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JPC-3210

NOT Open Access | In Vivo Efficacy and Pharmacokinetics of the 2-Aminomethylphenol Antimalarial, JPC-3210, in the Aotus Monkey-Human Malaria Model

December 23, 2019 - 15:10 -- NOT Open Access
Author(s): 
McCallum F, Birrell GW, Chavchich M, Harris I, Obaldia N 3rd, Van Breda K, Heffernan GD, Jacobus DP, Shanks D, Edstein MD
Reference: 
Antimicrob Agents Chemother. 2019 Dec 16. pii: AAC.01538-19

Nonimmune Aotus monkeys infected with Plasmodium falciparum and Plasmodium vivax were cured of their infections when treated with a single oral dose of 5 mg/kg and 10 mg/kg of the 2-aminomethylphenol, JPC-3210, respectively.

Multi-omic characterisation of the mode of action of a potent new antimalarial compound, JPC-3210, against Plasmodium falciparum

December 23, 2019 - 14:43 -- Open Access
Author(s): 
Birrell GW, Challis MP, De Paoli A, Anderson D, Devine SM, Heffernan GD, Jacobus DP, Edstein MD, Siddiqui G, Creek DJ
Reference: 
Mol Cell Proteomics 2019 Dec 13. pii: mcp.RA119.001797.

The increasing incidence of antimalarial drug resistance to the first-line artemisinin combination therapies underpins an urgent need for new antimalarial drugs, ideally with a novel mode of action. The recently developed 2-aminomethylphenol, JPC-3210, (MMV 892646) is an erythrocytic schizonticide with potent in vitro antimalarial activity against multidrug-resistant Plasmodium falciparum lines, low cytotoxicity, potent in vivo efficacy against murine malaria, and favourable preclinical pharmacokinetics including a lengthy plasma elimination half-life.

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