Author: Abay, Efrem ; Nchinda, Aloysius T. ; Silue, Kigbafori D. ; Rochford, Rosemary ; Blasco, Benjamin ; Solapure, Suresh M. ; Fish, Paul V. ; Burke, John E. ; McPhail, Jacob A. ; Duffy, James ; Vanaerschot, Manu ; Njoroge, Mathew ; Noviyanti, Rintis ; Angulo-Barturen, Iñigo ; Paquet, Tanya ; Siegl, Peter ; Birkholtz, Lyn-Marie ; Leroy, Didier ; Marfurt, Jutta ; White, Karen L. ; Wirjanata, Grennady ; Price, Ric N. ; Wittlin, Sergio ; Gamo, Francisco Javier ; Marsh, Kennan C. ; Mancama, Dalu ; Chibale, Kelly ; Wiesner, Lubbe ; Herreros, Esperanza ; Le Manach, Claire ; Taylor, Dale ; Coetzer, Theresa L. ; de Kock, Carmen ; Denti, Paolo ; Reader, Janette ; van der Watt, Mariëtte E. ; Gonzàlez Cabrera, Diego ; Basarab, Gregory S. ; Jiménez-Díaz, Maria Belén ; Brunschwig, Christel ; Donini, Cristina ; Charman, Susan A. ; Street, Leslie J. ; Lawrence, Nina ; Fidock, David A. ; Waterson, David ; Witty, Michael J. ; Smith, Dennis A.

01 Sep 2018·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

Q2 · MEDICINE

Article

Author: Abay, Efrem ; Nchinda, Aloysius T. ; Silue, Kigbafori D. ; Rochford, Rosemary ; Blasco, Benjamin ; Solapure, Suresh M. ; Fish, Paul V. ; Burke, John E. ; McPhail, Jacob A. ; Duffy, James ; Vanaerschot, Manu ; Njoroge, Mathew ; Noviyanti, Rintis ; Angulo-Barturen, Iñigo ; Paquet, Tanya ; Siegl, Peter ; Birkholtz, Lyn-Marie ; Leroy, Didier ; Cabrera, Diego Gonzàlez ; Marfurt, Jutta ; White, Karen L. ; Wirjanata, Grennady ; Price, Ric N. ; Wittlin, Sergio ; Chibale, Kelly ; Mancama, Dalu ; Gamo, Francisco Javier ; Marsh, Kennan C. ; Wiesner, Lubbe ; Herreros, Esperanza ; Le Manach, Claire ; Taylor, Dale ; Coetzer, Theresa L. ; de Kock, Carmen ; Denti, Paolo ; Reader, Janette ; van der Watt, Mariëtte E. ; Basarab, Gregory S. ; Jiménez-Díaz, Maria Belén ; Brunschwig, Christel ; Donini, Cristina ; Charman, Susan A. ; Street, Leslie J. ; Lawrence, Nina ; Fidock, David A. ; Waterson, David ; Witty, Michael J. ; Smith, Dennis A.

The 2-aminopyridine MMV048 was the first drug candidate inhibiting Plasmodium phosphatidylinositol 4-kinase (PI4K), a novel drug target for malaria, to enter clinical development. In an effort to identify the next generation of PI4K inhibitors, the series was optimized to improve properties such as solubility and antiplasmodial potency across the parasite life cycle, leading to the 2-aminopyrazine UCT943.

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Indication	Highest Phase	Country/Location	Organization	Date
Malaria	Discovery	ZA	University of Cape Town	-
Malaria	Discovery	ZA	MMV Medicines for Malaria Venture	-

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