artemether / Generic mfg. - LARVOL DELTA

Formulation development and optimization of artemether-lumefantrine self-nanoemulsifying drug delivery systems. (PubMed, Pharmazie) - "Compatibility studies revealed no prominent or significant incompatibilities between the drugs and selected excipients. The optimized formulation was stable as dispersions with nano-sized droplets and a loading capacity >99 % for both ART and LMF and a release >95% within 15 min for both drugs, reflecting a significant increase in the rate and extent of dissolution compared to that of the pure drug."

Journal

A comprehensive review of artesunate-induced organ toxicity: mechanisms, resistance, biomarkers, and protective strategies. (PubMed, Drug Chem Toxicol) - "Overall, this paper underscores the need for more comprehensive research, including well-designed clinical trials, to better understand and manage the potential toxic effects of ART. Strengthening this knowledge is essential to ensure that the risk of organ damage does not compromise the life-saving benefits of malaria treatment."

Biomarker • Journal • Review • Infectious Disease • Inflammation • Malaria

Polycyclitol Derivatives Restore Long- Term Memory Via cdk5/p25 Activation of Tau Signaling in Experimental Cerebral Malaria. (PubMed, Neurochem Res) - "In this study, we employed an experimental cerebral malaria model to assess the therapeutic potential of four polycyclic derivatives, SR4-01 to SR4-04, as adjuncts to artemether...Western blot analysis confirmed reduced Cdk5-p25-mediated tau phosphorylation in the SR4-04 treated group. Collectively, our findings suggest that SR4-02 and SR4-04 hold promise as adjunctive therapies for reducing tau pathology and restoring cognitive function in cerebral malaria-associated neurodegeneration."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Infectious Disease • Malaria • CA3 • IL1B

Multi-target regulation by artemether in MAFLD through EGFR/HSP90 pathways. (PubMed, J Adv Res) - "These findings identify EGFR as a key target of Art, modulated directly or via HSP90, thereby offering new insights into Art's multi-target therapeutic mechanism in MAFLD."

Journal • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • CDC37 • EGFR • HSP90AA1

Antimalarial Drug Repurposing of Epirubicin and Pelitinib in Combination with Artemether and Lumefantrine. (PubMed, Pharmaceuticals (Basel)) - "Most combinations of PEL with ART and LU showed antagonism (FIC50 > 1) when tested against strains of P. falciparum and clinical isolates. This study underscores the utility of alternative drug discovery and development strategies to bypass cost, time, and safety barriers, thereby enriching the antimalarial drug pipeline and accelerating the transition from lab to market."

Journal • Infectious Disease • Malaria

Artemisinin derivatives maintain fibroblast normalization by acting on tumor-stroma interactions in oral tongue squamous cell carcinoma. (PubMed, Am J Cancer Res) - "Dihydroartemisinin (DHA) and artemether (ARM), semisynthetic derivatives of the natural compound artemisinin, have exhibited anticancer effects in various tumors...These findings were confirmed in xenograft models. Our study showed that artemisinin derivatives prevent the progression of oral tongue squamous cell carcinoma (OTSCC) by inhibiting the production of PDGF-BB in cancer cells to maintain the normal state of fibroblasts, thus providing a potential avenue for targeted OTSCC treatment."

Journal • Oncology • Oral Cancer • Squamous Cell Carcinoma • Tongue Carcinoma • CAFs

ER Stress Induced by Artemisinin and Its Derivatives Determines the Susceptibility to Their Synergistic Apoptotic Killing With TRAIL. (PubMed, Cancer Med) - "We concluded that dihydroartemisinin is the most effective contender among all the derivatives tested to enhance TRAIL-induced apoptosis."

Journal • Colon Cancer • Colorectal Cancer • Infectious Disease • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor

Therapeutic effectiveness and safety of artemether lumefantrine for the treatment of uncomplicated Plasmodium falciparum malaria in children aged 5 to 15 years in three epidemiological strata of malaria in Niger (PubMed, Ann Biol Clin (Paris)) - "No major adverse events were recorded. The results support the use of AL for the treatment of uncomplicated malaria as per the National Malaria Control Program (NMCP)."

