mefloquine / Generic mfg. - LARVOL DELTA

Global assessment of partial artemisinin resistance: Multicenter trial across Kenya, Peru, and Thailand in patients with uncomplicated Plasmodium falciparum malaria. (PubMed, Int J Infect Dis) - "This is the first concurrent evaluation of artemisinin resistance across three continents. The presence of 11% Thai subjects that satisfied WHO criteria for drug resistance establishes this area as endemic. Longer PC1/2 found in wildtype and candidate K13 mutant infections within the Thai cohort require further investigation to identify alternative mechanisms of resistance."

Journal • Infectious Disease • Malaria

Temporal GeneTerrain: advancing precision medicine through dynamic gene expression visualization. (PubMed, Front Bioinform) - "We applied Temporal GeneTerrain to compare transcriptomic perturbations induced by mefloquine (M), tamoxifen (T), and withaferin A (W), both individually and in all-pairwise and triple combinations (TM, TW, MW, and TMW), in LNCaP prostate cancer cells using the GSE149428 dataset (0, 3, 6, 9, 12, and 24 h). Compared to other approaches, such as heatmaps and static clustering, Temporal GeneTerrain uniquely captures the transient nature of gene expression patterns. This method significantly enhances the interpretability of complex biological datasets, thereby supporting informed decision-making in biological research and therapeutic development."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Progressive multifocal leukoencephalopathy secondary to idiopathic CD4 lymphocytopenia with balanced CD4/CD8 inflammation significantly improved after treatment with mirtazapine and mefloquine. (PubMed, J Neurol Sci) - No abstract available

Journal • CNS Disorders • Hematological Disorders • Inflammation • Rare Diseases • CD4

Arylmethylamino steroid compound 1o interferes with Plasmodium falciparum's hemoglobin metabolism. (PubMed, Antimicrob Agents Chemother) - "We found that 1o increases cytosolic [ATP] level and causes a slight drop in pH, similar to the effects of arylamino alcohols such as mefloquine. The compound also prevents chloroquine (CQ)-mediated proteolysis and limits cytosol acidification within the range of its EC50...These findings suggest that the mechanism underlying the killing activity of 1o may be the interference of a pathway within or upstream of hemoglobin digestion, particularly during the highly metabolically active earlier parasite stages. Our data open a new perspective on the compound's mode of action, information critically needed for target identification and further drug development."

Journal • Infectious Disease • Malaria • Targeted Protein Degradation

Contribution of Pannexin Channels to Afterimage Signals in the Amphibian Retina. (PubMed, Am J Physiol Cell Physiol) - "Whole-cell patch-clamp recordings showed that these channels have high permeability to Cl⁻ ions, which can be blocked by 10Panx1 peptide, carbenoxolone, and mefloquine, all recognized as Panx1 inhibitors. These delayed spontaneous responses in ganglion cells, known as rebound currents, are associated with afterimage signals in the retina. Our findings suggest that Panx1 channels help prevent over-excitation associated with bright light-induced afterimage phenomena."

Journal • CNS Disorders

A comprehensive revision on the use of quinoline antimalarial drugs as leishmanicidal agents. (PubMed, Front Chem) - "and against in vivo models of eleven key antimalarials, including chloroquine, sitamaquine, amodiaquine, mefloquine, quinine, primaquine, hydroxychloroquine, tafenoquine, quinacrine and moxipraquine. Mechanistic studies and advances in clinical treatment are also discussed. This mini-review aims to show the state of the art in using antimalarial drugs to discover alternative therapies for leishmaniasis treatment."

Journal • Review • Infectious Disease

Acute eosinophilic pneumonia associated with mefloquine prophylaxis: A case report. (PubMed, Respir Med Case Rep) - "Mefloquine should be considered a potential cause of acute eosinophilic pneumonia, particularly in patients with recent drug exposure. Early recognition and timely management, including drug discontinuation and corticosteroid therapy, are crucial to preventing severe complications and ensuring favorable outcomes."

Journal • Eosinophilia • Immunology • Infectious Disease • Malaria • Pneumonia • Pulmonary Disease • Respiratory Diseases

Evaluating the Safety and Efficacy of Malaria Preventive Measures in Pregnant Women with a Focus on HIV Status: A Systematic Review and Network Meta-Analysis. (PubMed, J Clin Med) - " In HIV-positive pregnant women, Co-trimoxazole with dihydroartemisinin significantly reduced malaria incidence compared to Co-trimoxazole alone (RR = 0.45, 95% CI [0.30; 0.68]) and sulfadoxine-pyrimethamine (SP) (RR = 0.14, 95% CI [0.04; 0.48]). Co-trimoxazole with dihydroartemisinin and mefloquine are effective for HIV-infected pregnant women, while azithromycin-piperaquine and mefloquine work well for those without HIV. Customized prevention strategies considering HIV status are crucial for optimal protection."

