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antimalarial drug

Reproducibility of malaria sporozoite challenge model in humans for evaluating efficacy of vaccines and drugs: a systematic review

December 28, 2021 - 20:55 -- Open Access
Shibeshi W, Bagchus W, Yalkinoglu Ö, Tappert A, Engidawork E, Oeuvray C
BMC Infect Dis. 2021 Dec 20;21(1):1274

The development of novel malaria vaccines and antimalarial drugs is limited partly by emerging challenges to conduct field trials in malaria endemic areas, including unknown effects of existing immunity and a reported fall in malaria incidence. As a result, Controlled Human Malaria Infection (CHMI) has become an important approach for accelerated development of malarial vaccines and drugs. We conducted a systematic review of the literature to establish aggregate evidence on the reproducibility of a malaria sporozoite challenge model.

Our Exciting Journey to ACT-451840

December 1, 2021 - 19:47 -- Open Access
Boss C, Wittlin S
Chimia (Aarau). 2021 Nov 24;75(11):916-922

We describe our work resulting in the selection of ACT-451840 ( 38 ) as a novel antimalarial drug with a novel mode of action. The compound was broadly characterized in vitro as well as in vivo in rat PK experiments as well as two different mouse malaria models.

Not Open Access | Simultaneous estimation of ZY-19489 and its active metabolite ZY-20486 in human plasma using LC-MS/MS, a novel antimalarial compound

November 17, 2021 - 09:24 -- NOT Open Access
Ghoghari AM, Patel HV, Nayak NN, Mansuri TH, Pillai SM, Jain MR, Patel HB, Kansagra K, Resta ID, Möhrle J, Parmar DV
Bioanalysis. 2021 Nov 15

ZY-19489 is a new antimalarial drug candidate and selective LC–MS/MS method was established for estimation of ZY-19489 and its metabolite in human plasma.

NOT Open Access | The transmission-blocking effects of antimalarial drugs revisited: fitness costs and sporontocidal effects of artesunate and sulfadoxine-pyrimethamine

October 30, 2021 - 11:59 -- NOT Open Access
Villa M, Buysse M, Berthomieu A, Rivero A
Int J Parasitol. 2021 Mar;51(4):279-289

Assays used to evaluate the transmission-blocking activity of antimalarial drugs are largely focused on their potential to inhibit or reduce the infectivity of gametocytes, the blood stages of the parasite that are responsible for the onward transmission to the mosquito vector. For this purpose, the drug is administered concomitantly with gametocyte-infected blood, and the results are evaluated as the percentage of reduction in the number of oocysts in the mosquito midgut. We report the results of a series of experiments that explore the transmission-blocking potential of two key antimalarial drugs, artesunate and sulfadoxine-pyrimethamine, when administered to mosquitoes already infected from a previous blood meal.

NOT Open Access | Safety, Pharmacokinetics, and Causal Prophylactic Efficacy of KAF156 in a Plasmodium falciparum Human Infection Study

October 13, 2021 - 12:43 -- NOT Open Access
Kublin JG, Murphy SC, Prince WT, et al.
Clin Infect Dis. 2021 Oct 5;73(7):e2407-e2414

KAF156 is a novel antimalarial drug that is active against both liver- and blood-stage Plasmodium parasites, including drug-resistant strains. Here, we investigated the causal prophylactic efficacy of KAF156 in a controlled human malaria infection (CHMI) model.

Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome

October 5, 2021 - 10:41 -- Open Access
Xie SC, Metcalfe RD, Tilley L, et al.
Proc Natl Acad Sci U S A. 2021 Sep 28;118(39):e2107213118

The Plasmodium falciparum proteasome is a potential antimalarial drug target. We have identified a series of amino-amide boronates that are potent and specific inhibitors of the P. falciparum 20S proteasome (Pf20S) β5 active site and that exhibit fast-acting antimalarial activity. They selectively inhibit the growth of P. falciparum compared with a human cell line and exhibit high potency against field isolates of P. falciparum and Plasmodium vivax They have a low propensity for development of resistance and possess liver stage and transmission-blocking activity.

Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs Artemether-Lumefantrine

September 23, 2021 - 08:35 -- Open Access
Volpe-Zanutto F, Fonseca-Santos B, Foglio MA, et al.
Biomed Mater. 2021 Sep 20

Artemether (ART) and lumefantrine (LUM) are the gold standard antimalarial drugs used for the treatment of malaria in children and pregnant women. Typically, ART and LUM are delivered orally in the form of a combined tablet, however, the appropriateness of this route of administration for these drugs is questionable due to the poor absorption and therefore bioavailability observed unless administered alongside lipid-rich foods.Transdermal drug delivery in the form of a patch-type system has been identified as a viable alternative to the conventional tablet-based therapy.

A Prioritized and Validated Resource of Mitochondrial Proteins in Plasmodium Identifies Unique Biology

September 14, 2021 - 09:32 -- Open Access
van Esveld SL, Meerstein-Kessel L, Huynen MA, et al.
mSphere. 2021 Sep 8:e0061421

Plasmodium species have a single mitochondrion that is essential for their survival and has been successfully targeted by antimalarial drugs. Most mitochondrial proteins are imported into this organelle, and our picture of the Plasmodium mitochondrial proteome remains incomplete. Many data sources contain information about mitochondrial localization, including proteome and gene expression profiles, orthology to mitochondrial proteins from other species, coevolutionary relationships, and amino acid sequences, each with different coverage and reliability.

Antimalarial drug resistance in the Central and Adamawa regions of Cameroon: Prevalence of mutations in P. falciparum crt, Pfmdr1, Pfdhfr and Pfdhps genes

August 25, 2021 - 16:18 -- Open Access
Tuedom AGB, Sarah-Matio EM, Nsango SE, et al.
PLoS One. 2021 Aug 19;16(8):e0256343

The spread of Plasmodium falciparum resistant parasites remains one of the major challenges for malaria control and elimination in Sub Saharan Africa. Monitoring of molecular markers conferring resistance to different antimalarials is important to track the spread of resistant parasites and to optimize the therapeutic lifespan of current drugs. This study aimed to evaluate the prevalence of known mutations in the drug resistance genes Pfcrt, Pfmdr1, Pfdhfr and Pfdhps in two different epidemiological settings in Cameroon. Dried blood spots collected in 2018 and 2019 from asymptomatic individuals were used for DNA extraction and then the Plasmodium infection status was determined byPCR.

NOT Open Access | Associations between varied susceptibilities of PfATP4 inhibitors and genotypes in Ugandan Plasmodium falciparum isolates

August 4, 2021 - 15:56 -- NOT Open Access
Kreutzfeld O, Rasmussen SA, Rosenthal PJ, et al.
Antimicrob Agents Chemother. 2021 Aug 2:AAC0077121

Among novel compounds under recent investigation as potential new antimalarial drugs are three independently developed inhibitors of the Plasmodium falciparum P-type ATPase (PfATP4): KAE609 (cipargamin), PA92, and SJ733. We assessed ex vivo susceptibilities to these compounds of 374 fresh P. falciparum isolates collected in Tororo and Busia districts, Uganda from 2016-2019. Median IC50s were 65 nM for SJ733, 9.1 nM for PA92, and 0.5 nM for KAE609. Sequencing of pfatp4 for 218 of these isolates demonstrated many non-synonymous single nucleotide polymorphisms; the most frequent mutations were G1128R (69% of isolates mixed or mutant), Q1081K/R (68%), G223S (25%), N1045K (16%) and D1116G/N/Y (16%).


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