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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).

A Case of Plasmodium falciparum Malaria Treated with Artesunate in a 55-Year-Old Woman on Return to Florida from a Visit to Ghana

December 23, 2020 - 09:51 -- Open Access
Rodriguez JA, Roa AA, Leonso-Bravo AA, Khatiwada P, Eckardt P, Lemos-Ramirez
Am J Case Rep. 2020 Dec 20;21:e926097

Malaria is the infection caused by inoculation with the mostly obligate intraerythrocytic protozoa of the genus Plasmodium. Severe malaria manifests as multiple organ dysfunction with high parasitemia counts characterized by coma, stupor, and severe metabolic acidosis. Physicians in the United States do not frequently encounter patients with malaria, and the drugs are only available through the Centers for Disease Control and Prevention, which makes the management of this disease somewhat complicated. In 2019, the marketing of quinine for malaria was discontinued. In May 2020, the US Food and Drug Administration approved the use of intravenous artesunate for the treatment of adults and children with severe malaria.

NOT Open Access | Delayed haemolysis following artesunate in a child with profound anaemia and Coca-Cola-coloured urine

December 23, 2020 - 08:27 -- NOT Open Access
Patel N, Thomson J, Re Ferre L
BMJ Case Rep. 2020 Dec 17;13(12):e238361

An 8-year-old girl of African descent presented to the hospital with a headache, lethargy, pallor and 'Coca-Cola'-coloured urine. She had been admitted 11 days before with Plasmodium falciparum malaria, which was successfully treated with 48 hours of parenteral artesunate. Investigations revealed signs of severe haemolytic anaemia, with a haemoglobin level of 52 g/L that reached a nadir of 10 g/L within 4 hours, in addition to haemoglobinuria, hyperbilirubinaemia and raised lactate dehydrogenase levels.

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.

Artesunate inhibits epithelial-mesenchymal transition in non-small-cell lung cancer (NSCLC) cells by down-regulating the expression of BTBD7

December 2, 2020 - 08:03 -- Open Access
Wang JS, Wang MJ, Lu X, Zhang J, Liu QX, Zhou D, Dai JG, Zheng H
Bioengineered. 2020 Dec;11(1):1197-1207

In recent years, more and more studies have shown that antiparasitic drugs can affect a variety of biological processes of tumor cells and exhibit a potential anti-tumor activity. Although artesunate (ART), a strong bioactive derivative of artemisinin and widely used clinically against malaria, was found to have an inhibitory effect on tumor cells, it is still unclear whether ART could regulate the tumor malignancy of non-small-cell lung cancer (NSCLC) cells.

NOT Open Access | Artemisinin-type drugs for the treatment of hematological malignancies

November 4, 2020 - 15:11 -- NOT Open Access
Mancuso RI, Foglio MA, Olalla Saad ST
Cancer Chemother Pharmacol. 2020 Nov 3

Qinghaosu, known as artemisinin (ARS), has been for over two millennia, one of the most common herbs prescribed in traditional Chinese medicine (TCM). ARS was developed as an antimalarial drug and currently belongs to the established standard treatments of malaria as a combination therapy worldwide. In addition to the antimalarial bioactivity of ARS, anticancer activities have been shown both in vitro and in vivo.

Health systems readiness and quality of inpatient malaria case-management in Kano State, Nigeria

November 4, 2020 - 09:55 -- Open Access
Abiodun A. Ojo, Kolawole Maxwell, Dejan Zurovac, et al.
Malaria Journal 2020 19:384, 30 October 2020

Nigeria was among the first African countries to adopt and implement change of treatment policy for severe malaria from quinine to artesunate. Seven years after the policy change health systems readiness and quality of inpatient malaria case-management practices were evaluated in Kano State of Nigeria.

NOT Open Access | The preclinical discovery and development of rectal artesunate for the treatment of malaria in young children; review of evidence

September 15, 2020 - 14:35 -- NOT Open Access
de Carvalho LP, Kreidenweiss A, Held J
Expert Opin Drug Discov. 2020 Sep 14:1-10

Plasmodium falciparum, the deadliest malaria parasite, kills hundreds of thousands of people per year, mainly young children in Sub-Saharan Africa. Artesunate suppositories are recommended as pre-referral malaria treatment in remote endemic areas for severely ill children to prevent progression of the disease and to provide extra time for patients until the definitive severe malaria treatment can be administered.

NOT Open Access | The anti-malaria agent artesunate exhibits cytotoxic effects in primary effusion lymphoma

September 12, 2020 - 15:04 -- NOT Open Access
Ishikawa C, Mori N
Invest New Drugs. 2020 Sep 3

Primary effusion lymphoma (PEL), caused by Kaposi's sarcoma-associated herpesvirus (KSHV), presents as a lymphomatous effusion in body cavities and has a poor prognosis. The anti-malaria drug, artesunate, possesses anti-neoplastic potential. Therefore, we aimed to investigate its effect on KSHV-infected PEL cell lines. Artesunate inhibited cell growth and viability of PEL cells, but its effect on peripheral blood mononuclear cells was less pronounced.

NOT Open Access | Retinal involvement in severe noncerebral malaria

August 25, 2020 - 08:21 -- NOT Open Access
Lando L, Borooah S, Maude RJ
Can J Ophthalmol. 2020 Aug 20:S0008-4182(20)30675-X

A 20-year-old male patient complained of reduced vision after being admitted to a hospital in Bangladesh with 5 days of fever associated with convulsions and anemia (hematocrit 11%). Uncorrected visual acuity was 20/80 OD and 20/64 OS.


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