Migsis (lomerizine) / Merck (MSD), Santen, Pfizer - LARVOL DELTA

Repurposing lomerizine, T-type calcium channel blocker, as a therapeutic strategy for glioblastoma by targeting the IL-6/STAT3 pathway (SNO 2025) - "Based on our data, lomerizine holds potential as a novel GBM therapeutic agent targeting both GICs and differentiated glioma cells."

Brain Cancer • Glioblastoma • Glioma • Solid Tumor • IL6 • STAT3

Repurposing lomerizine, T-type calcium channel blocker, as a therapeutic strategy for glioblastoma by targeting the IL-6/STAT3 pathway (WFNOS 2025) - "Based on our data, lomerizine holds potential as a novel GBM therapeutic agent targeting both GICs and differentiated glioma cells."

Glioblastoma • Oncology • Solid Tumor • IL6 • STAT3

Nutrient-Sensitising Drug Repurposing Screen Identifies Lomerizine As a Mitochondrial Metabolism Inhibitor in Chronic Myeloid Leukaemia (ASH 2023) - "In chronic myeloid leukaemia (CML), the persistence of leukaemic stem cells (LSCs) following first line treatment with tyrosine kinase inhibitors (TKIs) such as imatinib, can lead to disease relapse. In summary, we reveal for the first time that Ca2+ regulation is disrupted in CML stem cells and influx via CACNA1D and TRPC6 is crucial for maintaining high mitochondrial Ca2+ levels and enhanced mitochondrial OXPHOS. This renders CML stem cells sensitive to lomerizine, an FDA-approved Ca2+ inhibitor identified following metabolism-specific drug-repurposing screening."

IO biomarker • Chronic Myeloid Leukemia • CNS Disorders • Hematological Malignancies • Leukemia • Migraine • Oncology • CD34 • TRPC6

Deciphering the rules of disulfidptosis: a genome-wide signature for identifying disulfidptosis-related genes and analyzing hepatocellular carcinoma chemotherapy sensitivities. (PubMed, Free Radic Biol Med) - "Among these, NR-CL was validated as a disulfidptosis desensitizer, while lomerizine and clioquinol were confirmed as sensitizers through gene expression predictive analyses and cellular functional validation. These findings lay a robust foundation for uncovering novel regulatory mechanisms of disulfidptosis and provide practical strategies for enhancing cancer chemotherapy through targeted interventions."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor • NRF1

BIPOLAR PATIENT ON LITHIUM MAINTENANCE THERAPY WITH REVERSIBLE CEREBRAL VASOCONSTRICTION SYNDROME AFTER COVID-19 INFECTION (WCN 2025) - "She was diagnosed with bipolar II disorder and migraine, and taking lithium carbonate 600 mg daily for years...Two months after lomerizine, headache resolved. Zolmitriptan and celecoxib were effective... Headaches should not be overlooked when treating patients with psychiatric disorders, and consultation with a neurologist or headache specialist is necessary."

Clinical • Bipolar Disorder • CNS Disorders • Mental Retardation • Migraine • Psychiatry

Therapeutic effects of lomerizine on vasculopathy in Fabry disease. (PubMed, Sci Rep) - "Furthermore, FD-model mice (Gla-/-/TSP1Tg) treated orally with lomerizine for 6 months showed clear improvement of several FD phenotypes, including left ventricular hypertrophy, renal fibrosis, anhidrosis, and heat intolerance. Thus, our results suggest lomerizine as a novel candidate for FD therapy."

Journal • Fabry Disease • Fibrosis • Genetic Disorders • Immunology • Lysosomal Storage Diseases • Metabolic Disorders • Rare Diseases

Anti-Calcitonin Gene-Related Peptide Monoclonal Antibody Is Effective for Preventing Migraine Aura Without Headache. (PubMed, Neurol Int) - "The use of CGRP mAbs can be considered as a potential treatment in preventing migraine aura without headache. Currently, CGRP mAb is indicated only for migraines with and without auras. Given our findings and the promising effects of this medication for this migraine subtype, a large clinical trial is required to better assess the effects and potential adverse events of CGRP mAb in patients with migraine aura without headache."

