Cipargamin (PD058147, CKLPLPZSUQEDRT-WPCRTTGESA-N)

Structure formats

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[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]

Description

(extracted from source data)

DESCRIPTION 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 and awarded MMV Project of the Year (2009).
The active enantiomer is shown here, with the 1R,3S configuration essential for antimalarial activity .
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 .

DESCRIPTION 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 and awarded MMV Project of the Year (2009).
The active enantiomer is shown here, with the 1R,3S configuration essential for antimalarial activity .
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 P-type ATPase4 (PfATP4) may be the target .

DESCRIPTION Cipargamin (NITD609) is an potent antimalarial compound, with an IC50 of appr 1 nM against P. falciparum.

PRICE 114

DESCRIPTION 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 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. (GtoPdb)

DESCRIPTION Cipargamin (NITD609) is an effective antimalarial compound. It has an IC50 of appr 1 nM against P. falciparum. (TargetMol Bioactive Compound Library)