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Identification of mCMQ069, a novel antimalarial with potential for a single-dose cure and/or 28-day chemoprevention.

Anil Kumar GuptaJames PedroarenaArmen NazarianJenya Antonova-KochFrank WeissKrittikorn KumpornsinVictor ChiAshley K WoodsKyoung-Jin LeeSean B JosephShuangwei LiJason BrittainEugenio De HostosJames DuffyAnne CooperPeter G SchultzCase W MacNamaraArnab K Chatterjee
Published in: bioRxiv : the preprint server for biology (2024)
In efforts towards eliminating malaria, a discovery program was initiated to identify a novel antimalarial using KAF156 as a starting point. Following the most recent TCP/TPP guidelines, we have identified mCMQ069 with a predicted single oral dose for treatment (∼40-106 mg) and one-month chemoprevention (∼96-216 mg). We have improved unbound MPC and predicted human clearance by 18-fold and 10-fold respectively when compared to KAF156.
Keyphrases
  • plasmodium falciparum
  • quality improvement
  • endothelial cells
  • small molecule
  • clinical practice
  • induced pluripotent stem cells
  • human health
  • risk assessment
  • bioinformatics analysis