Filarial nematode phenotypic screening cascade to identify compounds with anti-parasitic activity for drug discovery optimization

by Hawryluk NH, Zhiru L, Carlow C, Gokool S, Townson S, Kreiss T, Chojnowski A, Prorok M, Siekierka J, Ehrens A, Koschel M, Lhermitte-Vallarino N, Martin C, Hoerauf A, Hernandez G, Canan S, Khetani V, Zeldis, Specht S, Hübner MP, Scandale I. International Journal for Parasitology: Drugs and Drug Resistance 2022; 19:89-97. doi: 10.1016/j.ijpddr.2022.06.002

Summary: Drug discovery for onchocerciasis is challenging because of the lack of preclinical animal models using parasites that affect humans. The authors describe a platform to assess activity of test compounds that uses six surrogate parasites in ex vivo assays. This led to the successful establishment of a screening cascade and identification of multiple compounds with potential macrofilaricidal activity and desirable physicochemical and pharmacokinetic properties. Lead optimization efforts have been initiated on one of the two distinct chemical series identified.

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