Host Defence Peptides
- Pharma Holdings is addressing the problem with its drugs derived from host defence peptides through Structure-activity-relationship studies on Lactoferricin.
- Pharma Holdings’ infection drug candidate degrades the membranes of microorganisms
- Pharma Holdings’ current focus is on topical treatment of infections and nasal eradication of staphylococci pre-operatively
- Pharma Holdings’ infection drug candidate has proven efficacy against a broad range of resistant organisms
LTX-109 is an investigational antimicrobial drug with a novel membrane-lysing mechanism of action, based on the biological principle of innate immune effectors, lytic peptides. The drug has a rapid bactericidal lytic activity. The drug has been tested in vitro and in vivo models and has undergone a comprehensive nonclinical safety and toxicology program and been studied in man in a Phase I study, and two phase I/IIa studies. The drug is in development as a treatment for bacterial skin infections, fungal infections and nasal decolonisation of MRSA.
- A synthetic protein fragment; a peptidomimetic
- High stability against degradation
- Produced in large scale
Mechanism of Action
Antimicrobial peptides of multicellular organisms
Mechanism of lysing action. Illustration by Michael Zasloff, Department of Biochemistry and Biophysics, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104-6059, USA
- Murine skin infection model (tape-stripping, ATCC 33591
- Read-out: bact growth +9 hours after the first of 3 doses
Outstanding efficiency in animal models
A skin lesion is infected on day one, and the infection allowed to develop for 24 hours. The drug and comparators are applied 3 times in a single day. LTX-109 is strongly bactericidal against all strains of Staphylococci tested, including both hospital-acquired and community-acquired MRSA (USA300).
Green indicate living cells and red indicate dead cells
- Tape-stripping and scalpel blade cut injury
- TID treatment (every 3 hours)
- Bacterial tissue load determined by CFU from skin biopsies
LTX-109 is rapidly bactericidal
The onset of LTX-109 activity is rapid and dependent on concentration.