The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity | Zendy

Venée N. Tubman | Zendy; Pedro Mejia | Zendy; Boris E. Shmukler | Zendy; Amy K. Bei | Zendy; Seth L. Alper | Zendy; James R. Mitchell | Zendy; Carlo Brugnara | Zendy; Manoj T. Duraisingh | Zendy

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The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity

Author(s) -

Venée N. Tubman,

Pedro Mejia,

Boris E. Shmukler,

Amy K. Bei,

Seth L. Alper,

James R. Mitchell,

Carlo Brugnara,

Manoj T. Duraisingh

Publication year - 2015

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.01668-15

Subject(s) - pharmacology , chemistry , medicine

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.

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