The challenges of Chagas Disease have become a global issue. Increasing numbers of infected individuals are now found in places far from endemic areas of Latin America where 7.6 million people are estimated to be infected with the disease and 108 million are at risk [1]. Chagas disease is the result of human infection by the parasite Trypanosoma cruzi (T. cruzi) [2]. Research into new therapies must overcome a number of difficulties arising from the complex nature of the parasite's life cycle, its extensive impact on the body and the protracted nature of the illness. Modelling the disease in a laboratory setting is a significant challenge for drug discovery efforts.
Following a targeted screening campaign in 2008, we identified fenarimol, a fungal CYP51 inhibitor used in agriculture, as a suitable starting point for a drug discovery effort to develop new treatments for Chagas disease. Progression of fenarimol from a hit through to pre-clinical candidate status will be presented, with discussion of the medicinal chemistry, pharmacokinetic and biological challenges encountered in the development of an efficacious and affordable potential new treatment of this persistent intracellular parasite
[1] Tanowitz HB, Weiss LM, Montgomery SP (2011) Chagas Disease Has Now Gone Global. PLoS Negl Trop Dis 5(4): e1136. doi:10.1371/journal.pntd.0001136
[2] Nature Outlook 2010, 24th June