The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity
Tubman, Venée N.
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CitationTubman, Venée N., Pedro Mejia, Boris E. Shmukler, Amy K. Bei, Seth L. Alper, James R. Mitchell, Carlo Brugnara, and Manoj T. Duraisingh. 2015. “The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity.” Antimicrobial Agents and Chemotherapy 60 (1): 613–16. https://doi.org/10.1128/aac.01668-15.
AbstractSenicapoc, a Gardos channel inhibitor, prevented erythrocyte dehydration in clinical trials of patients with sickle cell disease. We tested the hypothesis that senicapoc-induced blockade of the Gardos channel inhibits Plasmodium growth. Senicapoc inhibited in vitro growth of human and primate plasmodia during the clinical blood stage. Senicapoc treatment suppressed P. yoelii parasitemia in vivo in C57BL/6 mice. The reassuring safety and biochemical profile of senicapoc encourage its use in antimalarial development.
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