mefloquine / Generic mfg. - LARVOL DELTA

Shared-Output Aptamer-Gated DNA Nanodevices Program NbaSPARDA Trans-Cleavage for Metabolite and Drug Sensing. (PubMed, Small) - "Adenosine-gated devices achieve detection limits of 0.28 and 0.40 µM in buffer, while Ade-SSA14 supports matrix-spiked relative readout of pentostatin-induced adenosine-related changes in processed HeLa lysate filtrates. A mefloquine aptamer reconfigured with the same 16 nt output achieves detection limits of 0.018 µM in buffer and 0.061 µM by matrix-matched calibration in an acetonitrile-processed blank-serum extract...An exploratory estradiol construct accesses the output channel. Together, these results establish a shared-output interface for programming NbaSPARDA trans-cleavage in metabolite and drug analysis."

Journal

Acute and prolonged effects of anti-malarial drugs on mitochondrial respiration in atrial cardiomyocytes for cardiac safety evaluation. (PubMed, PLoS One) - "These findings provide insights into the effects of anti-malarial drugs on mitochondrial function in cardiomyocytes. Further studies should aim to elucidate the molecular mechanisms underlying these drug-induced mitochondrial effects."

Journal • Cardiovascular • Infectious Disease • Malaria

Pharmacokinetics and Pharmacodynamics of Antimalarial Agents: Optimizing Combination Therapies to Overcome Resistance Mechanisms. (PubMed, J Clin Pharmacol) - "A discussion of PK/PD modeling across agents, including chloroquine, artemisinin and its derivatives, mefloquine, primaquine, and tafenoquine, highlights how inadequate drug exposure, mismatched partner drug kinetics, and host metabolic variability contribute to treatment failure. Collectively, the evidence suggests that refining combination regimens through PK/PD-guided dose optimization is crucial for maintaining efficacy and preventing resistance. Future research must prioritize host-specific factors, stage-specific drug activity, and optimized combination regimens to improve therapeutic outcomes and support malaria eradication."

Journal • PK/PD data • Review • Infectious Disease • Malaria

Comparative efficacy of free and PNAGA-encapsulated antimalarial drugs: temperature-dependent modulation of Plasmodium falciparum growth. (PubMed, Front Pharmacol) - "After 24 h at 4 °C (below the sol-gel transition), PNAGA-mefloquine matched free mefloquine in efficacy, while PNAGA-pyrimethamine remained less effective than free pyrimethamine. These findings confirm that PNAGA is a reproducible, temperature-responsive hydrogel that efficiently encapsulates antimalarial drugs and modulates their availability according to its UCST, with reduced immediate efficacy at 37 °C (above the sol-gel transition) and higher efficacy below the sol-gel transition (4 °C) for PNAGA-mefloquine."

Journal • Infectious Disease

Avian malaria: an in-depth overview on its biology, epidemiology, pathogenesis, clinical features, economic impacts, diagnostic, treatment and control strategies. (PubMed, J Parasit Dis) - "Treatment options are limited, typically involving antimalarial drugs such as chloroquine phosphate, primaquine phosphate, mefloquine, sulfachloropyrazine, sulfaquinoxaline, Trimethoprim, and Pyrimethamine-sulfadoxine combination along with supportive care and environmental management. This review synthesizes current knowledge on the epidemiology, transmission dynamics, and ecological consequences of avian malaria, with the goal of informing conservation and management strategies. The online version contains supplementary material available at https://doi.org/10.1007/s12639-025-01887-z."

HEOR • Journal • Review • Hematological Disorders • Infectious Disease • Malaria

The effect of mefloquine dose on outcome of uncomplicated falciparum malaria treated with artesunate-mefloquine: a WWARN systematic review and individual patient data meta-analysis. (PubMed, Malar J) - "AS-MQ administered over three days is a highly efficacious ACT in low to moderate transmission areas without artemisinin resistance. While further optimisation of the mefloquine dose in the coformulation in children aged 1-5 years could be considered, dose-related early vomiting is highest in this age group and may preclude this."

Clinical • Journal • Retrospective data • Review • Infectious Disease • Malaria

Innovative drug-modified low-generation PAMAM dendrimer complexes for enhancing the solubility and permeability of BCS class II and IV drugs. (PubMed, Int J Pharm) - "The aqueous solubility and membrane permeability of Biopharmaceutics Classification System (BCS) class II and IV drugs, such as furosemide (FUR), sulfadiazine (SDZ), verapamil (VEP), mefloquine (MEF), and the bioactive compound quercetin (QUE), are low. PAMAM dendrimer complexes were able to considerably enhance the solubility of BCS class II and IV drugs through amorphization and non-covalent interactions. We expect that these systems will further improve key biopharmaceutical properties directly associated with the bioavailability of other poorly water-soluble drug candidates."

