artemether / Generic mfg. - LARVOL DELTA

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

Hemozoin: a waste product after heme detoxification? (PubMed, Parasit Vectors) - "Hemozoin is not a waste byproduct of heme detoxification but instead plays a crucial role in the parasite's life cycle."

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

A Comprehensive Review on the Antimicrobial Activity of the Genus Artemisia, Artemisinin, and its Derivatives. (PubMed, Curr Top Med Chem) - "Other derivatives, such as artesunate, artemether, and arteether, have also shown antimicrobial activity that can be administered orally, rectally, intramuscularly, or intravenously...However, further translational and experimental research is required for optimization and the establishment of pharmacokinetic profiles. In addition, health authorities are also required to regulate the present Artemisinins and newly discovered derivatives to ensure their long-term effectiveness in the worldwide fight against antibiotic resistance."

Journal • Epstein-Barr Virus Infections • Infectious Disease • Malaria • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Artemether relieves liver fibrosis by triggering ferroptosis in hepatic stellate cells via DHHC12-mediated S-palmitoylation of the BECN1 protein. (PubMed, Free Radic Biol Med) - "ART alleviates liver fibrosis by inducing HSC ferroptosis via DHHC12-mediated BECN1 protein S-palmitoylation."

Journal • Fibrosis • Hepatology • Immunology • Liver Cirrhosis • BECN1 • TGFB1

Extended Treatment Duration of Artemether-Lumefantrine in Ugandan Children with HIV on Efavirenz-Based Antiretroviral Therapy: A Randomized Controlled Pharmacokinetic and Pharmacodynamic Trial. (PubMed, J Clin Pharmacol) - "The extended regimen in children with HIV did not result in a statistically significant reduction in recurrence risk at 28 or 42 days. Extending the duration of AL to 5 days compensated for a clinically significant reduction in all components of AL in the context of EFV-based antiretroviral therapy in young children."

Journal • PK/PD data • Human Immunodeficiency Virus • Infectious Disease • Malaria

Two-photon NAD(P)H-FLIM reveals unperturbed energy metabolism of Ascaris suum larvae, in contrast to host macrophages upon artemisinin derivatives exposure. (PubMed, Sci Rep) - "Artemisinin derivatives (ARTs)-artesunate, artemether, and dihydroartemisinin-are standard malaria treatments and are also known to influence the energy metabolism of parasites, tumors, and immune cells...In contrast, exposure of M2-like macrophages to ARTs induced a metabolic shift towards high anaerobic glycolysis and reduced metabolic activity, suggesting a possible indirect effect of ARTs on the helminth infection. Overall, two-photon NAD(P)H-FLIM proved to be a powerful tool for studying specific metabolic pathways in Ascaris larvae and host macrophages, offering valuable insights into the metabolic mechanisms of drug action on both parasite and host."

Journal • Infectious Disease • Malaria • Oncology • IL4

Research progress on artemisinin and its derivatives in treatment of orthopedics-related diseases (PubMed, Zhongguo Zhong Yao Za Zhi) - "Artemisinin, a sesquiterpene lactone compound extracted from Artemisia annua, has led to the gradual synthesis of various derivatives such as dihydroartemisinin, artesunate, artemether, and arteether. Recent pharmacological studies have found that artemisinin and its derivatives can treat osteoporosis, osteoarthritis, rheumatoid arthritis, osteosarcoma, and other orthopedic diseases by regulating osteoblast-osteoclast coupling, modulating immune response, inhibiting angiogenesis, protecting cartilage, and inhibiting tumor growth. This paper reviewed the metabolic characteristics and mechanisms of action of artemisinin and its derivatives in the treatment of orthopedic diseases, aiming to inspire modern research on artemisinin-based drugs and orthopedic diseases."

Journal • Review • Immunology • Musculoskeletal Diseases • Oncology • Orthopedics • Osteoarthritis • Osteoporosis • Osteosarcoma • Pain • Rheumatoid Arthritis • Rheumatology • Sarcoma • Solid Tumor

Artemether Ameliorates Non-Alcoholic Steatohepatitis by Restraining Cross-Talk Between Lipotoxicity-Induced Hepatic Hepatocytes and Macrophages. (PubMed, Phytother Res) - "Impaired mitochondrial structure and function were confirmed in FFA-stressed hepatocytes and the HFHF-diet-induced NASH mouse model, which was reversed by Art treatment. The present study provides evidence for Art as a potential anti-pyroptosis therapeutic agent for NASH treatment."

Journal • Fibrosis • Hepatitis B • Hepatology • Immunology • Inflammation • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • IL18 • IL1B

Microvolume analysis of antimalarial drugs for pediatric pharmacokinetic-pharmacodynamic studies (ASTMH 2024) - "We have developed plasma methods to determine concentrations of artemether and dihydroartemisinin (50 μL), piperaquine (25 μL), hydroxychloroquine and its metabolites (20 μL), amodiaquine (AQ) and desethylamodiaquine (DEAQ, 10 μL), lumefantrine and desbutyl lumefantrine (5 μL), sulfadoxine (SDX), and pyrimethamine (PYR, 5 μL). The method was used to analyze 366 clinical samples, among which 82% have quantifiable AQ/DEAQ and 83% have quantifiable SDX/PYR. In summary, LC-MS/MS enables microvolume sampling and subsequent drug analysis to support clinical studies in pediatric populations."

