Development of ELQ300 as a long acting antimalarial

ELQ-300 is a long-duration antimalarial currently positioned as a chemoprophylactic agent. The compound possesses a similar mechanism of action of atovaquone, a marketed chemoprophylactic agent to which resistance rapidly developed. ELQ-300 is active against atovaquone-resistant strains. Hence, in addition to its potential for long duration of coverage (ideal profile for chemoprotection), and it has a reduced resistance risk. ELQ300 could also have potential for single-dose treatment of malaria in combination with a fast-acting partner.

ELQ300 entered preclinical development in Q3 2012. The principal risks are associated with its very low solubility in aqueous and biorelevant media, which has hampered absorption in high doses in vivo DMPK (Distribution Metabolism and PharmacoKinetics) experiments and achievement of adequate levels of exposure to demonstrate therapeutic margins. The proposed partnership will enable extensive formulation work which, coupled with a standard preclinical development package, should allow establishment of a safety margin and progression into man.

Specifically, the areas to still be explored include lipid-based formulations, co-solvents, and amorphous dispersions. Frontrunner formulations would then be tested in rodents and dogs to confirm increased exposure of drug necessary for safety studies and further development

.Whilst this partnership is focused on a single workstream, the reformulation of the compound, it could be expanded in the future to include subsequent steps (i.e. GLP safety studies etc.), and could potentially form the basis for a longer-term partnership for the development and commercialization of ELQ-300 within a Japanese regulatory context.

Basic Science
Drug-based Strategies

Jan 2013

$216,790