Journal

Emergence and spread of Plasmodium falciparum PX1 polymorphisms associated with decreased susceptibility to antimalarials in Uganda. (PubMed, Nat Med) - "In Africa, artemether-lumefantrine is the most widely used first-line artemisinin-based combination therapy, but its efficacy in Uganda is increasingly threatened by the emergence of artemisinin partial resistance and reduced lumefantrine susceptibility...PIN-carrying parasites showed significantly decreased ex vivo susceptibilities to lumefantrine, mefloquine and dihydroartemisinin, an active metabolite of artemether. A parasite strain in which px1 was disrupted in vitro showed increased susceptibility to the three drugs. Thus, PX1 polymorphisms appear to impact on the susceptibilities of African malaria parasites to key drugs."

Journal • Infectious Disease • Malaria

Synthesis and antimalarial activity of novel C30-aminated betulin derivatives. (PubMed, Bioorg Med Chem Lett) - "Screening of the seventeen synthesized C30-aminated betulin derivatives for antimalarial activity revealed that the C30-tryptamine analogue 5g exhibited good inhibitory activity against P. falciparum 3D7 and the chloroquine-mefloquine-pyrimethamine multiresistant strain P. falciparum Dd2 with IC50 values of 0.62 μM and 0.24 μM, respectively. Moreover, the compound did not cause red blood cell lysis at concentrations up to 25 μM and displayed moderate cytotoxicity with an IC50 value of 4.2 μM against human keratinocytes HaCaT cells. These results highlight the great potential of the prop-1-en-2-yl moiety on lupane triterpenoids to improve biological and physicochemical properties and support the extension of the chemical diversity at the C30 position towards new bioactive antiprotozoal betulin analogues."

Journal • Infectious Disease • Malaria

An orally available PfPKG inhibitor blocks Plasmodium's infection of the liver. (PubMed, PLoS Pathog) - "The compound retains activity against field isolates resistant to chloroquine, mefloquine, cycloguanil, sulfadoxine and pyrimethamine, suggesting low likelihood of cross-resistance to existing antimalarials. While selectivity profiling identified off-target activity against human kinases, structural modeling provides a clear path for optimization. These results establish PfPKG inhibitors as promising candidates for chemoprevention and support further preclinical development of the RUPB-61 chemotype."

Journal • Infectious Disease • Malaria

A combination of artemisinin, moxidectin, and doxorubicin drugs can selectively and efficiently induce apoptosis in acute lymphoblastic and chronic myeloid leukemia cells in vitro and ex vivo. (PubMed, Med Oncol) - "The first step determines the lowest EC50 for each drug (e.g., artemisinin, chloroquine, primaquine, mefloquine, ivermectin, moxidectin, doxorubicin, and minocycline) by analyzing four cell endpoints (e.g., cell cycle, sub-G1, mitochondrial membrane potential (ΔΨm), autophagy (lysosomes), and cleaved caspase 3 (CC3)) on K562 cells. The combined drugs were innocuous to peripheral blood lymphocytes (PBLs) (S phase = 40%; G2/M = 26%; ΔΨm = 4%; lysosomes = 3%; CC3 = 4%; n = 3). Our approach to combining drugs has the potential to provide a new pharmacological treatment for leukemias."

Journal • Preclinical • Acute Lymphocytic Leukemia • Chronic Myeloid Leukemia • Hematological Malignancies • Infectious Disease • Leukemia • Oncology • CASP3

Anti-malarial contact dependent blocking of transmission of Plasmodium vivax by Anopheles darlingi mosquito vector. (PubMed, PLoS Pathog) - "Among the antimalarials evaluated were Atovaquone (ATQ), Tafenoquine (TQ), Chloroquine (CQ), Mefloquine (MQ), Primaquine (PQ), and the compound Nanchangmycin (NCG). In addition, MQ also significantly reduced infection intensity, but there was no difference in infection prevalence. No significant differences were observed for the other antimalarials."

