artemether / Generic mfg. - LARVOL DELTA

Pharmacogenomics in Orofacial Clefts Care: Insights from Whole-Genome Sequencing of Case-Parents Trios. (PubMed, J Pers Med) - "The identified variations were linked to the metabolism of frequently used pharmaceuticals in Africa, such as caffeine, ketoconazole, efavirenz, carbamazepine, and artemether. These findings highlight the need for pharmacogenetic screening to inform personalized medicine, diminish ADRs, and enhance the clinical care of OFCs in Sub-Saharan Africa."

Biomarker • Journal • ABCC3 • CYP1A2 • CYP27A1

Identification of a novel locus associated with decreased susceptibility of Plasmodium falciparum to lumefantrine and artemisinin in Uganda (ASTMH 2025) - "The most common artemisinin-based combination (ACT), artemether-lumenantrine, is threatened in Uganda, where multiple artemisinin partial resistance (ART-R) mutations in Kelch13 (K13), including the C469Y and A675V mutations, are spreading, and decreasing lumefantrine (LUM) susceptibility has been demonstrated...PIN-carrying isolates showed significantly decreased ex vivo susceptibility to LUM, mefloquine and dihydroartemisinin (DHA) compared to WT (P<0.0001 for each drug). The newly identified PIN haplotype represents a candidate marker for decreased susceptibility to DHA and/or LUM. Its rapid spread in Uganda underscores the importance of evaluating its distribution and role in the emergence of ART-R elsewhere in East Africa."

Late-breaking abstract • Infectious Disease

Population pharmacokinetics of artemether-lumefantrine plus amodiaquine in patients with uncomplicated Plasmodium falciparum malaria. (PubMed, Br J Clin Pharmacol) - "The DDI effect of amodiaquine on the pharmacokinetics of artemether-lumefantrine is expected to be minimal, the based on the current analysis. However, further large-scale clinical trials are needed to confirm this finding."

Journal • PK/PD data • Infectious Disease • Malaria

Arterolane and Piperaquine Vs. Artemether and Lumefantrine in Uncomplicated Malaria: A Randomized Study in Nigeria. (PubMed, Int J Infect Dis) - "Once-daily dosing of AMP demonstrates comparable efficacy and safety to standard twice-daily dosing of AL in the treatment of uncomplicated P. falciparum malaria."

Journal • Infectious Disease • Malaria

Anti-Inflammatory Efficacy of a Functional Shampoo Mixed With 0.063% Artemether for Seborrheic Dermatitis. (PubMed, J Cosmet Dermatol) - "The 0.063% artemether shampoo has comparable clinical efficacy to the 2% ketoconazole shampoo in the treatment of SD, and may exhibit stronger anti-inflammatory effects."

Journal • Dermatitis • Dermatology • Immunology • Inflammation • Seborrheic Dermatitis • CXCL8 • IL17A • IL1B • NFKB1

Discovery of novel Plasmodium falciparum PfDHFR-TS inhibitors from ConMedNP natural compounds: a multi-computational approach. (PubMed, Mol Divers) - "DFT analysis highlighted CA0001's reactivity as a soft electrophile, contrasting with artemether's higher reactivity. This comprehensive approach integrating docking, QSAR, DFT, and MD positions CA0001 as a promising PfDHFR-TS inhibitor alongside artemether, with ConMedNP and predictive models guiding future experimental validation."

Journal • Infectious Disease • DHFR • TYMS

Artemether ameliorates type 1 diabetes mellitus by modulating glycolipid metabolism in skeletal muscle. (PubMed, Am J Transl Res) - "Artemether treatment inhibited pyruvate dehydrogenase kinase 4 activity and activated pyruvate dehydrogenase, promoting aerobic glucose metabolism and suppressing fatty acid metabolism in skeletal muscle. These findings suggest that artemether can alleviate symptoms in T1D mice by modulating glycolipid metabolism in skeletal muscle."

Journal • Diabetes • Infectious Disease • Metabolic Disorders • Type 1 Diabetes Mellitus • PDK4

Efficacy of Anti-Toxoplasma Medications in Symptom Severity and Cognition in Patients with Schizophrenia or Schizoaffective Disorder: Systematic Review and Meta-analysis. (PubMed, Braz J Psychiatry) - "Anti-Toxoplasma antibiotics may offer potential benefits as adjunctive therapy for schizophrenia. However, heterogeneity and methodological limitations complicate conclusions. Large-scale RCTs are needed further to clarify the role of anti-Toxoplasma antibiotics in schizophrenia treatment."

Journal • Retrospective data • CNS Disorders • Infectious Disease • Psychiatry • Schizophrenia

Acetyl-CoA synthetase mutations affect the susceptibility of Plasmodium falciparum to antimalarial drugs. (PubMed, Microbiol Spectr) - "The results demonstrated that PfAcAS S868G and V950I mutations alone or in combination affected the susceptibility of P. falciparum to several antimalarial drugs, including the artemisinin derivatives (dihydroartemisinin, artesunate, and artemether) and chloroquine, although absolute changes in susceptibilities were modest.IMPORTANCEMalaria, an infectious disease caused by Plasmodium parasites and transmitted by mosquitoes, continues to be one of the most pressing public health challenges worldwide. In this study, we performed whole-genome sequencing analysis on P. falciparum strains that reemerged following ACT treatment. We aim to identify molecules potentially associated with drug resistance, which may provide new molecular markers for monitoring drug resistance in P. falciparum."

Journal • Infectious Disease • Malaria

Comparison of Artemether Versus Quinine for the Treatment of Cerebral Malaria in Children: A Meta-Analysis of Randomized Controlled Trials. (PubMed, Cureus) - "In summary, artemether demonstrated a mildly superior efficacy in comparison to quinine. Thus, regions with artemisinin-sensitive strains of malaria are encouraged to continue the use of artemisinin; however, regions with artemisinin resistance may consider the use of quinine as an alternative in the treatment of cerebral malaria in children. Future comprehensive randomized controlled studies are needed to arrive at a robust conclusion."

Journal • Retrospective data • Review • Infectious Disease • Malaria

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