Journal • Infectious Disease • Malaria

Slurry Conversion: A General Method for Formulating Amorphous Solid Dispersions and Fully Integrating Drug and Polymer Components. (PubMed, Mol Pharm) - "While clearing did not occur for some drugs (e.g., clofazimine), the product was still fully amorphous, through solvent-mediated conversion...In addition to binary ASDs, ternary ASDs containing two drugs (LMF and artemether or LMF and artesunate) were successfully prepared to support applications in combination therapies...We find that slurry conversion can be scaled up 60-fold from the typical batch size without any difficulties or adverse effect on the structure and properties of the product. Overall, our results demonstrate that slurry conversion is a general, low-cost, and green alternative to conventional methods for manufacturing ASDs where the components are fully integrated."

Journal • Infectious Disease

Autochthonous cases of malaria in central Anatolia. (PubMed, Trop Doct) - "Artemether (20 mg)-lumefantrin were given to all patients...The second case improved, but the third case developed organ failure and died. Malaria should be considered in the preliminary clinical diagnosis of patients even when no history of endemic region residence can be verified."

Journal • Infectious Disease • Malaria

Artemether Improves Aβ1-42-Induced Mitochondrial Dysfunction and Protects Against Blood-Brain Barrier Damage Through Activating the CAMKK2/AMPK/PGC1α Signaling Pathway. (PubMed, Mol Neurobiol) - "In the AD mice model, we found that artemether treatment increased the expression level of ZO-1, CLDN-5, and OCLN of the AD mice model. Collectively, these findings demonstrate that artemether exerts neuroprotection against Aβ1-42-induced injury in brain microvascular endothelial cells through activation of the CAMKK2/AMPK/PGC1α signaling axis, which supports the protective effect of artemether in the prevention and treatment of AD through improving cerebrovascular dysfunction."

Journal • Alzheimer's Disease • CNS Disorders • Dementia • Infectious Disease • Metabolic Disorders • CAMKK2 • OCLN • TJP1

Artemether ameliorates DSS-induced ulcerative colitis by modulating macrophage polarization. (PubMed, Int Immunopharmacol) - "These effects may be mediated by regulating Notch signaling activation and suppressing pro-inflammatory M1 macrophages. This discovery provides new potential therapeutic strategies for colitis."

Journal • Atherosclerosis • Cardiovascular • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Arthritis • Inflammatory Bowel Disease • Lupus • Systemic Lupus Erythematosus • Ulcerative Colitis • IL1B • IL6 • OCLN • TJP1

Three Asparagine insertions in the K13-propeller led to Plasmodiumfalciparum becoming resistant to multiple antimalarial drugs. (PubMed, Int J Parasitol Drugs Drug Resist) - "However, the insertion of three asparagine residues resulted in significantly higher IC50 values compared to the first two forms when tested with Artesunate, Artemether, Dihydroartemisinin, Pyronaridine Phosphate, and Naphthoquine, showing resistance to all five drugs...Additionally, 3N-3D7 exhibited a fitness defect, with the proportion decreasing gradually during co-culture with 3D7, its fitness cost calculated as 14.88 ± 2.87. All these results support the opinion that the insertion of three asparagines was a molecular marker of resistance to artemisinin derivatives, Pyronaridine Phosphate, and Naphthoquine in P. falciparum."

Journal • CNS Disorders • Infectious Disease • Malaria • Psychiatry • Schizophrenia

Artesunate alleviates cerebral ischemia/reperfusion injury by suppressing FUNDC1-mediated excessive mitophagy. (PubMed, Brain Res Bull) - "Mechanically, artesunate regulated FUN14 domain containing 1 (FUNDC1)-mediated mitophagy via the AMPK (AMP-activated protein kinase)-mTOR (mechanistic target of rapamycin)-TFEB (transcription factor EB) signaling pathway. Additionally, artemether reduced the infarct size in MCAO rats, inhibited neurological dysfunction, and enhanced memory performance. In summary, our data revealed a novel mechanism whereby artesunate suppresses apoptosis by inhibiting excessive mitophagy. These findings offered a new promising therapy for cerebral I/R injury."

