2017
DOI: 10.1038/nrdp.2017.50
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Malaria

Abstract: Malaria is caused in humans by five species of single-celled eukaryotic Plasmodium parasites (mainly Plasmodium falciparum and Plasmodium vivax) that are transmitted by the bite of Anopheles spp. mosquitoes. Malaria remains one of the most serious infectious diseases; it threatens nearly half of the world's population and led to hundreds of thousands of deaths in 2015, predominantly among children in Africa. Malaria is managed through a combination of vector control approaches (such as insecticide spraying and… Show more

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Cited by 565 publications
(620 citation statements)
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References 257 publications
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“…Some compounds like KAF156 and DSM265 have reported activity against liver schizonts in preclinical test (Burrows et al., ; Wells et al., ). Few compounds in the preclinical development pipelines are PA92 (aminopyrazole), DSM421 (triazolopyrimidine alternative to DSM265), MMV642943 (alternative to MMV048), DDD498, MMV253 (triaminopyrimidine), and AN762 (oxaborole; Phillips et al., ).…”
Section: New‐generation Antimalarial Drugsmentioning
confidence: 99%
See 1 more Smart Citation
“…Some compounds like KAF156 and DSM265 have reported activity against liver schizonts in preclinical test (Burrows et al., ; Wells et al., ). Few compounds in the preclinical development pipelines are PA92 (aminopyrazole), DSM421 (triazolopyrimidine alternative to DSM265), MMV642943 (alternative to MMV048), DDD498, MMV253 (triaminopyrimidine), and AN762 (oxaborole; Phillips et al., ).…”
Section: New‐generation Antimalarial Drugsmentioning
confidence: 99%
“…However, the decreased activity of KAF156 is not only regulated by the mutation of PfCARL alone; mutation in few other genes is also affecting the role of KAF156 . Currently, the drug is in the pipeline of clinical trials in combination with lumefantrine (Ashley & Phyo, ; Phillips et al., ). The imidazolopiperazines target multiple stages of the parasite: asexual stage, sexual stage, and liver stage schizonts (Burrows et al., ; Gamo, ; Kuhen et al., ; Leong et al., ; Phillips et al., ; Phyo & Seidlein, ; Satish et al., ; White et al., ).…”
Section: New‐generation Antimalarial Drugsmentioning
confidence: 99%
“…Malaria, caused by the genus Plasmodium ( P. falciparum, P. vivax, P. malariae, P. ovale , and P. knowlesi ), remains a global public health concern due to its morbidity and mortality. [ 1,2 ] The World Health Organization (WHO) estimated that around 3.3 billion people live in areas at risk for malaria transmission and 219 million malaria cases with 435,000 deaths occurred throughout the world in 2017. [ 3 ] The deployment of artemisinin‐based combination therapies (ACTs) is indispensable for the treatment of malaria.…”
Section: Introductionmentioning
confidence: 99%
“…810 A recent evidence suggests that additional resistance mechanisms may also be emerging, 11 and of particular concern is the increased association between ACT treatment failures and resistance toward the partner compound. 3,12 The emergence of ACT resistance combined with treatment failures with other antimalarial agents (e.g., chloroquine and sulfadoxine/pyrimethamine) highlights the need for new drug development for the treatment of malaria.…”
Section: Introductionmentioning
confidence: 99%
“…3,13,14 This effort has led to the identification of four new compounds that are currently in phase II clinical development, including a fully synthetic peroxide OZ439 , 15,16 a novel imidazolopiperazine KAF156 (17) of an unknown mechanism of action, a spiroindolone KAE609 (18) that inhibits P. falciparum ATP4, and DSM265 ( 1 ) 19 (Figure 1), an inhibitor of Plasmodium dihydroorotate dehydrogenase (DHODH). A number of additional compounds are either in phase I clinical development or undergoing preclinical testing.…”
Section: Introductionmentioning
confidence: 99%