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Technology

Bacterial resistance to  antibiotics is a major and fast growing health problem

  • Pharma Holdings is addressing the problem with it’s 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’ focus is on topical treatment of skin infections and nasal eradication of staphylococci, regardless of resistance
  • Pharma Holdings’ infection drug candidate has proven efficacy against a broad range of resistant organisms
  Highlights LTX-109:
  •     A synthetic protein fragment; a peptidomimetic
  •     High stability against degradation
  •     Produced in large scale
  •     Low cost of synthesis
 
 
 
 
 

About Lytixar™ (LTX-109)
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 bacteriocidal 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.

 

LTX-109 Characteristics

LTX-109 toxicology and safety

Lack of resistance development

In general, compounds acting on the cell membrane have low propensity for developing resistance. The occurrence of spontane-ous resistance towards LTX-109 was studied by plating a heterogeneous mixture of bacteria. Neither in wild-type, MRSA nor glyco-peptide-resistant Staphylococcus arueus was any spontaneous resistance observed. No signs of resistance development have been observed in 5 different Staphylococcus aureus strains after 14 passages.

LTX-109 kills MRSA better than ‘Gold Standard’ drugs

  • Murine skin infection model (tape-stripping, ATCC 33591
  • Read-out: bact growth +9 hours after the first of 3 doses

Outstanding efficacy in animal models

In vivo efficacy has been investigated at Statens Serum Institut (SSI) in Copenhagen, Denmark, and NAEJA, Canada, using a well-documented skin infection model.
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).

Highly effective on MRSA wound biofilm​

Green indicate living cells and red indicate dead cells

LTX-109 reduces CA-MRSA (USA300) significantly faster than Mupirocin

  • Tape-stripping and scalpel blade cut injury
  • TID treatment (every 3 hours)
  • Bacterial tissue load determined by CFU from skin biopsies

LTX-109 is as fungicidal as Amphotericin B

  • T

LTX-109 kills S. aureus and S. pyogenes more effectively than ‘Gold Standard’ drugs

  • Murine skin infection model (razor/tape-stripping)
  • Read-out is bacterial growth +9 hours after the first of 3 doses

LTX-109 is rapidly bactericidal

The rapid onset of LTX-109 activity gives opportunity for combination treatments.

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