Journal • Infectious Disease • Malaria

Post-Deployment Screening of Thailand Military Units Deployed to South Sudan from 2023 to 2025 Reveals High Rates of Sub-Microscopic P. falciparum Malaria. (PubMed, Trop Med Infect Dis) - "The unit is given doxycycline one week before travel before switching to the UN-provided mefloquine during deployment and for four weeks after returning. Furthermore, post-deployment screening revealed high rates of sub-microscopic and sub-clinical parasitemia with 40% of all malaria cases being identified as asymptomatic during post-deployment screening, and 61% of those asymptomatic cases being detected by PCR only. While factors underlying the high prophylaxis failure rate, as well as the high rate of sub-microscopic and sub-clinical parasitemia are unclear, these findings highlight the limitations of relying on clinical symptoms or microscopy for detecting malaria in military units returning from endemic regions and underscore the importance of unit-wide post-deployment molecular screening."

Journal • Infectious Disease • Malaria

Assessment of long-term mental health effects of mefloquine use during pregnancy: a secondary analysis of a randomized clinical trial in Benin. (PubMed, Travel Med Infect Dis) - P=N/A | "We found no evidence that MQ compared with SP affected maternal depression, anxiety, or infant development at one year. The associations with maternal involvement and learning materials warrant further investigation into possible indirect or behavioral effects of MQ."

Clinical • Journal • CNS Disorders • Depression • Infectious Disease • Malaria • Mood Disorders • Postpartum Depression • Psychiatry

Variance in IC50 in in vitro/ex vivo antimalarial drug susceptibility assays in laboratories across Africa. (PubMed, J Antimicrob Chemother) - "The IC50 values of the major antimalarial drugs, including dihydroartemisinin (DHA), lumefantrine (LUM), mefloquine (MFQ), amodiaquine (AMD), chloroquine (CQ), piperaquine (PPQ), artesunate (ATS), artemisinin (ART) and quinine (QN), were reported. These differences together could account for the variance in IC50 values across sSA. We therefore recommend regional harmonization of the IC50 protocol for antimalarial drug efficacy surveillance and formation of a regional quality assessment network of malaria IC50 labs, as a step towards reliable data sharing and integration into strategic plans for malaria elimination."

Journal • Preclinical • Infectious Disease • Malaria

Targeting ALKBH5 with mefloquine as a therapeutic strategy to enhance antitumor immunity in osteosarcoma. (ASCO 2026) - "These findings identify ALKBH5 as a clinically relevant regulator of osteosarcoma progression and antitumor immunity. Mefloquine, an FDA-approved antimalarial drug, demonstrates potent antitumor and immunomodulatory activity through ALKBH5 inhibition and represents a promising repurposing strategy for osteosarcoma treatment. This work provides a strong preclinical rationale for further clinical investigation of ALKBH5-targeted therapies, including combination strategies with immunotherapy, in patients with osteosarcoma."

Infectious Disease • Oncology • Osteosarcoma • Sarcoma • Solid Tumor • ALKBH5

To explore molecular targets and combination antimalarial chemotherapeutics as tissue and erythrocytic schizonticides. (PubMed, J Parasit Dis) - "It prevents the entry of sporozoite into hepatocytes by fusing the CSP with recombinant RTS, S protein Surface other antimalarial drugs that target the Erythrocytic stage are Quinine, Chloroquine, Amodiaquine, Mefloquine, Hydroxyethylamines. These either prevent the detoxification or invasion inside RBC or kill the parasite. Several combinations antimalarial chemotheraputics like ELQ300, MMV019066 are also used for the full reduction of parasite from the body."

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

Molecular Surveillance of Plasmodium vivax and Plasmodium falciparum Drug Resistance Genes in the Republic of Korea: 2022-2025. (PubMed, Pathogens) - "In the Republic of Korea (ROK), chloroquine is the first-line treatment for Plasmodium vivax (P. vivax), and primaquine is also prescribed to prevent relapse...falciparum), atovaquone-proguanil, pyronaridine-artesunate, and mefloquine are recommended...Group comparisons revealed significant differences (p < 0.05), whereas temporal trends were not observed. Because drug resistance gene mutations can be closely linked to treatment, surveillance of drug resistance genes is expected to contribute to malaria eradication in the ROK through providing basic information related to treatment."

Journal • Infectious Disease • Malaria • ABCB1

Structural and mechanistic insights into the inhibition of Plasmodium falciparum MDR1. (PubMed, Nat Commun) - "The P-glycoprotein homolog P. falciparum Multidrug Resistance Protein 1 (PfMDR1) is a key determinant of resistance to first-line antimalarials like mefloquine (MFQ) and chloroquine. Furthermore, a comparative structural analysis and biochemical characterization with human ABCB1 reveal the selective mechanism of ACT-451840 against PfMDR1. Our findings provide a structural basis for the inhibitory mechanism of ACT-451840, which may inform the future development of antimalarial candidates targeting PfMDR1."

Journal • Infectious Disease • Malaria • ABCB1 • ABCC1

Progressive Multifocal Leukoencephalopathy (PubMed, Brain Nerve) - "In PML patients with human immunodeficiency virus (HIV) infection, antiretroviral therapy is fundamental. In patients with non-HIV PML, various treatments including combination therapy with mefloquine and mirtazapine, as well as new antiviral drugs, have been attempted in recent years."

Journal • Review • CNS Disorders • Infectious Disease • Rare Diseases

Repositioning Mefloquine as an Anticancer Drug: An Evidence-Based Review. (PubMed, Curr Med Chem) - "Apart from its anticancer effects as a single agent, mefloquine has been shown to improve the efficacy of clinical cancer drugs in various study models when used in combination therapy. Keeping in view the aforesaid research findings, Mefloquine may warrant further investigation for potential repurposing in cancer therapy, either as monotherapy or in combination with other clinically practiced chemotherapeutics."

Journal • Brain Cancer • Breast Cancer • Cervical Cancer • Chronic Myeloid Leukemia • Colorectal Cancer • Gastric Cancer • Genito-urinary Cancer • Glioblastoma • Hematological Malignancies • Infectious Disease • Leukemia • Malaria • Neuroblastoma • Oncology • Oral Cancer • Prostate Cancer • Solid Tumor • Squamous Cell Carcinoma

Connexin Regulation and Modulation of Neural Stem Cell Differentiation Induced by Cell-Permeable Itaconate. (PubMed, J Cell Physiol) - "We found that dimethyl itaconate modulates Cxs expression in NSCs, increasing Cx36 levels, and promotes NSCs differentiation toward a neuronal phenotype, while inhibition of Cxs-based channels with carbenoxolone or mefloquine abolishes these dimethyl itaconate-induced effects. Collectively, these findings highlight a regulatory role for cell-permeable itaconate and contribute to the understanding of intercellular communication in the CNS microenvironment, providing insights into potential therapeutic strategies for CNS repair and regeneration."

Journal • Immunology • Inflammation

Drug-associated insomnia: A pharmacovigilance study based on FDA adverse event reporting system. (PubMed, Medicine (Baltimore)) - "The top 3 medications with the highest reporting frequency were mefloquine, viloxazine, and flibanserin. Subgroup analyses revealed distinct drug signal profiles across age groups and genders, with pediatric cases dominated by nervous system and anti-infective agents, adults and the elderly showing additional endocrine or hormonal signals, and sex specific signals such as finasteride in males and flibanserin in females. This pharmacovigilance study identifies insomnia risk signals across multiple drug classes, underscoring the need for clinical vigilance regarding drug-related sleep disturbances. Further prospective research is required to confirm these associations."

Adverse events • Journal • CNS Disorders • Insomnia • Pediatrics • Sleep Disorder

Chloroquine resistance transporter drives divergent multilocus drug resistance genetic backgrounds and susceptibility in Gambian Plasmodium falciparum. (PubMed, J Glob Antimicrob Resist) - "ACTs remain effective in The Gambia, supported by the absence of pfkelch13 mutations. However, reversion to chloroquine sensitivity tend to result in reduced sensitivity to ACT drugs. These genotype-phenotype dynamics needs continuous monitoring to guide drug interventions towards malaria elimination."

Journal • Infectious Disease • Malaria • ABCB1

Spontaneous splenic rupture as a rare complication of Plasmodium vivax: a case report. (PubMed, Pan Afr Med J) - "We report the case of a thirty-year-old Moroccan soldier who presented with fever six months after returning from a deployment in a malaria-endemic country, despite appropriate mefloquine chemoprophylaxis. Malaria due to Plasmodium vivax was confirmed by blood film, and oral treatment (Artemether-Lumefantrine) was initiated...This case illustrates that splenic rupture should be considered in malaria patients with abdominal pain associated with clinical features of hypovolaemia and no history of trauma. It also shows that conservative management can preserve splenic function and lead to a good clinical outcome."

Journal • Infectious Disease • Malaria • Mood Disorders • Pain