Journal • Cardiovascular • CNS Disorders • Reperfusion Injury • AMPK • mTOR • TFEB

Artemisinin derivatives differently affect cell death of lung cancer subtypes by regulating GPX4 in patient-derived tissue cultures. (PubMed, Cell Death Discov) - "To overcome resistance mechanisms artemisinin derivatives, known for its complementary use during cancer treatement and ferroptosis induction, were investigated both as single agents and in combination with cisplatin (3 µM) in a complex organotypic tissue model of non-small cell lung cancer (NSCLC) patient samples. All substances-artemisinin (ART, 100 µM), artemether (ATM, 50 µM), artesunate (ATS, 20 µM), and dihydroartemisinin (DHA, 10 µM)-showed beneficial effects in most of the investigated patient-derived tissue cultures (PDTC)...The enzyme GPX4, inhibiting ferroptosis was up-regulated in LUAD but not in LUSC. Taken together, in the complex PDTC model system, LUSC displayed a higher sensitivity to ART derivatives, due to the lack of GPX4-mediated resistance to ferroptosis."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • GPX4

SEVERE AND NON-SEVERE MALARIA: DIAGNOSTIC AND TREATMENT CHALLENGES IN ATHENS PEDIATRIC HOSPITAL (ESPID 2025) - "The third patient didn't meet the criteria for severe malaria and received only per os artemether and 3 rd generation cephalosporin...Learning Points/Discussion Due to recent migration waves, incidence of malaria in greek settings has rised. Complementary training of clinicians and laboratory scientists as well as multidisciplinary coordinated approach is necessary for the early and efficient diagnosis and treatment of malaria patients, especially those who present with severe malaria"

Clinical • Infectious Disease • Malaria • Novel Coronavirus Disease

Exploring the mechanisms of artemisinin and its derivatives in the treatment of atopic dermatitis based on network pharmacology and molecular docking: A review. (PubMed, Medicine (Baltimore)) - "ARS and its derivatives have the potential to treat AD. Artemisinin, artesunate, dihydroartemisinin, artemether, artemisinin and artemisinone could potentially treat AD by targeting MAPK14 and MAPK10."

Journal • Review • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • Oncology • IL17A • MAPK10 • MAPK14 • MAPK4

Artemisinin and Its Derivatives: Promising Therapeutic Agents for Age-Related Macular Degeneration. (PubMed, Pharmaceuticals (Basel)) - "However, no comprehensive review has systematically summarized the specific roles of ART and its derivatives in AMD pathogenesis and treatment. This paper aims to fill the knowledge gap by synthesizing the therapeutic efficacy and molecular mechanisms of ART and its derivatives in AMD, thereby providing a foundation for future investigations."

Journal • Review • Age-related Macular Degeneration • Fibrosis • Immunology • Infectious Disease • Macular Degeneration • Metabolic Disorders • Ophthalmology • Retinal Disorders • Wet Age-related Macular Degeneration

DIORS: Enhancing drug-target interaction prediction via structure and signature integrated-driven approach and discovering potential targeted molecules. (PubMed, Pharmacol Res) - "In Piezo1-targeted molecule prediction, among the top ten predicted molecules by DIORS, four of them, namely gefitinib, rifaximin, bosutinib and vandetanib, exhibited binding affinities. In the prediction of TLR4/MD2-targeted anti-inflammatory molecules, among the top ten predicted molecules, three of them, namely enoxolone, dabrafenib and ponatinib, exhibit both high binding affinities and anti-inflammatory activities. The results demonstrated that DIORS can serve as a better approach with high performance to predict and find new targeted drugs by combining structural and signature information."

Journal • TLR4

Cambodian Plasmodium vivax parasites with reduced hemoglobin digestion display delayed clearance upon artesunate treatment. (PubMed, medRxiv) - "Evidence before this study: The WHO treatment guidelines recommend artemisinin-combination therapy (ACT) for treatment of blood-stage infections caused by Plasmodium vivax in all areas (with chloroquine recommended only in areas where P. vivax are still chloroquine-sensitive)...We searched Pubmed for studies containing the terms "vivax" AND "clearance" AND ("artesunate" OR "dihydroartemisinin" OR "artemether" OR "artemisinin") published between 1990 and February 2025, with no language restrictions...While all these studies concluded that artemisinin derivatives provided rapid clearance of P. vivax parasites, two studies reported a low frequency of day 3 positivity following artesunate-amodiaquine treatment (2.6% in Brazil) or dihydroartemisinin-piperaquine (0.6% in Indonesia)...Gene expression analyses suggest that metabolic variations may underlie slow clearance. Increased monitoring of treatment efficacy and..."

