Identification of mCMQ069, a novel antimalarial with potential for a single-dose cure and/or 28-day chemoprevention

Anil K. Sen Gupta; James R. Pedroarena; Armen Nazarian; Jenya Antonova-Koch; Frank Weiss; Krittikorn Kümpornsin; Victor Chi; Ashley K. Woods; Kyoung-Jin Lee; Sean B. Joseph; Shuangwei Li; Jason Brittain; Eugenio L. de Hostos; James Duffy; Anne E. Cooper; Peter G. Schultz; Case W. McNamara; Arnab K. Chatterjee

doi:10.1101/2024.07.01.601566

MicrobiologybioRxivJul 1, 2024

Preprint

Identification of mCMQ069, a novel antimalarial with potential for a single-dose cure and/or 28-day chemoprevention

Anil K. Sen Gupta iD, James R. Pedroarena iD, Armen Nazarian, Jenya Antonova-Koch, Frank Weiss, Krittikorn Kümpornsin iD, Victor Chi iD, Ashley K. Woods, Kyoung-Jin Lee, Sean B. Joseph iD, Shuangwei Li iD, Jason Brittain, Eugenio L. de Hostos, James Duffy iD, Anne E. Cooper, Peter G. Schultz iD, Case W. McNamara iD, Arnab K. Chatterjee iD

Abstract

In efforts towards eliminating malaria, a discovery program was initiated to identify a novel antimalarial using KAF156 as a starting point. Following the most recent TCP/TPP guidelines, we have identified mCMQ069 with a predicted single oral dose for treatment ([~]40-106 mg) and one-month chemoprevention ([~]96-216 mg). We have improved unbound MPC and predicted human clearance by 18-fold and 10-fold respectively when compared to KAF156.

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