Novel Nucleoside-based Antiprotozoan Drugs


Infectious diseases caused by parasites are a serious global health problem with significant rates of morbidity and mortality. Due to the emergence of treatment-resistant strains of many pathogens, there is a clear need for novel approaches to infectious disease treatment.

Description of Technology

University of Calgary researchers have developed a library of small molecule pro-drugs that are converted into toxic metabolites by enzymes unique to bacteria and protozoa. These enzymes are not found in humans, potentially making these drugs less toxic to the infected host.

Lead molecules identified from in vitro infectivity assays have IC50 values of 120nM and 60nM for L. donovani (which causes Leishmaniasis, the second largest parasitic killer in the world) and P. falciparum (which causes Malaria, the world's largest parasitic killer), respectively.

  • Lead molecules identified by in vitro infectivity assays are effective against two prevalent parasitic diseases in the world:
    • The malarial parasite, P. falciparum - 216 million cases of malaria were reported in 2016 resulting in 445,000 deaths, IC50 value 60nM
    • The Leishmaniasis parasite, L. donovani - 1.6 million people were estimated to be infected by this parasite in 2013, ∼400,000 people were infected with the fatal visceral form of the disesase, IC50 value 120nM
Areas of Application
  • Infectious disease treatment
IP Status
  • Patent Pending
Competitive Advantages
  • Compounds target fundamental, evolutionary conserved enzymes of the purine salvage pathway present in protozoa and bacteria, but not mammals
  • Lead molecules demonstrate in vitro activity in the nM range with minimal toxicity in mammalian cells
Stage Of Development
  • Library of ∼100 small molecules, many of which are novel, have been synthesized and evaluated in vitro for activity against a variety of parasites
  • Lead molecules have been identified with in vitro activity against L. donovani and P. falciparum
  • Seeking industry partners to assist in the evaluation of these compounds in animal models of disease and pre-clinical development