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cipargamin

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Also known as KAE609, NITD609

Cipargamin (also known as KAE609 or NITD609) is a synthetic antimalarial compound belonging to the novel spiroindolone drug class. Developed by Novartis Institute for Tropical Diseases in Singapore, through a collaboration with the Genomics Institute of the Novartis Research Foundation (GNF), the Biomedical Primate Research Centre and the Swiss Tropical Institute, cipargamin represents a promising next-generation antimalarial drug currently undergoing Phase II clinical trials with a particular focus on safety evaluation. Cipargamin was awarded MMV Project of the Year 2009.

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Encyclopedic overview

10 sections
Contents
  • Mechanism of action
  • Structure-activity relationships
  • Clinical development
  • Phase I studies
  • Phase II studies
  • Intravenous formulation development
  • Adverse events
  • Resistance mechanisms
  • History
  • References

Cipargamin (also known as KAE609 or NITD609) is a synthetic antimalarial compound belonging to the novel spiroindolone drug class. Developed by Novartis Institute for Tropical Diseases in Singapore, through a collaboration with the Genomics Institute of the Novartis Research Foundation (GNF), the Biomedical Primate Research Centre and the Swiss Tropical Institute, cipargamin represents a promising next-generation antimalarial drug currently undergoing Phase II clinical trials with a particular focus on safety evaluation. Cipargamin was awarded MMV Project of the Year 2009.

==Mechanism of action== Cipargamin exerts its antimalarial activity by targeting PfATP4, a P-type Na+ ATPase located on the plasma membrane of Plasmodium parasites. By inhibiting this essential sodium pump, cipargamin disrupts the sodium homeostasis within the parasite, leading to cell swelling and ultimately parasite death. This mechanism of action distinguishes cipargamin from existing antimalarial drugs, including artemisinin derivatives and other peroxide-based compounds.

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