TABLE 1.
Clinical trial(s) of AMPs under investigation and in clinical use.
| Peptide name | Description | Target | Administration | Phase | Clinical Trial ID | Mechanism | MW (g/mol) | Length | Net charge | References |
| Nisin | Polycyclic lantibiotic | Gram-positive bacteria | Oral | NCT02928042; NCT02467972 | Depolarization of cell membrane | 3354 | 34 | 4 | Prince et al., 2016 | |
| Gramicidin | Polycyclic peptide | Infected wounds and ulcers | Topical | III | NCT00534391 | Membrane disruption/immunomodulation | 1882 | 16 | 0 | David and Rajasekaran, 2015 |
| Polymyxin B | Cyclic polypeptide | Gram-negative bacteria | Topical | III | NCTOO490477; NCT00534391 | Membrane disruption/immunomodulation | 1204 | 10 | 5 | Morrison and Jacobs, 1976 |
| Polymyxin E (Colistin) | Cyclic polypeptide | A. baumannii/pneumonia | Intravenous | III | NCT01292031; NCT02573064 | Membrane disruption/immunomodulation | 1155 | 10 | 5 | Yu et al., 2015 |
| Daptomycin | Lipopeptide | Skin infection/bacteremia | Intravenous | III | NCT01922011; NCT00093067; NCT01104662; NCT02972983 | Membrane disruption/immunomodulation | 1621 | 13 | 0 | Taylor and Palmer, 2016 |
| LL-37 | Human cathelicidin | Leg ulcers | Topical | II | EUCTR2012-002100-41 | Membrane disruption/immunomodulation | 4491 | 37 | 6 | Brown et al., 2011 |
| Melittin | α-helical peptide | Inflammation | Intradermal | I/II | NCT02364349, NCT01526031 | Membrane disruption/immunomodulation | 2846.5 | 26 | 5 | Lee and Bae, 2016 |
| Friulimicin | Cyclic lipopeptide | MRSA/pneumonia | Intravenous | I | NCT00492271 | Membrane disruption | 1303.5 | 12 | −2 | Schneider et al., 2009 |
| Murepavadin (POL7080) | Analog of Protegrin | P. aeruginosa, K. pneumoniae | Intravenous | II | EUCTR2017-003933-27-EE | Binding to LptD | 1553.8 | 14 | 5 | Srinivas et al., 2010 |
| Neuprex® (rBPI21) | Derivative of BPI | Pediatric meningococcemia | Intravenous | III | NCT00462904 | Membrane disruption | ∼21000 | 193 | Schultz and Weiss, 2007 | |
| Iseganan (IB-367) | Analog of Protegrin | Pneumonia/oral mucositis | Topical | III | NCT00118781; NCT00022373 | Membrane disruption | 1900.3 | 17 | 4 | Orlov et al., 1805 |
| Surotomycin (CB-315) | Cyclic lipopeptide | C. difficile | Oral | III | NCT01597505 | Membrane disruption | 1680.8 | 13 | −3 | Alam et al., 2015 |
| Pexiganan (MSI-78) | Analog of Magainin | Diabetic foot ulcers | Topical | III | NCT00563394; NCT00563433; NCT01590758; NCT01594762 | Membrane disruption/immunomodulation | 2477.2 | 22 | 9 | Gottler and Ramamoorthy, 2009 |
| XOMA-629 (XMP-629) | Derivative of BPI | Impetigo/acne rosacea | Topical | III | Immunomodulation | 1158.4 | 9 | 3 | Easton et al., 2009 | |
| Omiganan (MBI-226) | Derivative of Indolicidin | Antisepsis/catheter infection | Topical | III | NCT00231153; NCT00608959 | Membrane disruption/immunomodulation | 1779.2 | 12 | 5 | Rubinchik et al., 2009 |
| NVB-302 | Lantibiotic | C. difficile | Oral | I | ISRCTN40071144 | Inhibition of cell wall synthesis | 1754.0 | 19 | 0 | Crowther et al., 2013 |
| OP-145 | Derivative of LL-37 | Chronic middle ear infection | Ear drops | I/II | ISRCTN84220089 | Membrane disruption/immunomodulation | 3093.8 | 24 | 6 | Malanovic et al., 2015 |
| P113 (PAC-113) | Fragment of Histatin-5 | Oral candidiasis | Mouth rinse | II | NCT00659971 | Membrane disruption/immunomodulation | 1564.8 | 12 | 5 | Woong et al., 2008 |
| LTX-109 | Synthetic tripeptide | MRSA/impetigo | Topical | I/II | NCT01803035; NCT01158235 | Membrane disruption | 788.1 | 3 | 2 | Isaksson et al., 2011; Sivertsen et al., 2014 |
| EA-230 | Oligopeptide | Sepsis | Intravenous | II | NCT03145220 | Immunomodulation | 415.5 | 4 | 0 | Van Groenendael et al., 2018 |
| SGX942 (Dusquetide) | Analog of IDR-1 | Oral mucositis | Oral rinse | III | NCT03237325 | Immunomodulation | 553.7 | 5 | 2 | Kudrimoti et al., 2016 |