Clinical • PK/PD data • Infectious Disease • Pediatrics

Leveraging a Plasmodium falciparum genetic cross to identify candidate determinants of multigenic resistance to quinine and chloroquine (ASTMH 2024) - "The WHO recommends quinine (QN) as an option for treating severe malaria when artesunate or artemether are not available or are contraindicated. This chromosome 12 peak was also associated with CQ resistance in addition to the dominant pfcrt peak on chromosome 7. Our data reveal a multigenic basis of QN resistance and identify a potential new modulator of mutant pfcrt -mediated CQ resistance."

Infectious Disease • Malaria • DMRT1

Malaria risk stratification: a critical tool for malaria control and elimination in high burden country, case of Mali (ASTMH 2024) - "Finally, to delay drug resistance with Artemether Lumefatrine (AL), Dihydro-artemisinin-Piperaquine (DHA-PPQ) will be introduced as a first line treatment along with AL in 5 high burden regions. Malaria stratification is a critical for strategic planning and appropriate deployment of malaria control interventions. It requires a multi-disciplinary team as well as recent and reliable data, with periodic updates."

Clinical • Infectious Disease • Malaria

Effects of nanocapsules containing lumefantrine and artemether in an experimental model of cerebral malaria. (PubMed, Discov Nano) - "Nanoformulations can potentially improve the efficacy of antimalarial drugs and be considered a promising approach to treat malaria."

Journal • Infectious Disease • Malaria • IL1B • TNFA

Advances in the study of artemisinin and its derivatives for the treatment of rheumatic skeletal disorders, autoimmune inflammatory diseases, and autoimmune disorders: a comprehensive review. (PubMed, Front Immunol) - "Recent studies have demonstrated that artemisinin-based antimalarial drugs, such as artesunate, dihydroartemisinin, and artemether, not only possess excellent antimalarial properties but also exhibit antitumor, antifungal, and immunomodulatory effects...These downstream targets regulate various immune cell functions, apoptosis, proliferation, signal transduction, and antioxidant responses, ultimately intervening in systemic autoimmune diseases and autoimmune responses in organs such as the kidneys, nervous system, skin, liver, and biliary system by modulating immune dysregulation and inflammatory responses. Ongoing multicenter randomized clinical trials are investigating the effects of these compounds on rheumatic, inflammatory, and autoimmune diseases, with the aim of translating promising preclinical data into clinical applications."

Clinical • IO biomarker • Journal • Review • Immune Modulation • Immunology • Infectious Disease • Inflammation • Malaria • Oncology • GPX4 • IL6

Truth is relative; Client report versus provider report, a post-modern analysis of data from a trial in the private retail medicine sector. (PubMed, Res Sq) - "Outlets reported that 97% of test-positive clients received a first-line Artemether Combination Therapy (ACT), but only 77% of clients who reported a positive test also reported receiving the first-line ACT in the exit interview...Contrasting outcomes reported by the provider and the client highlight barriers to improving testing and adherence for malaria as well as challenges for monitoring case management in the retail sector. These include accurate communication of results to the client, poor confidence in a negative result, and reluctance to withhold antimalarials from test-negative clients."

Journal • Infectious Disease • Malaria

Haematological Profile and Antibiotic Resistance of Bacteria Responsible for Enteric Infections Isolated From Patients Suffering From Malaria and Enteric Infections on Consultation at the Dschang Regional Hospital. (PubMed, Can J Infect Dis Med Microbiol) - "Quinine (53[50.00%]; 6[42.86%]) presented a minimal inhibitory concentration (MIC) of 32 μg/mL on the bacteria isolates from coinfected and monoinfected patients, respectively, while Artemether 89 (83.96%), Maloxine 5 (3.94%) and Surquina 250 (39.37%) presented a MIC of 64 μg/mL on bacterial isolates of coinfected and monoinfected patients...coli showed high resistance against AKI (45.93%), AMX (43.75%) and ERY (59.37%) in malaria patients who were under antimalarial drugs compared to malaria patients who were not under malaria drugs (29.68%, 34.37% and 32.81%, respectively). This study highlights that antimalarial drugs might certainly have an influence on the acquisition and emergence of bacterial resistance in the case of malaria bacterial coinfection, and therefore, adequate management and planning effective control programmes might certainly go a long way to reduce the rate of morbidity and mortality."

Journal • Hematological Disorders • Infectious Disease • Malaria • CD4 • CD8

Developing Self-Nanoemulsifying Drug Delivery Systems Comprising an Artemether-Lumefantrine Fixed-Dose Combination to Treat Malaria. (PubMed, Front Biosci (Elite Ed)) - "This study offers evidence that SNEDDSs from selected natural oils comprising an artemether-lumefantrine FDC can potentially enhance the bioavailability of these lipophilic drugs."

Journal • Infectious Disease • Malaria

Antimalarial Mechanisms and Resistance Status of Artemisinin and Its Derivatives. (PubMed, Trop Med Infect Dis) - "Scientists have created dihydroartemisinin, artemether, artesunate, and other derivatives preserving artemisinin's peroxide bridge to increase its clinical utility value...Understanding the antimalarial and resistance mechanisms of artemisinin drugs helps develop novel antimalarials and guides the rational application of antimalarials to avoid the spread of resistance, which is conducive to malaria control and elimination efforts. This review will discuss the antimalarial mechanisms and resistance status of artemisinin and its derivatives, which will provide a reference for avoiding drug resistance and the research and development of new antimalarial drugs."

Journal • Review • Infectious Disease • Malaria