Journal • CNS Disorders • Depression • Immunology • Migraine • Pain • Psychiatry

A Case of Migraine Treated Through Hybrid Consultation via In-Person and Online Telemedicine at an Occupational Health Nurse's Office. (PubMed, Cureus) - "He was on prophylactic treatment with 10 mg of lomerizine, experiencing one monthly migraine attack, often relieved by 50 mg of sumatriptan. Performing online telemedicine at the workplace, such as the occupational nurse's office, could overturn the conventional wisdom that occupational physicians cannot perform medical treatment at non-medical institutions and can only refer patients to other clinics based on the Japanese Medical Act. Our case suggested the importance of strategic collaboration between occupational doctors and telemedicine-enabled medical facilities in ensuring seamless healthcare delivery, particularly for busy workers."

Journal • CNS Disorders • Migraine • Pain

Reversible Cerebral Vasoconstriction Syndrome without Headache. (PubMed, J Med Invest) - "Invest. 71 : 323-326, August, 2024."

Journal • Cardiovascular • CNS Disorders • Pain • Vascular Neurology

Study Protocol for LOMCAD Trial: Effect of Lomerizine Hydrochloride to Prevent Recurrence of Cerebral Ischemic Events in CADASIL Patients. (PubMed, J Stroke Cerebrovasc Dis) - "We have planned a clinical trial to verify the effectiveness of lomerizine hydrochloride as prophylaxis to prevent recurrent cerebral ischemic events in CADASIL patients."

Journal • Cardiovascular • CNS Disorders • Ischemic stroke • Migraine • Pain

Effects of Lomerizine and Its Metabolite on Glioblastoma Cells. (PubMed, Anticancer Res) - "Lomerizine has been used for migraine treatment because of its brain-penetrating properties without serious side-effects; thus, it might potentially be expected to be used alone for glioblastoma, including temozolomide-resistant glioblastoma, or in combination with temozolomide."

Journal • Brain Cancer • CNS Disorders • CNS Tumor • Glioblastoma • Migraine • Oncology • Pain • Solid Tumor

Characterizing Lomerizine metabolites in camel urine: High-resolution mass spectrometry method development and validation for enhanced doping control. (PubMed, Rapid Commun Mass Spectrom) - "The developed method enables the detection and characterization of LMZ and its metabolites in camels. The identified metabolites has the potential to act as marker metabolites for the distinctive detection of LMZ in camel urine to ensure efficient analytical strategies for routine doping control applications."

Journal • CNS Disorders • Migraine • Pain

Effectiveness of CGRP monoclonal antibody in preventing migraine aura without headache (AHS 2024) - "Initial treatment with oral migraine preventive medication, lomerizine (a calcium antagonist), showed partial efficacy; however, the aura persisted...Following the initial galcanezumab injection, her photo hypersensitivity and aura ceased... CGRP monoclonal antibody is effective in preventing aura without headache, as demonstrated in this case report."

CNS Disorders • Depression • Migraine • Pain • Psychiatry

Nutrient-sensitizing drug repurposing screen identifies lomerizine as a mitochondrial metabolism inhibitor of chronic myeloid leukemia. (PubMed, Sci Transl Med) - "Through stable isotope-assisted metabolomics and functional assays, we observe that lomerizine treatment inhibits mitochondrial isocitrate dehydrogenase activity and mitochondrial oxidative metabolism and selectively sensitizes CML LSCs to imatinib treatment. In addition, combination treatment with imatinib and lomerizine reduced CML tumor burden, targeted CML LSCs, and extended survival in xenotransplantation model of human CML, suggesting this as a potential therapeutic strategy to prevent disease relapse in patients."

IO biomarker • Journal • Chronic Myeloid Leukemia • CNS Disorders • Hematological Malignancies • Leukemia • Migraine • Oncology • Pain • Transplantation • CD34 • TRPC6

Prognostic significance vestibular examination results in patients with vestibular migraine. (PubMed, Front Neurol) - "Lifestyle modifications for VM and conventional pharmacological prophylactic treatments, including lomerizine, amitriptyline, and valproic acid, were performed. Vestibular examinations, especially o- or c-VEMP, are beneficial for predicting the treatment outcomes of VM. The pathophysiology of VM is closely related to vestibular abnormalities, particularly the otolith-related pathways."