| hLF1-11 | Fragment of human lactoferrin | Bacterial/fungal infections | Intravenous | I/II | NCT00430469 | Membrane disruption/immunomodulation | 1373.7 | 11 | 4 | Nibbering et al., 2001; Welling et al., 2018 |
| C16G2 | Synthetic peptide | Streptococcus mutans | Mouth wash | II | NCT03004365 | Membrane disruption | 4077.4 | 35 | 10 | Guo et al., 2015 |
| Novexatin (NP213) | Cyclic Cationic peptide | Fungal nail infection | Topical | II | NCT02933879 | Membrane disruption | 1093.3 | 7 | 7 | Mercer et al., 2020 |
| Ramoplanin (NTI-851) | Glycolipodepsipeptide | C. difficile, VRE | Oral | III | Inhibition of cell wall synthesis | 2568.1 | 17 | 2 | Fulco and Wenzel, 2006 | |
| p2TA (AB103) | Synthetic peptide | Necrotic tissue infection | Intravenous | III | Immunomodulation | 1037.2 | 8 | −1 | Bulger et al., 2014 | |
| D2A21 | Synthetic peptide | Burn wound infections | Topical | III | Membrane disruption | 2775.4 | 23 | 9 | Muchintala et al., 2020 | |
| Melamine | Chimeric peptide | Contact lenses microbials | Topical | II/III | Membrane disruption | 2786.6 | 29 | 15 | Yasir et al., 2019, 2020 | |
| Mel4 | Derivative of melamine | Contact lenses microbials | Topical | II/III | ACTRN1261500072556 | Membrane disruption | 2347.8 | 17 | 14 | Yasir et al., 2020 |
| LFF571 | Semisynthetic thiopeptide | C. difficile | Oral | II | NCT01232595 | Inhibition of protein synthesis | 1366.6 | Leeds et al., 2012 | ||
| Delmitide (RDP58) | Derivative of HLA | Inflammatory bowel disease | Topical | II | ISRCTN84220089 | Immunomodulation | 1228.6 | 10 | 2 | Travis et al., 2005 |
| DPK-060 | Derivative of Kininogen | Acute external otitis | Ear drops | II | NCT01447017 | Membrane disruption/immunomodulation | 2503.2 | 20 | 7 | Håkansson et al., 2019 |
| GSK1322322 (Lanopepden) | Synthetic hydrazide | Bacterial skin infection | Oral | II | NCT01209078 | Peptide deformylase inhibitor | 479.3 | Peyrusson et al., 2015 | ||
| PXL01 | Analog of Lactoferrin | Postsurgical adhesions | Topical | II | NCT01022242 | Immunomodulation | 3061.6 | 25 | 5 | Edsfeldt et al., 2017 |
| AP-214 | Derivative of α-MSH | Post-surgical organ failure | Intravenous | II | NCT00903604 | Membrane disruption/immunomodulation | 2433.9 | 19 | 7 | Doi et al., 2008 |
| PMX-30063 (Brilacidin) | Defensin mimetic | Acute bacterial skin infection | Intravenous | II | NCT01211470; NCT02052388 | Membrane disruption/immunomodulation | 936.9 | Mensa et al., 2014 | ||
| XF-73 (Exeporfinium chloride) | Derivative of porphyrin | Staphylococcal infection | Topical | II | NCT03915470 | Membrane disruption | 765.8 | Ooi et al., 2009 | ||
| CZEN-002 | Derivative of α-MSH | Antifungal | Topical | II | Immunomodulation | 971.2 | 8 | 2 | Csato et al., 1989 | |
| Ghrelin | Endogenous peptide | Chronic respiratory infection | Intravenous | II | NCT00763477 | Immunomodulation | 3314.9 | 28 | 5 | Gualillo et al., 2003 |
| Wap-8294A2 (Lotilibcin) | Produced by Lysobacter species | Gram-positive bacteria | Topical | I/II | Membrane disruption | 1562.8 | 12 | 1 | Itoh et al., 2017 | |
| PL-5 | Synthetic peptide | Skin infections | Topical | I | Membrane disruption | 2933.5 | 26 | 6 | Miyake et al., 2004 | |
| IDR-1 | Bactenecin | Infection prevention | Intravenous | I | Immunomodulation | 1391.7 | 13 | 3 | Yu et al., 2009 |
A. baumannii; Acinetobacter baumannii; BPI, bactericidal permeability increasing protein; C. difficile, Clostridium difficile; HLA, human leukocyte antigen; IDR, innate defense regulator; K. pneumoniae, Klebsiella pneumoniae; LptD, lipopolysaccharide transport protein D; MRSA, methicillin-resistant Staphylococcus aureus; MSH, melanocyte-stimulating hormone; P. aeruginosa, Pseudomonas aeruginosa; VRE, vancomycin-resistant Enterococci.