mefloquine / Generic mfg. - LARVOL DELTA

Structural basis of PANX1 permeation and positive modulation by mefloquine. (PubMed, Nat Commun) - "We also identify mefloquine as a positive modulator of PANX1 that binds near the side tunnel to control ion flow through this pathway. Together, these findings define the structural principles underlying PANX1 permeation and modulation."

Journal

Tolerance of Plasmodium falciparum mefloquine-resistant clinical isolates to mefloquine-piperaquine with implications for triple artemisinin-based combination therapies. (PubMed, Nat Commun) - "Mechanistic investigations reveal that MQ inhibits PPQ accumulation in a dose-dependent manner, providing a functional explanation for the compromised efficacy of the combination. These findings demonstrate that MQ resistance alone can undermine MQ-PPQ TACT efficacy, calling into question the strategic rationale of this combination and underscoring the need for alternative regimens with a lower risk of resistance selection."

Journal • ABCB1

Niosomal mefloquine and cisplatin in breast cancer: comparative effects on apoptosis and angiogenesis via in vitro and in silico analysis. (PubMed, BMC Cancer) - "The niosomal formulation of MEF synergistically enhances CIS efficacy by promoting apoptosis, and suppressing angiogenesis in TNBC. These findings highlight NMEF as a promising chemosensitizer to overcome cisplatin resistance. Future studies should focus on in vivo validation and clinical translation."

IO biomarker • Journal • Preclinical • Breast Cancer • Infectious Disease • Oncology • Solid Tumor • Triple Negative Breast Cancer • BAX • BCL2 • CASP3 • KDR

A Case of Cerebellar-Onset Progressive Multifocal Leukoencephalopathy (PML) Associated with Hepatitis B-related Liver Cirrhosis. (PubMed, Intern Med) - "Treatment with mefloquine and mirtazapine resulted in viral clearance from the cerebrospinal fluid (CSF) and clinical stabilization. This case highlights that crescent-shaped cerebellar lesions should raise suspicion of PML, even in patients without severe immunodeficiency."

Journal • Ataxia • CNS Disorders • Fibrosis • Gastroenterology • Hepatitis B • Hepatology • Immunology • Infectious Disease • Inflammation • Liver Cirrhosis • Movement Disorders • Rare Diseases

Transplacental Transfer of Lumefantrine, Mefloquine, and Piperaquine: A Comparison of Concentrations in Mothers, Neonates, and Cord Blood. (PubMed, Clin Infect Dis) - "Antimalarial drugs crossed the placenta variably. Neonatal concentrations ranged from less than half (lumefantrine, mefloquine) to near maternal equivalence (piperaquine). Collection of neonatal capillary samples at birth should be considered in future studies.SummaryWe compared antimalarial blood concentrations in mothers, neonates, and cords. Neonatal drug concentrations ranged from near maternal equivalence (piperaquine) to less than half (lumefantrine, mefloquine). Cord concentrations may underestimate neonatal exposure. Future studies should consider neonatal capillary sampling."

Journal • Infectious Disease • Malaria

Targeting Glycolysis with 2-Deoxy-D-Glucose and Lysosomal Integrity with L-Leucyl-L-Leucine Methyl Ester as Antimelanoma Strategy. (PubMed, Pharmaceutics) - "Background/Objectives: Melanoma cells enhance glycolysis and expand lysosomes to support energy metabolism, proliferation, and metastasis. However, mefloquine and siramesine induced stronger LMP in A375 cells than in fibroblasts and showed melanoma-selective toxicity when combined with 2DG. 2DG-mediated glycolysis inhibition in combination with lysosomal destabilization induced by mefloquine and siramesine, but not with non-selectively toxic LLOMe, may be promising antimelanoma strategy."

Journal • Melanoma • Metabolic Disorders • Oncology • Solid Tumor • CTSC • CTSS • HK2

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

Field-deployable targeted nanopore sequencing to assess molecular markers of anti-malarial resistance, clonality, and Plasmodium falciparum hrp2/3 gene deletions in western Kenya (ASTMH 2025) - "We implemented a rapid amplicon nanopore sequencing panel for crt (chloroquine), dhfr (pyrimethamine), dhps (sulfadoxine), kelch13 (artemisinin), mdr1 (mefloquine), ama1 (complexity of infection), and hrp2/3 (RDT) genes...Nearly all, 97.2% (139/145) samples exhibited the quintuple dhfr (N51I, C59R, S108N) and dhps (A437G, K540E) genotype associated with sulfadoxine-pyrimethamine resistance...Among the 34 samples with potential hrp2/3 gene deletion based on RDT results, none had hrp2/3 gene deletions by nanopore sequencing. Nanopore sequencing is a robust methodology which can be carried out locally, providing powerful information to inform programming."

