.

Name Mode of Action Conditions Route(s) Status Investigator(s)/Ownership
Oritavancin Inhibition of peptidoglycan biosynthesis (a glycopeptide) Wound infections, Abscess, Systemic inflammation, cellulitis IV Phase III The Medicine Co. (Parsippany, NJ)
Dalbavancin Inhibition of peptidoglycan biosynthesis (a lipoglycopeptide) Abscess, wound infection, surgical site infection, cellulitis IV Phase III Pfizer
TD-1792 (Theravance) Inhibition of peptidoglycan biosynthesis Staphylococcal skin infection IV Phase II Theravance (San Francisco, CA)
Mupirocin and Chlorhexidine Inhibition of bacterial protein synthesis by inhibiting isoleucyl tRNA Synthase MRSA skin infection Intranasal, body wash Phase III Los Angeles Biomedical Research institute, (Los Angeles, CA)
Iclaprim Inhibition of Dihydrofolate reductase Complicated skin and skin structure infections IV Phase III (development terminated) Acino Holding (Basel, Switzerland)
XF-73 Depolarization of cytoplasmic membrane Staphylococcal skin infection Intranasal Phase II Destiny Pharma (Brighton, UK)
TP-434 Inhibition of bacterial protein synthesis by targeting ribosome Complicated intra-abdominal infections IV Phase II Tetraphase (Watertown, MA)
BC-3781 Inhibition of bacterial protein synthesis by targeting 50S ribosomal subunit Skin infections and bacterial pneumonia caused by MRSA Oral, IV Phase I Nabriva Therapeutics (Vienna, Austria)
BC-7013 Inhibition of bacterial protein synthesis by targeting 50S ribosomal subunit Skin and skin structure infections and CA-pneumonia Topical Phase I Nabriva Therapeutics (Vienna, Austria)
BC-3205 Inhibition of bacterial protein synthesis by targeting 50S ribosomal subunit Skin and skin structure infections and CA-pneumonia Oral Phase I Nabriva Therapeutics (Vienna, Austria)
RX-1741 Inhibition of bacterial protein synthesis by targeting 50S ribosomal subunit CA-pneumonia, Staphylococcal skin infections, Streptococcal infections, Abscess Oral Phase II Rib-X Pharmaceuticals (New Haven, CT)
Tedizolid Inhibition of bacterial protein synthesis by targeting 50S ribosomal subunit Skin and subcutaneous tissue infections Oral, IV Phase III Trius Therapeutics (San Diego, CA)/Bayer HealthCare
Tomopenem Inhibition of bacterial cell wall synthesis by binding to Penicillin Binding protein Nosocomial infections due to Gram-negative and –positive bacteria, including MRSA IV Phase II Daiichi-Sankyo (Tokyo, Japan)
Cethromycin (Restanza) Inhibition of bacterial protein synthesis by targeting 50S ribosomal subunit CA-bacterial pneumonia (The US FDA designated cethromycin an orphan drug for the prophylactic treatment of patients exposed to inhalation anthrax and in May 2007) Oral Phase III Abbott/Advanced Life Sciences, Inc. (Chicago, IL)
EDP-420 Inhibition of bacterial protein synthesis by targeting 50S ribosomal subunit CA-pneumonia Oral Phase II Enanta (Watertown, MA)
NXL 103 (XRP 2868) Inhibition of bacterial protein synthesis by targeting ribosomal subunits (synergistic effect) Acute bacterial skin and skin structure infections, CA- pneumonia Oral Phase II AstraZeneca
Delafloxacin Inhibition of bacterial Gyrase Acute bacterial skin and skin structure infections, Complicated skin and skin structure infections Oral, IV Phase II Rib-X (New Haven, CT)
LBM-415 Inhibition of bacterial protein synthesis by inhibiting peptide deformylase CA-respiratory tract infections Oral Phase I (development terminated) Novartis
GSK1322322 Inhibition of bacterial protein synthesis by inhibiting peptide deformylase Bacterial skin and skin structure infections and hospitalized CA- pneumonia Oral Phase II GlaxoSmithKline
Locilex (MSI-78 topical cream) Formation of an amphipathic α-helical peptide on membranes that induces pore or changes membrane permeability Diabetic foot infections caused by drug-sensitive and –resistant bacteria including MRSA, VRE, extended-spectrum β-lactamase producing bacteria Topical Phase III Dipexium Pharmaceuticals (White Plains, NY)
OligoG CF-5/20 Immunomodulating activity Lung infections in cystic fibrosis Inhalation Phase I Algipharma (Sandvika, Norway)
F598 Inhibition of virulence by targeting the PNAG carbohydrate of the bacterial capsule S. aureus and other clinically relevant bacteria IV Phase I Sanofi (Paris, France)