Journal • Retrospective data • Review • Human Immunodeficiency Virus • Infectious Disease • Malaria

Synthesis of 3-Carboxy-6-sulfamoylquinolones and Mefloquine-Based Compounds as Panx1 Blockers: Molecular Docking, Electrophysiological and Cell Culture Studies. (PubMed, Molecules) - "In particular, 12f was a more potent Panx1 blocker than the reference compound CBX (IC50 = 2.7 µM versus IC50 = 7.1 µM), and its profile was further investigated in a cell culture model of polycystic kidney disease. Finally, interesting results have been highlighted by new molecular modeling studies."

Journal • Preclinical • Cardiovascular • Genetic Disorders • Ischemic stroke • Nephrology • Neuralgia • Oncology • Pain • Polycystic Kidney Disease • Renal Disease

Atovaquone Inhibits ABCC1 and Decreases Camp Egress in Human Airway Smooth Muscle Cells (ATS 2025) - "This abstract is funded by: NIH, National Heart, Lung, and Blood Institute grant P01HL114471, R01HL164404 RATIONALE: Evidence suggests that atovaquone and mefloquine, anti-malarial drugs, modulate the activity of ATP-binding cassette (ABC) transport proteins. Atovaquone inhibits ABCC1 activity in HASM cells, offering a new approach to repurpose anti-malaria drugs to enhance cAMP signaling and PKA-dependent HASM relaxation in the treatment of airflow obstruction in asthma."

Asthma • Immunology • Infectious Disease • Malaria • Respiratory Diseases • ABCC1

Genetic surveillance of Plasmodium falciparum populations following treatment policy revisions in the Greater Mekong Subregion. (PubMed, Nat Commun) - "While regional artemisinin resistance levels remained high, no evidence of emerging mefloquine resistance was found. Routine genetic surveillance proved valuable in monitoring rapid parasite population changes in response to public health interventions, providing actionable information for NMCPs."

Journal • Infectious Disease • Malaria

Screening and transcriptomic analysis of anti-Sporothrix globosa targeting AbaA. (PubMed, Front Microbiol) - "Azelastine and Mefloquine effectively inhibit S. globosa and S. schenckii...And qRT-PCR and transcriptome results underscore the significance of the abaA gene in Sporothrix. Our results lay the foundation for the search for new treatments for other mycosis."

Journal • Dermatology • Infectious Disease

Efficacy of mefloquine for progressive multifocal leukoencephalopathy: a review of five cases (JSNE 2025) - No abstract available

Clinical • Review • CNS Disorders • Rare Diseases

Temozolomide, Memantine Hydrochloride, Mefloquine, and Metformin Hydrochloride in Treating Patients With Glioblastoma Multiforme After Radiation Therapy (clinicaltrials.gov) - P1 | N=144 | Terminated | Sponsor: M.D. Anderson Cancer Center | Trial completion date: Sep 2025 ➔ Feb 2025 | Active, not recruiting ➔ Terminated | Trial primary completion date: Sep 2025 ➔ Feb 2025; <75 % participant accrual

Trial completion date • Trial primary completion date • Trial termination • Brain Cancer • Glioblastoma • Gliosarcoma • Oncology • Sarcoma • Solid Tumor

Mechanism of read-through enhancement by aminoglycosides and mefloquine. (PubMed, Proc Natl Acad Sci U S A) - "The results underscore the crucial role of the bridge B7b/c in mediating the effects of MFQ on subunit rotation dynamics. Through a comprehensive analysis of the interactions between the drugs and the eukaryotic ribosome, we propose a unifying hypothesis for read-through enhancement by small molecules, highlighting the role of decoding center rearrangements and intersubunit rotation dynamics."

Journal • Infectious Disease

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) - "In some cats with feline infectious peritonitis a high-dose induction protocol, using acute-phase proteins and the albumin/globulin ratio for treatment cessation, enabled a shorter treatment period than the conventional 12 weeks, without observed recurrence. The criteria used in this study appear adequate for determining appropriate times for feline infectious peritonitis treatment cessation."

Journal

CYP1A2 contributes to the metabolism of mefloquine: Exploration using in vitro metabolism and physiologically-based pharmacokinetic modelling. (PubMed, Drug Metab Dispos) - "Simulated mefloquine exposures increased by 88% when an interaction with fluvoxamine, a CYP1A2 inhibitor was modeled. Here, we identify CYP1A2 as a key enzyme involved in mefloquine metabolism and use physiologically-based pharmacokinetic modeling to demonstrate the contribution of this route to interactions with mefloquine. The in vitro data and revised physiologically-based pharmacokinetic model are important starting points for future exploration of this pathway using clinical data."

Journal • PK/PD data • Preclinical • Infectious Disease • Malaria • CYP1A2 • CYP3A4

Mefloquine reduces the bacterial membrane fluidity of Acinetobacter baumannii and distorts the bacterial membrane when combined with polymyxin B. (PubMed, mBio) - "MFQ synergized with the membrane permeabilizers polymyxin B and colistin and the MFQ + polymyxin B combination killed bacterial cells more effectively than either treatment alone. In contrast, the membrane permeabilizer polymyxin B is associated with significant neurotoxicity and nephrotoxicity. Our findings highlight the potential of membrane-acting compounds, such as MFQ, to enhance combinatorial activity while mitigating polymyxin B-associated toxicity."