Biomarker • Infectious Disease • Malaria • ABCB1 • DHFR

Mining for Malaria: Delayed Diagnosis and Prolonged Parasitemia in a Active Duty Servicemember (ASTMH 2025) - "He took doxycycline prophylaxis for the first eight months but switched to mefloquine for less frequent dosing and reported complete adherence. The reason for his delayed parasitemia clearance is unclear. This case highlights the pitfalls of relying on RDT for the diagnosis of malaria and the potential complexities the management of delayed parasitemia clearance and possible artemisinin resistance."

Anemia • Fatigue • Hematological Disorders • Infectious Disease • Influenza • Malaria • Musculoskeletal Pain • Novel Coronavirus Disease • Respiratory Diseases

Genomic Epidemiological Analysis of Antimalarial Drug Resistance Evolution in Mali, 2007-2017 (ASTMH 2025) - "Analyzed haplotypes included mutations in the Pfdhfr and Pfdhps genes, critical for resistance to Sulfadoxine-Pyrimethamine (SP). Chloroquine resistance has notably decreased. No resistance to piperaquine, mefloquine, or artemisinin was detected, indicating their continued efficacy."

Clinical • Infectious Disease • Malaria • ABCB1 • DHFR

Field-deployable targeted nanopore sequencing to assess molecular markers of anti-malarial resistance, clonality, and Plasmodium falciparum hrp2/3 gene deletions in western Kenya (ASTMH 2025) - "We implemented a rapid amplicon nanopore sequencing panel for crt (chloroquine), dhfr (pyrimethamine), dhps (sulfadoxine), kelch13 (artemisinin), mdr1 (mefloquine), ama1 (complexity of infection), and hrp2/3 (RDT) genes...Nearly all, 97.2% (139/145) samples exhibited the quintuple dhfr (N51I, C59R, S108N) and dhps (A437G, K540E) genotype associated with sulfadoxine-pyrimethamine resistance...Among the 34 samples with potential hrp2/3 gene deletion based on RDT results, none had hrp2/3 gene deletions by nanopore sequencing. Nanopore sequencing is a robust methodology which can be carried out locally, providing powerful information to inform programming."

Biomarker • Infectious Disease • Malaria • ABCB1 • DHFR

Natural in vitro susceptibility of Plasmodium falciparum to pyronaridine over 2009-2023 in French Guiana (ASTMH 2025) - "Currently, only artemether-lumefantrine remains effective in the region...Correlation between pyronaridine and other aminoquinoline derivatives including chloroquine, monodesethylamodiaquine, and mefloquine was assessed (r2=0.01; r2=0.04; r2=0.11, respectively), but no cross-resistance was found...However, the synonymous mutation PfMDR1S1034S, observed in 63% of French Guiana isolates, was associated with decreased pyronaridine susceptibility (p < 0.0001). The findings of this study suggest that artesunate-pyronaridine could be a new treatment alternative for P. falciparum in the Amazon region."

Preclinical • Infectious Disease • Malaria • ABCB1

Application of GC3,a locus read coverage assessment tool, and machine learning to predict copy number variations of pfmdr1, plasmepsin-2, and plasmepsin-3 among Plasmodium falciparum strains (ASTMH 2025) - "Specifically, we are focusing on CNVs at the Plasmodium falciparum (Pf) multidrug resistant protein 1 (Pfmdr1), plasmepsin-2 (pm2) and plasmepsin-3 (pm3) genes, which are associated with resistance to partner drugs used in some artemisinin-based combination therapies (ACTs), including mefloquine and piperaquine...Follow up analysis aims to expand our sample set to ~700 publicly available WGS samples from 13 malaria endemic countries in South America, Africa and Asia, and apply machine learning models to improve the prediction of CNVs. By expanding on the previous application of GC3 to identify CNVs, results aim to demonstrate the feasibility of applying bioinformatics to automate accurate prediction and measure the prevalence of CNVs associated with drug resistance using WGS data."

