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antimalarial drug

NOT Open Access | Liver-targeted polymeric prodrugs of 8-aminoquinolines for malaria radical cure

January 1, 2021 - 16:00 -- NOT Open Access
Srinivasan S, Roy D, Stayton PS, et al.
J Control Release. 2020 Dec 27:S0168-3659(20)30770-7

Primaquine and tafenoquine are the two 8-aminoquinoline (8-AQ) antimalarial drugs approved for malarial radical cure - the elimination of liver stage hypnozoites after infection with Plasmodium vivax. A single oral dose of tafenoquine leads to high efficacy against intra-hepatocyte hypnozoiites after efficient first pass liver uptake and metabolism. Unfortunately, both drugs cause hemolytic anemia in G6PD-deficient humans. This toxicity prevents their mass administration without G6PD testing given the approximately 400 million G6PD deficient people across malarial endemic regions of the world.

ATP2, the essential P4-ATPase of malaria parasites, catalyzes lipid-stimulated ATP hydrolysis in complex with a Cdc50 beta-subunit

December 30, 2020 - 13:33 -- Open Access
Lamy A, Macarini-Bruzaferro E, Dieudonné T, Perálvarez-Marín A, Lenoir G, Montigny C, le Maire M, Vázquez-Ibar JL
Emerg Microbes Infect. 2020 Dec 29:1-32

Gene targeting approaches have recently demonstrated the essential role for the malaria parasite of membrane transport proteins involved in lipid transport and in the maintenance of membrane lipid asymmetry, representing emerging oportunites for therapeutical intervention. This is the case of ATP2, a Plasmodium-encoded 4 P-type ATPase (P4-ATPase or lipid flippase), whose activity is completely irreplaceable during the asexual stages of the parasite. Moreover, a recent chemogenomic study has situated ATP2 as the possible target of two antimalarial drug candidates.

Ex vivo susceptibility of Plasmodium falciparum to antimalarial drugs in Northern Uganda

December 30, 2020 - 13:30 -- Open Access
Fukuda N, Tachibana SI, Mita T, et al.
Parasitol Int. 2020 Dec 25:102277

In Uganda, artemether-lumefantrine was introduced as an artemisinin-based combination therapy (ACT) for malaria in 2006. We have previously reported a moderate decrease in ex vivo efficacy of lumefantrine in Northern Uganda, where we also detected ex vivo artemisinin-resistant Plasmodium falciparum. Therefore, it is necessary to search for candidate partner alternatives for ACT.

NOT Open Access | Predicting the Disposition of the Antimalarial Drug Artesunate and its Active Metabolite Dihydroartemisinin Using Physiologically-Based Pharmacokinetic Modeling

December 29, 2020 - 15:33 -- NOT Open Access
Arey R, Reisfeld B
Antimicrob Agents Chemother. 2020 Dec 23:AAC.02280-20

Artemisinin-based combination therapies (ACTs) have proven to be effective in helping to combat the global malaria epidemic. To optimally apply these drugs, information about their tissue-specific disposition is required, and one approach to predict these pharmacokinetic characteristics is physiologically-based pharmacokinetic (PBPK) modeling. In this study, a whole-body PBPK model was developed to simulate the time-dependent tissue concentrations of artesunate (AS) and its active metabolite, dihydroartemisinin (DHA).

NOT Open Access | Recent advances in Quantitative Structure-Activity Relationship models of antimalarial drugs

December 29, 2020 - 15:15 -- NOT Open Access
Ojha PK, Kumar V, Roy J, Roy K
Expert Opin Drug Discov. 2020 Dec 26

Due to emerging resistance to the first-line artemisinin-based antimalarials and lack of efficient vaccines and limited chemotherapeutic alternatives, there is an urgent need to develop new antimalarial compounds. In this regard, quantitative structure-activity relationship (QSAR) modeling can provide essential information about required physicochemical properties and structural parameters of antimalarial drug candidates.

NOT Open Access | Recent advances in the development of chemotherapeutic agents for malaria

December 23, 2020 - 09:22 -- NOT Open Access
Shrivastava N, Khan SA, Ahmad S, Al Balushi K, Husain A
Mini Rev Med Chem. 2020 Dec 21

Malaria, a devastating infectious parasitic disease, has been recognized by the World Health organization (WHO) as a major public health problem worldwide. It is one of the leading causes of morbidity and mortality in the developing countries. There are fewer number of the antimalarial drugs available in the market to combat this deadly disease. The situation is further worsened due to the emergence of resistant strains of Plasmodium falciparum, which warrants the search for novel antimalarial drugs capable of acting at multiple targets to expand the current antimalarial drug arsenal for better therapeutic outcome.

A Systematic Literature Review of Microscopy Methods Reported in Malaria Clinical Trials

December 23, 2020 - 08:50 -- Open Access
Das D, Dahal P, Dhorda M, Citarella BW, Kennon K, Stepniewska K, Felger I, Chappuis F, Guerin PJ
Am J Trop Med Hyg. 2020 Dec 21

Microscopy of stained blood films is essential for the diagnosis of malaria, differentiation of parasite species, and estimation of parasite density performed for assessments of antimalarial drug efficacy. The accuracy and comparability of these measures over time and space are vital to discern the emergence or spread of antimalarial drug resistance. Although evidence-based guidelines for malaria microscopy methods exist, the age-old microscopy techniques for parasitological assessments are subject to considerable methodological variations.

Tafenoquine: a toxicity overview

December 16, 2020 - 10:21 -- Open Access
Chu CS, Hwang J
Expert Opin Drug Saf. 2020 Dec 11

A century long history in 8-aminoquinolines, the only anti-malaria drug class preventing malaria relapse, has resulted in the approval of tafenoquine by the U.S. Food and Drug Administration (FDA) and the Australian Therapeutic Goods Administration (TGA) and to date registration in Brazil and Thailand. Tafenoquine is an alternative anti-relapse treatment for vivax malaria and malaria prophylaxis. It should not be given in pregnancy, during lactation of infants with glucose-6-phosphate dehydrogenase (G6PD) unknown or deficient status, and in those with G6PD deficiency or psychiatric illness.

NOT Open Access | Could Artesunate Have a Positive Effect on the Neurological Complications Related to Infection When It Is Used in the Treatment of COVID-19

December 8, 2020 - 10:42 -- NOT Open Access
Uzun T, Toptaş O, Aydın Türkoğlu Ş
ACS Chem Neurosci. 2020 Dec 3

Artesunate is a safe noncytotoxic drug with low side effects which is used in the treatment of chloroquine-resistant malaria. In addition to being an antimalarial drug, artesunate also has immunomodulatory, anticarcinogenic, and antiviral activity. There are in vivo and in vitro studies reporting that artesunate may have a positive effect on the treatment of COVID-19.

Assessment of antimalarial drug resistant markers in asymptomatic Plasmodium falciparum infections after 4 years of indoor residual spraying in Northern Ghana

December 8, 2020 - 10:05 -- Open Access
Myers-Hansen JL, Abuaku B, Oyebola MK, Mensah BA, Ahorlu C, Wilson MD, Awandare G, Koram KA, Ngwa AA, Ghansah A
PLoS One. 2020 Dec 7;15(12):e0233478

Drug resistance remains a concern for malaria control and elimination. The effect of interventions on its prevalence needs to be monitored to pre-empt further selection. We assessed the prevalence of Plasmodium falciparum gene mutations associated with resistance to the antimalarial drugs: sulfadoxine-pyrimethamine (SP), chloroquine (CQ) and artemisinin combination therapy (ACTs) after the scale-up of a vector control activity that reduced transmission.


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