Journal • Infectious Disease • Malaria

Artemether exerts neuroprotective effect in Parkinson's disease through the PI3K/Akt/GSK-3β signaling pathway. (PubMed, Eur J Pharmacol) - "Artemether exerted neuroprotective effects in Parkinson 's disease models in vitro and in vivo induced by 6-OHDA through the PI3K/Akt/GSK-3β signaling pathway."

IO biomarker • Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Dementia • Infectious Disease • Malaria • Movement Disorders • Parkinson's Disease • BCL2

Computational Analysis of Plasmodium falciparum DNA Damage Inducible Protein 1 (PfDdi1): Insights into Binding of Artemisinin and its Derivatives and Implications for Antimalarial Drug Design. (PubMed, Cell Biochem Biophys) - "Our study included clinically relevant ART derivatives such as artemether (ARM), arteether (AET), artemiside (AMD), and artesunate (ATS)...Importantly, three key binding regions-Loop 1 (GLN 266 - ILE 269), Loop 2 (ILE 323 - TYR 326), and Loop 3 (ALA 292 - GLY 294)-were identified as potential targets for new antimalarial drugs against PfDdi1. This study highlights the potential of ART derivatives as PfDdi1 inhibitors, paving the way for further experimental validation."

Journal • Infectious Disease • Malaria • Targeted Protein Degradation

Unlocking the Therapeutic Benefits of Artemisia Annua: A Comprehensive Overview of its Medicinal Properties. (PubMed, J Pharm Bioallied Sci) - "At the moment, Artemisia annua is the sources of artemisinin and semisynthetic artemisinin derivatives (including dihydroartemisinin, artesunate, artemether, and arteether) used in the development of malaria combination treatments (ACTs = Artemisinin-based combination therapy)...Experiences with malaria treatment indicate that artemisinin-based medicines are generally well-tolerated. This study highlights A. annua's traditional use and contemporary pharmacological research, bringing unique insights into the usage of A. annua in the treating a wide range of ailments."

Journal • Review • Infectious Disease • Malaria • Oncology

Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment. (PubMed, BMC Chem) - "The optimized formulation was stable and nanomeric (size 292.90 ± 5.01 nm, polydispersity index 0.191 ± 0.09, and zeta-potential + 32.50 ± 1.58 mV) with good encapsulation efficiency (82.03%), demonstrated minimal toxicity on Caco-2 cells, exhibited controlled drug release compared with fast release of artemether suspension and gave significantly (p < 0.05) greater antimalarial activity than artemether suspension. Artemether-loaded chitosan-coated SRMS-based SLNs improved the antimalarial activity of the drug and can be pursued as a novel alternative for improved oral malaria treatment."

Journal • Infectious Disease • Malaria

Exploring the glucose-lowering and anti-inflammatory immune mechanism of artemether by AMPK/mTOR pathway and microbiome based on multi-omics. (PubMed, Front Pharmacol) - "C57BL/KsJ-db/db mice were treated with 80 and 160 mg/kg of ATM for 8 weeks, with metformin as a positive control. The elevation of SCFAs, especially propionic acid, may activate the AMPK/mTOR pathway, leading to a decrease in the levels of TNF-α, IL-1β, IL-6, NF-κB, and IL-17A, while increasing the levels of IL-10, thereby alleviating the inflammatory state and improving glucolipid metabolic disorder in T2DM. These findings laid a theoretical foundation for the clinical application of ATM in T2DM."

Journal • Diabetes • Hepatology • Inflammation • Inflammatory Bowel Disease • Liver Failure • Metabolic Disorders • Type 2 Diabetes Mellitus • IL10 • IL17A • IL1B • IL6 • OCLN • TLR4 • TNFA