Machine learning • Infectious Disease • Malaria • ABCB1

Impact of COVID-19 pandemic in parasite populations from the Western Brazilian Amazon (ASTMH 2025) - "Samples were collected between 2019 and 2023 were analyzed and subjected to ex vivo assays to determine their response to artemisinin, chloroquine, pyronaridine, pyrimethamine, mefloquine, lumefantrine, ferroquine, piperaquine, and amodiaquine...A high variation in chloroquine susceptibility was observed in both P. falciparum and P. vivax isolates over the analyzed period, which included part of the COVID-19 pandemic, when hydroxychloroquine was broadly used as COVID treatment...Nucleotide insertion in the pvcrt promoter sequences were also detected in parasites with lower chloroquine susceptibility. Our findings reinforce the need for continuous monitoring of antimalarial resistance in the Amazon, highlighting the importance of ex vivo testing and the identification of genetic markers as complementary tools in malaria molecular and epidemiological surveillance."

Clinical • Infectious Disease • Malaria • Novel Coronavirus Disease • ABCB1

Changes in susceptibility of Plasmodium falciparum to antimalarial drugs in Uganda over time: 2019-2024 (ASTMH 2025) - "Between 2019 and 2024, susceptibilities increased for chloroquine (IC50 24.0 nM → 15.4 nM) and decreased for lumefantrine (5.9 nM → 20.0 nM), mefloquine (12.5 nM → 20.1 nM), and dihydroartemisinin (1.8 nM → 3.8 nM)...For aminoquinolines and pyrimethamine, genotypes associated with susceptibility were those previously identified...For DHA, susceptibility was decreased with the PfK13 C469Y (WT 2.0 nM vs. mutant 3.6 nM) or A675V (WT 2.0 nM vs. mutant 3.8 nM) and PfMDR1 Y500N (WT 1.9 nM vs. mutant 5.4 nM) mutations. Decreasing activities of lumefantrine and DHA may lead to decreased antimalarial efficacy of artemether-lumefantrine, the first-line regimen in Uganda."

Infectious Disease • Malaria • ABCB1 • WT1

Drug susceptibility and PfK13 mutations in Plasmodium falciparum isolates from severe and uncomplicated malaria patients in northern Uganda (ASTMH 2025) - "Susceptibility to all 9 drugs was similar for isolates collected from severe and uncomplicated malaria patients by IC50 (median: DHA 3.9 nM vs 3.6 nM, lumefantrine 13.8 vs 16.8, piperaquine 3.8 vs 4.7, pyronaridine 0.6 vs 0.8, mefloquine 13.5 vs 15.9, monodesethylamodiaquine 6.1 vs 7.3, chloroquine 14.3 vs 11.3, quinine 78.9 vs 92.2, and pyrimethamine 26,369 vs 26,548) and DHA RSA (median survival 2.4% vs 2.4%). In summary, P. falciparum susceptibility to standard antimalarials did not differ between patients with uncomplicated or severe malaria, but ART-R-mediating PfK13 mutations were more prevalent in severe malaria isolates. These results might be explained by enhanced virulence of mutant parasites or an increased likelihood of recent treatment, selecting for PfK13 mutations, in those presenting with severe compared to uncomplicated malaria."

Clinical • Infectious Disease • Malaria

Comprehensive profiling of ex vivo drug susceptibility of clinical isolates of Plasmodium vivaxin Southeast Asia (ASTMH 2025) - "Fresh P. vivax clinical isolates (N = 997) from six provinces in Cambodia and Thailand from 2019 - 2023 were evaluated using an ex vivo culture growth inhibition assay against a panel of 14 antimalarial drugs: dihydroartemisinin (DHA), artemisinin (AS), mefloquine (MQ), quinine (QN), chloroquine (CQ), doxycycline (DOX), proguanil (PG), atovaquone (ATQ), lumefantrine (LUM), cycloguanil (CYC), tafenoquine (TQ), primaquine (PQ), piperaquine (PPQ) and pyronaridine (PND). This study represents one of the largest systematic efforts to collect ex vivo drug susceptibility data from P. vivax isolates in Southeast Asia. Our findings demonstrate the feasibility of carrying out systematic monitoring of P. vivax drug susceptibility and highlight the importance of continued monitoring in the region."

