Drug Database
AR

artesunate (artesunate, Amivas)

✓ Approved

Amivas · Small Molecule · Small Molecule

What is artesunate?

artesunate is a small molecule developed by Amivas. It is approved for therapeutic indications via injectable (others) or intravenous (iv).

Drug Profile

Brand Namesartesunate, Amivas
CompanyAmivas
Drug ClassSmall Molecule
RouteInjectable (Others), Intravenous (IV)
StatusApproved
Sources: ClinicalTrials.gov, Amivas

Therapeutic Indications

artesunate is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Infections and infestationsPlasmodium malariae infection✓ Approved
Infections and infestationsCytomegalovirus infectionPreclinical

Related Research Articles

PubMedMalaria journal2026-08-25

The effect of mefloquine dose on outcome of uncomplicated falciparum malaria treated with artesunate-mefloquine: a WWARN systematic review and individual patient data meta-analysis.

WWARN AS-MQ Dose Impact Study Group

A combination of mefloquine associated with artesunate (AS-MQ) was the first artemisinin-based combination therapy (ACT) to be used widely for acute uncomplicated P. falciparum malaria. Individual patient data from 31 studies of patients with uncomplicated falciparum malaria treated with various AS-MQ regimens (target mefloquine dose 25 mg/kg), conducted in Asia, Africa and South America, were pooled and analysed to investigate the effects of MQ mg/kg dosing on malaria recurrence and other clinical, parasitological and tolerability endpoints. A total of 6,761 patients were enrolled in clinical studies conducted between 1995 and 2018; the majority (74%) were from Asia. The median age of study participants was 18 years (interquartile range IQR 8-30 years), of whom 13.5% (915/6761) were aged less than 5 years old. Participants received an estimated median [range] total mg/kg dose of mefloquine and artesunate of 25 [6.8-60] and 12 [3.6-33.3] respectively, and 1,572 (23.4%) participants were treated with the coformulation. The PCR-corrected recrudescence rate 42 days after any ASMQ treatment was 2.4% for patients enrolled in Asia and 2.5% in Africa, before artemisinin resistance emerged. Corresponding rates in children aged 1 to < 5 years were 2.9% and 3.3%. After adjusting for background artemisinin resistance, the hazard of recrudescence was higher in children aged 1 to < 5 years than in adults in Asia, but not in Africa (Asia, HR 3.01, 95%CI 1.60-5.64, p < 0.001; Africa HR 5.18, 95% CI 0.61-44.28, p = 0.133). There was only one recrudescent infection in South America. A significant MQ dose-effect was observed in Asia in patients treated with 3-dose regimens (AHR 0.89, 95% CI 0.83-0.96, p = 0.003 for 1 mg/kg increase in dose). Vomiting rates within an hour of dosing were highest in children 1- 5 years of age (n = 140) at 3.4% doses (13/378) compared to 1.7% (20/1,168) in children 5-11 years (n = 476), and 1.1% (47/4,191) in patients 12 years of age or older (n = 2027) (p < 0.001, test for trend). AS-MQ administered over three days is a highly efficacious ACT in low to moderate transmission areas without artemisinin resistance. While further optimisation of the mefloquine dose in the coformulation in children aged 1-5 years could be considered, dose-related early vomiting is highest in this age group and may preclude this.

PMID 42638106
Read full article →
PubMedMini reviews in medicinal chemistry2026-08-24

Neuroprotective Potential of Terpenoids: A Promising Avenue in Neurology.

Gairola Nidhi N, Uniyal Sushmita S, Martolia Jaya J, Gogoi Himanko H et al.

Neurodegenerative diseases are progressive disorders characterised by the deterioration of neuronal structure and function, ultimately leading to cognitive deficits and functional impairment. Due to neuroinflammation, oxidative stress, and mitochondrial dysfunction, neurones, which cannot regenerate themselves, are highly susceptible to degeneration. There are many possible side effects associated with traditional pharmacotherapies, although they often offer symptomatic relief, highlighting the need for safer and more effective therapeutics. Natural products such as terpenoids, a structurally diverse class of isoprenoid compounds, have shown promising neuroprotective effects. Classes of terpenoids exhibit anti-inflammatory, antioxidant, anti-apoptotic, and mitochondrialprotective effects by regulating crucial signalling cascades, including Nuclear Factor kappa B (NF- κB), Mitogen-activated protein kinase (MAPK), c-Jun N-terminal Kinase (JNK), Phosphoinositide 3-kinase/Protein kinase B (PI3K/Akt), and Nuclear factor erythroid 2-related factor 2 (Nrf2)/Heme oxygenase-1 (HO-1). Across preclinical models, representative compounds like catalpol, geniposide, artesunate, ginkgolides, alisol A 24-acetate, echinocystic acid, lycopene, and astaxanthin have demonstrated efficacy against Parkinson's disease, Alzheimer's disease, stroke, ischaemia, and haemorrhage by preserving neuronal integrity and function. Despite these promising findings, challenges such as poor bioavailability, limited blood-brain barrier penetration, metabolic instability, and a lack of standardised human safety data limit translational progress. Structural optimisation and advanced delivery systems, such as nanoparticles, cyclodextrin inclusion, combined therapeutic strategies, precision-targeted interventions, and rigorous clinical trials, may be considered future directions. In short, terpenoids have the potential to be developed as novel multitarget neurotherapeutic agents with further research to bridge preclinical promise and clinical validation.

PMID 42634530
Read full article →
PubMedJournal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy2026-08-24

Severe Plasmodium falciparum Malaria with Marked ADAMTS13 Reduction and Secondary Microangiopathic Features: A Case Report.

Huang Ming M, Jia Xishuai X, Wang Xiaomei X, Hu Lin L et al.

To report a case of severe Plasmodium falciparum malaria with marked ADAMTS13 reduction and secondary microangiopathic manifestations resembling TTP, highlighting the diagnostic challenge of distinguishing malaria-associated microangiopathic changes from primary TTP-spectrum disorders. The patient's clinical features, laboratory data, peripheral blood smear findings, ADAMTS13 activity, treatment, outcomes,and relevant literature were retrospectively analyzed. A 46-year-old man returning from Nigeria presented with severe P. falciparum malaria after 11 days of intermittent fever and fatigue, followed by jaundice and dark urine. Laboratory testing showed severe anemia, thrombocytopenia, hyperbilirubinemia, acute kidney injury, and elevated lactate dehydrogenase. Peripheral blood smear revealed intraerythrocytic P. falciparum with high parasitemia (approximately 17%) and a low proportion of schistocytes (approximately 1%).The patient subsequently developed impaired consciousness and multi-organ dysfunction. ADAMTS13 activity was 7.6%. Given the coexistence of thrombocytopenia, microangiopathic hemolysis, neurological impairment, renal dysfunction, and marked ADAMTS13 reduction, a TMA phenotype raising concern for TTP-spectrum disease was suspected. However, because severe falciparum malaria itself can cause endothelial injury, secondary TMA, and reduced ADAMTS13 activity, immune-mediated TTP could not be confirmed. After combined treatment with intravenous artesunate, therapeutic plasma exchange, continuous renal replacement therapy, and intensive supportive care, the patient showed improvement in platelet count, hemolysis markers, renal function, and neurologic status, with ADAMTS13 activity increasing to 42%. Severe falciparum malaria may be accompanied by marked ADAMTS13 reduction and secondary microangiopathic features resembling TTP-spectrum manifestations. Early recognition of microangiopathic features and evaluation of ADAMTS13 activity when available may support timely diagnostic evaluation and individualized management in selected patients.

PMID 42636958
Read full article →
PubMedCell and tissue banking2026-08-20

The evaluation of biological effects of artesunate on ovarian cancer using three-dimensional cell culture methods.

Yuan Yijun Y, Luo Xiaojing X, Tang Longyu L, He Tianwen T et al.

Ovarian cancer (OC) is one of the most aggressive malignancies, with high mortality rates largely attributed to late-stage diagnosis, tumor heterogeneity, recurrence, and resistance to chemotherapy. Artesunate (ART), a water-soluble derivative traditionally used to treat malaria, has recently gained attention as a promising anticancer agent. Recently, studies have shown that ART can inhibit the migration and invasion of cancer cells. However, theses studies are always based on conventional two-dimensional (2D) culture models, which neglect the complex interactions between cells and the extracellular matrix (ECM) or in vivo microenvironment. To address these challenges, in this study, honeycomb-like gelatin methacryloyl (GelMA) hydrogel microspheres as a three-dimensional (3D) culture platform were introduced to mimic the native ECM microenvironment and assess the effects of ART on ovarian cancer cells. The results showed that these GelMA microspheres exhibited a uniform and highly porous structure, which supported cell adhesion, proliferation, and migration. Notably, 3D culture promoted DNA synthesis and induced G1-to-S phase transition, indicating enhanced proliferative capacity. Furthermore, ovarian cancer cells cultured in 3D exhibited stronger invasive and chemoresistant phenotypes. RNA sequencing revealed that after ART treatment, tumor-related proliferation and invasion genes of ovarian cancer cells were significantly up-regulated under 3D culture compared with 2D culture. This might be related to the up-regulation of TNF signaling pathway, NF-kappa B signaling pathway, and Pl3K-Akt signaling pathway. Correspondly, epithelial-mesenchymal transition (EMT) of ovarian cancer cells was markedly enhanced when cultured on GelMA hydrogel microspheres after ART treatment. These effects might be attributed to the altered microenvironment provided by the GelMA hydrogel microspheres, which could be responsible for the enhanced resistance of ovarian cancer cells to ART. These findings suggest that, compared to traditional 2D. These findings suggest that, compared to traditional 2D culture, the 3D extracellular matrix-based system better mimics the in vivo tumor architecture, thereby improving the sensitivity of anticancer drug screening and offering a more reliable platform for evaluating drug resistance and tumor cell heterogeneity.

