Novel compounds with activity against multi-resistant bacteria

Seeking pharmaceutical companies for further development

SUMMARY OF INVENTION

Researchers at UiT have developed a novel class of antibiotics inspired by small marine antimicrobials and antimicrobial peptides that display high activity against 30 multiresistant clinical isolates of Gram-negative and Gram-positive bacteria. In vitro studies against multi-resistant clinical isolates reveals antimicrobial activity with minimum inhibitory concentration (MIC) values in the range 2 – 16 μg/ml; including activity against ESBL -CARBA producing and colistin resistant bacteria (table). Importantly, the compounds show good selectivity for bacteria vs. human cells (RBCs, HepG2, MRC5). Both compound optimization, toxicity studies and in-vivo efficacy studies are ongoing.

 

Key Properties

  • Highly potent against clinical isolates of multi-resistant Gram-negative bacteria
  • Small cyclic/rigid amphipathic peptidomimetics with a membrane disrupting mode-of-action
  • Simple synthesis that allows for easy variation of functional groups and synthesis scale-up
  • Non-chiral molecules; hence avoidance of enantiomers with undesired effects
  • Rapid killing of bacteria & Novel MoA imply less risk of resistance development (Active against biofilm producing bacteria)

 

Advantages & applications

  • The method of synthesis allows easy variation in the structure of functional groups
  • Non-chiral molecules; hence no enantiomers with undesired effects
  • Novel membrane lytic mode of action; ongoing studies to identify other targets

 

The compounds show activity against Gram-positive and Gram-negative bacteria, including against multi-drug resistant isolates. We foresee several ways the compounds may be developed for clinical use:

  • Novel class of antibiotics against multi-resistant bacteria
  • The novel MoA may imply less danger of resistance development

 

 

Status and Further development

The compounds are in lead optimization phase and will require further testing and development before before pre-clinical development. We are now looking for a commercial partner which can contribute towards directing further development towards a license. Patent application is filed.

 

 

Licensing Opportunity

We are seeking established companies in the field of antibiotics interested in developing a new treatment against multi-resistant Gram-negative and Gram-positive bacteria.

 

Key info


Origin


Table: Antimicrobial activity of a representative compound against five clinical isolates of each of multi-resistant S. aureusE. faeciumE. coliP. aeruginosaK. pneumonia and A. baumanii. In total 30 multi-resistant clinical isolates.

Clinical isolates* MIC in μg/ml
S. aureus  2
E. faecium  2 – 4
E. coli  4
P. aeruginosa  8 – 16
K. pneumoniae  4
A. baumanii  4 – 8

*Activity against five clinical isolates of each bacteria.



Inventor(s)

Morten B. Strøm
Annette Bayer
Stig Olov Magnus Engqvist
Marianne Hegensen Paulsen
Dominik Ausbacher




Contact Person


Anne-Karin Måseide
Business developer
(+47) 97726705
LinkedIn
anne-Karin(a)norinnova.no

Norinnova Technology Transfer AS