Journal • Infectious Disease • Pneumonia

Not Fishy at All: Hair Cell Damage and Protection in the Zebrafish Model System (ARO 2025) - ": We demonstrate that lateral line hair cells are susceptible to damage from several putative COVID-19 therapies, such as mefloquine and prazosin, with comparable hair cell loss to a known ototoxin, gentamicin. Our studies underscore the potential of zebrafish as an excellent model for understanding hair cell damage and provide a valuable platform for developing preventative therapies targeted to specific toxic insults. Our future studies will determine ototoxin-specific signatures to identify targets for therapeutic intervention."

Infectious Disease • Mood Disorders • Novel Coronavirus Disease • Otorhinolaryngology

In vitro synergistic effects of mefloquine combined with other antimicrobial agents on carbapenem-resistant Enterobacterales. (PubMed, Eur J Clin Microbiol Infect Dis) - "According to our study, COL-MEF may offer a potential alternative for treating CRE infections, especially COL-R Gram-negative bacterial infections."

Journal • Preclinical • Infectious Disease • Pneumonia

Mefloquine Suppresses Metastasis in Renal Cell Carcinoma Through Targeting SPC25. (PubMed, Cancer Sci) - "It was the first to report that mefloquine achieves its anti-metastatic effects by binding to SPC25 and inhibiting epithelial-mesenchymal transition. These results suggest that SPC25 has the potential to serve as an early biomarker for metastatic risk in RCC and highlight a novel strategy where mefloquine inhibits RCC metastasis through SPC25 binding, offering new avenues to improve the prognosis of RCC patients."

IO biomarker • Journal • Genito-urinary Cancer • Oncology • Solid Tumor

PBPK-Led Assessment of Antimalarial Drug Concentrations in Breastmilk: A Strategy for Optimal Use of Prediction Methods to Guide Decision Making in an Understudied Population. (PubMed, CPT Pharmacometrics Syst Pharmacol) - "Physiologically based pharmacokinetic (PBPK) modeling was used to predict milk-to-plasma (M/P) ratios, infant daily doses (IDD) and relative infant doses (RID) for five antimalarials with clinical lactation data (chloroquine, pyrimethamine, piperaquine, mefloquine and primaquine)...RID was  10% for lumefantrine and tafenoquine. For atovaquone, RID was > 10% with Model 1 but not Model 2...These prediction methodologies can be used, alongside any licensed dosing information for < 1 year-olds, to evaluate whether a clinical lactation study is necessary and to inform drug label or policy recommendations. The ultimate goal is to better inform optimal treatment for lactating women supporting malaria eradication."

Journal • Infectious Disease • Malaria

Quinoline analogs: multifaceted heterocyclic compounds with varied synthetic strategies and potent antitubercular properties. (PubMed, RSC Adv) - "Some fused analogs of quinoline, such as graveolinine, ciprofloxacin, kokusaginine, bedaquiline, levofloxacin, moxifloxacin, and mefloquine, are commercially available as antitubercular drugs. There are various methods available to synthesize quinoline-containing antitubercular drugs. In this review paper, we present three types of synthetic methods in which substituted quinolines, substituted anilines, and miscellaneous starting materials are used and outline MIC values for all the synthesized compounds to signify their anti-TB activity."

Journal • Review • Alzheimer's Disease • Asthma • CNS Disorders • Fatigue • Human Immunodeficiency Virus • Immunology • Infectious Disease • Oncology • Pain • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Endolysosome-targeted nanoparticle delivery of antiviral therapy for coronavirus infections. (PubMed, Life Sci Alliance) - "Mefloquine is a more effective inhibitor of viral endocytosis than hydroxychloroquine in cellular models of COVID-19. MFQ-NPs inhibit coronavirus infection in mouse MHV-A59 and human OC43 coronavirus model systems and inhibit SARS-CoV-2 WA1 and its Omicron variant in a human lung epithelium model. Organelle-targeted delivery is an effective means to inhibit viral infection."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Mefloquine reduces the bacterial membrane fluidity of Acinetobacter baumannii and distorts the bacterial membrane when combined with polymyxin B. (PubMed, bioRxiv) - "MFQ synergized with the membrane permeabilizers polymyxin B and colistin and the MFQ+polymyxin B combination killed bacterial cells more effectively than either treatment alone. In contrast, the membrane permeabilizer polymyxin B is associated with significant neurotoxicity and nephrotoxicity. Our findings highlight the potential of membrane-acting compounds, such as MFQ, to enhance combinatorial activity while mitigating polymyxin B-associated toxicity."

Journal • Infectious Disease • Pneumonia