PMID 42622742
Read full article →
PubMedJournal of visualized experiments : JoVE2026-08-18

Computational Protocol To Quantify Artesunate-Associated Transcriptomic Shifts In Experimental Cerebral Malaria Brain Tissue Using DESeq2.

George Oche Ambrose OA, Igunnu Adedoyin A, Adebayo Joshua Oluwatope JO

RNA sequencing (RNA-seq) is widely used to define disease-associated transcriptional programs, but consistent, end-to-end workflows are required to ensure reproducible comparisons across experimental groups and to facilitate biologically interpretable outputs. Here, a complete RNA-seq analysis protocol is presented for evaluating brain transcriptomic changes in experimental cerebral malaria (ECM) and following artesunate treatment using the public dataset GSE162535. The workflow analyzes three groups-control brain (CB), ECM brain (MB), and artesunate-treated ECM brain (AB)-starting from an HTSeq-count matrix. After importing and formatting raw counts, the protocol constructs a DESeq2 dataset with CB as the reference level, filters low-count genes, and performs quality control using library-size visualization, principal component analysis, and sample distance clustering. Differential expression is then calculated for three primary contrasts (MB vs CB, AB vs MB, AB vs CB), with log2 fold-change shrinkage applied for stable effect-size estimation. The protocol exports full and significant differential-expression tables, generates volcano plots and MA plots, and produces heatmaps of the most variable genes and top-ranked differentially expressed genes per contrast. To support mechanistic interpretation, the workflow includes targeted immune marker extraction (e.g., cytokines, chemokines, microglial activation markers, BBB/endothelial genes) and conducts Gene Ontology and KEGG enrichment analyses for significantly up- and downregulated gene sets. This protocol provides a reproducible template for characterizing ECM-associated neuroinflammatory transcriptional programs and for quantifying artesunate-associated modulation of these signatures.

PMID 42612112
Read full article →
PubMedACS omega2026-08-14

Synthesis and Biological Evaluation of Thiophene-Bridged Indole-Artesunate Hybrids as Selective Anticancer Agents.

Kavak Emrah E, Çetin Doğan D, Konuş Metin M, Kivrak Arif A

In this study, five thiophene-bridged indole-artesunate hybrid molecules were synthesized and evaluated as anticancer candidates. Antioxidant screening by DPPH, ABTS, galvinoxyl, and FRAP methods showed no measurable radical scavenging or reducing activity, indicating that these compounds should not be described as antioxidants. Cytotoxic effects were evaluated in Ishikawa, HepG2, HT-29, MDA-MB-231, and Panc-1 cancer cell lines using the MTT assay, and compounds (3R,5aS,6R,8aS,9R,12R,12aR)-3,6,9-trimethyldecahydro-12H-3,12-epoxy-[1,2]-dioxepino-[4,3-i]-isochromen-10-yl 4-(5-(1-methyl-2-phenyl-1H-indol-3-yl)-thiophen-2-yl)-4-oxobutanoate (D1), synthesis of (3R,5aS,6R,8aS,9R,12R,12aR)-3,6,9-trimethyldecahydro-12H-3,12-epoxy-[1,2]-dioxepino-[4,3-i] isochromen-10-yl 4-(5-(1-methyl-2-pentyl-1H-indol-3-yl)-thiophen-2-yl)-4-oxobutanoate (D2), and synthesis of (3R,5aS,6R,8aS,9R,12R,12aR)-3,6,9-trimethyldecahydro-12H-3,12-epoxy-[1,2]-dioxepino-[4,3-i]-isochromen-10-yl 4-(5-(1-methyl-2-(p-tolyl)-1H-indol-3-yl)-thiophen-2-yl)-4-oxobutanoate (D3) were found to exhibit significant cytotoxic activity. Compound D1 (EC50: 20.22 μM) showed activity similar to paclitaxel (EC50: 19.3 μM) in Ishikawa cells, while compounds D1 and D2 (EC50: 5.43 μM, EC50: 5.63 μM) showed comparable activity to the positive control (EC50: 4.5 μM) in HepG2 cells; compound D3 (EC50: 2.75 μM) showed a higher cytotoxic effect. No measurable cytotoxicity was observed in the healthy human endothelial (HUVEC) cell line for any of the tested compounds. Invasion assay showed that compounds D1 and D2 strongly inhibited cell invasion, particularly in HepG2 and Panc-1 cell lines. Annexin V/PI assays and real-time PCR results showed that the compounds induced apoptosis, increasing the expression of BAX, P53, and caspase genes while suppressing Bcl-2 expression. Overall, the findings indicate that although the compounds studied in this work do not possess antioxidant properties, they exhibit selective cytotoxic, anti-invasive, and proapoptotic effects, warranting further investigation as potential anticancer agent candidates.

PMID 42598472
Read full article →

+4186 more articles available with a free account

Sign up free to view all articles →

Ask about artesunate