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The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity.

ABSTRACT: Senicapoc, 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.

SUBMITTER: Tubman VN

PROVIDER: S-EPMC4704178 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature

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The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity.

Tubman Venée N VN Mejia Pedro P Shmukler Boris E BE Bei Amy K AK Alper Seth L SL Mitchell James R JR Brugnara Carlo C Duraisingh Manoj T MT

Antimicrobial agents and chemotherapy 20151012 1

Senicapoc, 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 antim ...[more]

PMID: 26459896

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