Preclinical • Infectious Disease • Malaria

Comment to "High-dose induction therapy and treatment termination criteria for feline infectious peritonitis with remdesivir, GS-441524 and adjunctive mefloquine: 46 cases (2023)". (PubMed, J Small Anim Pract) - No abstract available

Journal

Making the most of existing antimalarial medicines: a single dose cure with sulfadoxine-pyrimethamine plus artesunate-pyronaridine. (PubMed, Malar J) - "Multi-drug regimens, such as artemether-lumefantrine-amodiaquine appear to be well tolerated, but these are under development to address emerging resistance to lumefantrine and will be unlikely to improve compliance...Mefloquine is excluded for tolerability concerns, amodiaquine because of its use in seasonal malaria chemoprevention, and lumefantrine and piperaquine due to concerns of emerging resistance...Importantly, a comprehensive clinical evaluation will generate valuable real-world insights into community acceptance and operational feasibility. This information will be an important foundation for future design of single dose malaria therapies involving new chemical entities."

Journal • Review • Infectious Disease • Malaria

Evaluation of in vitro drug-drug interactions of ivermectin and antimalarial compounds. (PubMed, Malar J) - "Several of the commonly used antimalarial drugs, are mostly or in part metabolized by CYP3A4 and showed a notable DDI effect on the in vitro metabolism of ivermectin. This could potentially lead to clinically important pharmacokinetic and pharmacodynamic DDIs if co-administered, and needs to be evaluated in prospective clinical trials."

Journal • Preclinical • Infectious Disease • Malaria • CYP3A4

MRI Findings in Sporotrichoid Leishmaniasis: Fascial and Lymphatic Dissemination in Disease Evolution (EADV 2025) - "Due to limited access to Glucantime and the unavailability of Mefloquine in Turkey, treatment with Itraconazole (200 mg/day for 2 months) and topical Imiquimod (3 times per week for 3 months) was initiated...The treatment regimen was switched to liposomal amphotericin B. Treatment with 3 mg/kg/day liposomal amphotericin B resulted in the regression of the lesions. Sporotrichoid leishmaniasis can present with atypical deep tissue involvement, including fascial and lymphatic dissemination. Early diagnosis and appropriate treatment are crucial to managing the progression of the disease."

Dermatology • Infectious Disease

Progress in Synthesis and Therapeutic Applications of Mefloquine: A Review. (PubMed, Curr Top Med Chem) - "In recent years, mefloquine has gained attention for its potential therapeutic applications beyond malaria, with research exploring its use in cancer therapy, parasitic infections, neurological disorders, tuberculosis, and COVID-19. This article covers its synthetic approaches, established application as an antimalarial compound, as well as repurposed therapeutic applications."

Journal • CNS Disorders • Infectious Disease • Malaria • Novel Coronavirus Disease • Oncology • Pulmonary Disease • Respiratory Diseases • Tuberculosis

A common DNA deletion altering the 3'UTR of mdr1 is associated with reduced mefloquine susceptibility in P. vivax parasites from Cambodian patients. (PubMed, Res Sq) - "Finally, we genotyped 592 Cambodian isolates collected between 2014 and 2024 and showed that the mdr1 deletion increased in frequency in Cambodia since the introduction of mefloquine as ACT partner drug. Overall, these findings indicate that a common deletion of a non-coding sequence affects the transcription, stability, or translation of mdr1 in P. vivax parasites and could mediate reduced susceptibility to antimalarial drug(s) currently used for the treatment of uncomplicated vivax malaria."

Journal • Infectious Disease • Malaria • ABCB1

Quinolines interfere with heme-mediated activation of artemisinins. (PubMed, bioRxiv) - "We found that chloroquine (CQ), piperaquine (PPQ), and amodiaquine substantially antagonize dihydroartemisinin (DHA), the active metabolite of artemisinins. Finally, we probed beyond traditional ACTs, evaluating interactions of the proposed triple ACT, DHA-PPQ-Mefloquine, as well as OZ439-quinoline combinations, which were all found to be antagonistic. Collectively, these data raise concerns for the clinical use of peroxide-quinoline combination therapies."

Journal • Infectious Disease • Malaria

Development of quinoline-based carboxamides targeting non-tuberculous mycobacteria (ACS-Fall 2025) - "Some developed or commercial antibiotics containing a quinoline ring have shown potent antimycobacterial activity against NTM, as bedaquiline (BQ), mefloquine (MQ) and Labio-17. The main objective of this work was to develop 2,8-bis(trifluoromethyl)quinoline-4-carboxamides based on the MQ's pharmacophore as alternative to antimycobacterial therapy. Here, we present the design, the synthesis and biological evaluation of these new MQ-based carboxamides."

Nontuberculous mycobacteria • Bronchiectasis • Chronic Obstructive Pulmonary Disease • Cystic Fibrosis • Genetic Disorders • Immunology • Infectious Disease • Nontuberculous Mycobacterial Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis