MMV085203

MMV085203 (20-120 nM; 6 months) generates in vitro evolution of Plasmodium falciparum 3D7 strain clones with 4- to 6-fold reduced sensitivity (IC₅₀ range: 213.9 to 311.6 nM) via nonsynonymous mutations in the pfmfr3 gene^[1].
MMV085203 shows reduced sensitivity in Plasmodium falciparum Dd2 MFR3‑KO and 3D7 Q487E mutants, increased sensitivity upon PfMFR3 overexpression, and unchanged sensitivity with yeast DHODH overexpression, confirming its action independent of cytochrome bc1 inhibition^[1].
MMV085203 inhibits the growth of mature sexual-stage Plasmodium falciparum with an IC₅₀ of 2.9 μM^[1].
MMV085203 inhibits the growth of Plasmodium falciparum laboratory strains (3D7, W2mef, Dd2, NF54, K1) with an average IC₅₀ of 327.7 nM^[2].
MMV085203 inhibits the growth of twenty Plasmodium falciparum clinical isolates with an average IC₅₀ of 90.48 nM, demonstrating greater potency against clinical isolates than laboratory strains^[2].
MMV085203 inhibits the growth of combined Plasmodium falciparum laboratory strains and clinical isolates with an average IC₅₀ of 176.6 nM^[2].
MMV085203 inhibits the growth of Plasmodium falciparum clinical isolates with two parasite genotypes with an average IC₅₀ of 37.79 nM, and isolates with more than two parasite genotypes with an average IC₅₀ of 14.69 nM, demonstrating greater potency against clonally diverse isolates^[2].
MMV085203 inhibits Plasmodium falciparum thioredoxin reductase (PfTrxRd) activity with an EC₅₀ of 900 nM^[2].

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