Journal • CNS Disorders • Migraine • Otorhinolaryngology • Pain • Vertigo

Identification of lomerizine as a potential anti-glioblastoma drug (SNO 2023) - "This study suggests that lomerizine has anti- GBM effects."

Brain Cancer • CNS Disorders • CNS Tumor • Glioblastoma • Glioma • Migraine • Oncology • Pain • Solid Tumor • ANXA5 • STAT3

Lomerizine attenuates LPS-induced acute lung injury by inhibiting the macrophage activation through reducing Ca influx. (PubMed, Front Pharmacol) - "And L-type Ca channel agonist Bay K8644 (BK) could restore cytokine generation. In conclusion, our study demonstrated that LMZ alleviates LPS-induced ALI and is a potential agent for treating ALI/ARDS."

Journal • Acute Lung Injury • Acute Respiratory Distress Syndrome • CNS Disorders • Inflammation • Migraine • Oncology • Pain • Pneumonia • Pulmonary Disease • Respiratory Diseases • IL6 • TNFA

Lomerizine inhibits LPS-mediated neuroinflammation and tau hyperphosphorylation by modulating NLRP3, DYRK1A, and GSK3α/β. (PubMed, Front Immunol) - "Finally, lomerizine abolished the LPS-mediated activation of GSK3α/β and upregulation of DYRK1A, which is responsible for tau hyperphosphorylation, in wild-type mice. These data suggest that lomerizine attenuates LPS-mediated neuroinflammatory responses and tau hyperphosphorylation and is a potential drug for neuroinflammation- or tauopathy-associated diseases."

Journal • Alzheimer's Disease • CNS Disorders • Inflammation • Migraine • Pain • DYRK1A • GFAP • NLRP3 • SOD2

Migraine Medication (PubMed, Brain Nerve) - "Furthermore, the development of lomerizine and the approval of valproic acid and propranolol for migraine prophylaxis have greatly improved the treatment of patients with migraines. Monoclonal antibodies targeting CGRP (galcanezumab and fremanezumab) and its receptor (erenumab) have shown consistent efficacy in migraine prophylaxis, with excellent safety profiles. Its effects on refractory cases have also been reported, and a paradigm shift in migraine treatment is emerging."

Journal • CNS Disorders • Migraine • Pain

Design, synthesis and anti-Chikungunya virus activity of lomerizine derivatives. (PubMed, Bioorg Med Chem Lett) - "Molecular docking study was performed to rationalize the SAR and analyze the possible binding modes between B1 and amino acid residues in the active site of nsP3 protein to enhance the understanding of their action as antiviral agents. These finding provides research basis for the design and synthesis of effective anti-CHIKV drugs with Lom as the lead compound."

Journal • Chikungunya • CNS Disorders • Infectious Disease • Migraine • Musculoskeletal Pain

Lomerizine Improved Bath-related Headache Presenting as Reversible Cerebral Vasoconstriction Syndrome. (PubMed, Intern Med) - No abstract available

Journal • Pain

Doping control analysis of trimetazidine in dried blood spot. (PubMed, Drug Test Anal) - "Contrary to urine analysis, the M6 was less detectable in blood. Laboratories should confirm intact lomerizine whenever trimetazidine is identified in DBS."

Journal

Identification of lomerizine, a prophylactic drug for migraines, as a potential anti-glioblastoma drug (SNO 2022) - "Lomerizine has anti-GBM effects."

Brain Cancer • CNS Disorders • Glioblastoma • Migraine • Oncology • Solid Tumor • ANXA5 • STAT3

Lomerizine blocks calcium ion influx to mitochondria and targets CML stem cells through inhibition of mitochondrial metabolism (ESH-CML 2022) - No abstract available

Hemiplegic migraine type 2 with new mutation of the ATP1A2 gene in Japanese cases. (PubMed, Neurosci Res) - "Additionally, oral administration of a combination of lomerizine hydrochloride and topiramate had a partial effect in three cases. We report four missense mutations in ATP1A2. This report will be useful for the future analysis of mutations and clinical types in Asians, as well as Westerners, with migraine."

Journal • CNS Disorders • Migraine • Pain