i.v., intravenous; FDA, Food and Drugs Administration.
Cationic antimicrobial peptides: update of clinical development
Article first published online: 22 MAR 2004
Journal of Internal Medicine
Volume 255, Issue 4, pages 519–520, April 2004
How to Cite
Andrès, E. and Dimarcq, J. L. (2004), Cationic antimicrobial peptides: update of clinical development. Journal of Internal Medicine, 255: 519–520. doi: 10.1046/j.1365-2796.2003.01278.x
- Issue published online: 22 MAR 2004
- Article first published online: 22 MAR 2004
We read with interest the paper of Boman about antibacterial peptides . It is an excellent and complete review and although the pharmaceutical value of these antibacterial peptides is still to be fully established, we think that there is no doubt that these compounds represent one of the most innovative families of anti-infective agents that have been characterized over the last 25 years. In this letter, we report additional informations about clinical development of these antimicrobial peptides, particularly about the cationic antimicrobial peptides [2, 3]. In fact, these compounds are emerging as ‘veritable’ drugs with several potential applications in future clinical practice. At present, several cationic antimicrobial peptides are being investigated or have completed phase III clinical trials, in topical and/or parenteral use. Our biotechnology company Entomed SA has characterized over 175 novel molecules from around 100 different species of insects (http://www.entomed.com). These compounds are already resulting in promising lead compounds being taken forward into clinical development. One example, ETD151, an antifungal 44 amino acid peptide, variant of a natural peptide from lepidopteran Heliothis virescens, is now in advanced preclinical development for the treatment of life-threatening invasive fungal infections (Table 1) . Other lead compounds are based on native defensin peptides, from a variety of insect species, which have been modified to improve their biological profiles against Gram-positive bacteria.
|Compound||Biotechnology company||Structural characteristics||Species||Topical or parenteral use||Indications – phase of clinical trials|
|Pexiganan (MSI-78)||Magainin Pharmaceuticals||α-helices||Skin of xenop||Cream||Impetigo and diabetic foot ulcer infections – phase III trial|
|Iseganan (IB-367)||Intrabiotics Pharmaceuticals||Peptides that contain disulphide bridges||Leucocytes of pig||Oral solutions||Anticancer therapies, induced oral mucosistis – phase III trial|
|Aerosol||Lung infections in cystic fibrosis patients and ventilator-associated pneumonia – phase I trial|
|Peptides MBI (MBI-226)||Micrologix Biotech||α-helices||Not communicated||Cream||Catheter-related bloodstream infections – phase III trial; acute acne and nasal carriage of Staphylococcus aureus– phase I trial|
|Histatine variants||Periondotix||α-helices||Human||Oral solutions (Histawash and Histagel)||Gingivitis and mouth infections – phase II trial; oral candidiasis and Pseudomonas aeruginosa lung infections – phase I trial|
|Heliomocin variants (ETD151)||Entomed SA||Peptides that contain disulphide bridges||Insect: lepidopteran Heliothis virescens||Parenteral use (i.v.)||Systemic deep and invasive fungal infections, immunocompromised patients – preclinical development|
|Insect defensin variants||Systemic multiresistant Gram-positive bacterial infections – preclinical development|
|Neuprex (RBPI 21)||Xoma Ltd||α-helices||Human||Parenteral use (i.v.)||Pediatrics meningococcaemia phase III trial (Orphan Drug status from FDA)|
|Mycoprex (XMP366)||Xoma Ltd||α-helices||Human||Parenteral use (i.v.)||Systemic fungal infections|
Conflict of interest statement
No conflict of interest was declared.
- 2Les peptides antimicrobiens cationiques et leurs applications potentielles. Antibiotiques 2001; 3: 201–5.,