- Guide to PHARMACOLOGY
Synonyms: KAE609 | NITD609
Compound class: Synthetic organic
Comment: Cipargamin is an antimalarial drug candidate, under clinical development. It is the optimised lead for the spiroindolones, a novel class of compounds identified from a phenotypic screen as having antimalarial activity [2,7] and awarded MMV Project of the Year (2009).
The active enantiomer is shown here, with the 1R,3S configuration essential for antimalarial activity .
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|Guide to Malaria Pharmacology Comments|
|Cipargamin has potent activity against the asexual blood stages of P. falciparum and P. vivax  and potential as a transmission-blocking therapy with a study reporting that the drug inhibits gametocytogenesis and blocks P. falciparum transmission to the Anopheles mosquito vector .
Potential Target/Mechanism Of Action: A number of studies have investigated the mechanism of action of cipargamin, with evidence from genetic experiments indicating Plasmodium non-SERCA-type Ca2+-transporting P-ATPase (PfATP4) may be the target [1-2].
|Target Candidate Profiles|
|Profile||Intended Use||Target Stage||Comment||References|
|TCP-1||reduce parasite burden||asexual blood stages|