Article
A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance.
Nature communications - 24 May 2017
O'Neill Paul M, Amewu Richard K, Charman Susan A, Sabbani Sunil, Gnädig Nina F, Straimer Judith, Fidock David A, Shore Emma R, Roberts Natalie L, Wong Michael H-L, Hong W David, Pidathala Chandrakala, Riley Chris, Murphy Ben, Aljayyoussi Ghaith, Gamo Francisco Javier, Sanz Laura, Rodrigues Janneth, Cortes Carolina Gonzalez, Herreros Esperanza, Angulo-Barturén Iñigo, Jiménez-Díaz María Belén, Bazaga Santiago Ferrer, Martínez-Martínez María Santos, Campo Brice, Sharma Raman, Ryan Eileen, Shackleford David M, Campbell Simon, Smith Dennis A, Wirjanata Grennady, Noviyanti Rintis, Price Ric N, Marfurt Jutta, Palmer Michael J, Copple Ian M, Mercer Amy E, Ruecker Andrea, Delves Michael J, Sinden Robert E, Siegl Peter, Davies Jill, Rochford Rosemary, Kocken Clemens H M, Zeeman Anne-Marie, Nixon Gemma L, Biagini Giancarlo A, Ward Stephen A
Abstract excerpt
K13 gene mutations are a primary marker of artemisinin resistance in Plasmodium falciparum malaria that threatens the long-term clinical utility of artemisinin-based combination therapies, the cornerstone of modern day malaria treatment. Here we describe a multinational drug discovery programme that has delivered a synthetic tetraoxane-based molecule, E209, which meets key requirements of the Medicines for...
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