- |||||||||| Tavegil (clemastine) / GSK
Journal: Clemastine Inhibits the Biofilm and Hemolytic of Staphylococcus aureus through the GdpP Protein. (Pubmed Central) - Apr 30, 2022
In this study, clemastine, which is a histamine receptor H1 (HRH1) antagonist, was found to have a novel role of the significant inhibition against the biofilm formation and hemolytic activity of S. aureus and enhanced antibacterial activity against S. aureus when used in combination with oxacillin by targeting the GdpP protein. The discovery of this study identified novel use and mechanism of action of clemastine as a potential anti-biofilm drug for clinical application for S. aureus infectious.
- |||||||||| opicinumab (BIIB033) / Biogen, Tavegil (clemastine) / GSK
Retrospective data, Review, Journal: Optic neuritis: aetiopathogenesis, diagnosis, prognosis and management (Pubmed Central) - Apr 5, 2022
Plasmapheresis has also been shown to be effective in patients with ON. In this review we will address basic aspects of the management of ON, in the fundamental context of MS, NMOSD and MOGAD, with emphasis on etiopathogenic, diagnostic, prognostic and therapeutic developments.
- |||||||||| Tavegil (clemastine) / GSK
Journal: Clemastine Induces an Impairment in Developmental Myelination. (Pubmed Central) - Apr 5, 2022
Altogether, these data suggest that clemastine impact on myelin development is more complex than previously thought and could be dependent on microglia-oligodendrocyte crosstalk. Further studies are needed to clarify the role of microglia cells on developmental myelination.
- |||||||||| Alesion (epinastine) / Boehringer Ingelheim
Clinical, Review, Journal: Antihistamine use during breastfeeding with focus on breast milk transfer and safety in humans - a systematic literature review. (Pubmed Central) - Mar 17, 2022
In addition, one study investigated the impact of chlorpheniramine or promethazine on prolactin levels among 17 women, and one study investigated possible adverse drug reactions in 85 breastfed infants exposed to various antihistamines...Most product labels of the ten antihistamines with available information in both EU and the US, reported lack of evidence and recommended to avoid use during breastfeeding. The knowledge gap on antihistamines and lactation is extensive, and further human studies are warranted to ensure optimal treatment of breastfeeding women with allergy.
- |||||||||| Tavegil (clemastine) / GSK
Journal: N-3 PUFA deficiency disrupts oligodendrocyte maturation and myelin integrity during brain development. (Pubmed Central) - Mar 11, 2022
Promoting developmental myelination with clemastine, a first-generation histamine antagonist and enhancer of oligodendrocyte precursor cell differentiation, rescues memory deficits in n-3 PUFA deficient animals. Our findings identify a novel mechanism through which n-3 PUFA deficiency alters brain functions by disrupting oligodendrocyte maturation and brain myelination during the neurodevelopmental period.
- |||||||||| Tavegil (clemastine) / GSK
Journal: Clemastine Rescues Chemotherapy-Induced Cognitive Impairment by Improving White Matter Integrity. (Pubmed Central) - Mar 3, 2022
We concluded that clemastine rescues cognitive function damage caused by chemotherapy through improving white matter integrity. Remyelination, oligodendrocyte differentiation and the increase of neurofilament protein promoted by clemastine are potential strategies for reversing the cognitive dysfunction caused by chemotherapy.
- |||||||||| Tavegil (clemastine) / GSK
Review, Journal: White matter alterations in Williams syndrome related to behavioral and motor impairments. (Pubmed Central) - Feb 3, 2022
We discuss fundamental aspects of WM in WS and how its alterations can affect motor abilities and social behavior. Overall, findings regarding changes in myelin genes and alterations in WM structure in WS suggest new targets for drug therapy aimed at improving conduction properties and altering brain-activity synchronization in this disorder.
- |||||||||| memantine / Generic mfg.
Retrospective data, Journal: Neuroprotective Effects of Novel Treatments on Acute Optic Neuritis-A Meta-Analysis. (Pubmed Central) - Jan 26, 2022
Larger randomized controlled trials with suitable outcome measures are warranted to evaluate the neuroprotective effects of novel treatments. Further studies should also tailor therapies to specific patient populations and investigate a more targeted treatment for acute optic neuritis.
- |||||||||| memantine / Generic mfg.
Journal: A chemical genomics-aggrephagy integrated method studying functional analysis of autophagy inducers. (Pubmed Central) - Jan 18, 2022
These results, with the combined approach, suggested that autophagy-activating small molecules may improve proteinopathies by eliminating nonfunctional protein aggregates. ADK: adenosine kinase; AMPK: AMP-activated protein kinase; ATF4: activating transcription factor 4; BECN1: beclin-1; DDIT3/CHOP: DNA damage inducible transcript 3; EIF2AK3/PERK: eukaryotic translation initiation factor 2 alpha kinase 3; EIF2S1/eIF2α: eukaryotic translation initiation factor 2 subunit alpha; ER: endoplasmic reticulum; ERN1/IRE1α: endoplasmic reticulum to nucleus signaling 1; FDA: Food and Drug Administration; GSH: glutathione; HD: Huntington disease; HSPA5/GRP78: heat shock protein family A (Hsp70) member 5; HTT: huntingtin; JAK: Janus kinase, MAP1LC3B/LC3: microtubule associated protein 1 light chain 3 beta; MAP2K/MEK: mitogen-activated protein kinase kinase; MAP3K8/Tpl2: mitogen-activated protein kinase kinase kinase 8; MAPK: mitogen-activated protein kinase; MPP: 1-methyl-4-phenylpyridinium; MTOR: mechanistic target of rapamycin kinase; MTORC: MTOR complex; NAC: N-acetylcysteine; NGF: nerve growth factor 2; NMDA: N-methyl-D-aspartate; PCA: principal component analysis; PD: Parkinson disease; PDA: pancreatic ductal adenocarcinoma; PIK3C3: phosphatidylinositol 3-kinase catalytic subunit type 3; PMA: phorbol 12-myristate 13-acetate; PRKC/PKC: protein kinase C; ROCK: Rho-associated coiled-coil protein kinase; RR: ribonucleotide reductase; SIGMAR1: sigma non-opioid intracellular receptor 1; SQSTM1/p62: sequestosome 1; STK11/LKB1: serine/threonine kinase 11; TFEB: Transcription factor EB; TGFB/TGF-β: Transforming growth factor beta; ULK1: unc-51 like autophagy activating kinase 1; XBP1: X-box binding protein 1.
- |||||||||| dexamethasone / Generic mfg., paclitaxel / Generic mfg.
Journal: The added value of H antagonists in premedication regimens during paclitaxel treatment. (Pubmed Central) - Dec 17, 2021
Thermodynamic parameters like heats of reaction, sublimation and solvation of clemastine fumarate were calculated and reported. As the upper boundary of the 90% CI does not exceed the predefined non-inferiority margin of +6%, it can be concluded that a premedication regimen without ranitidine is non-inferior to a premedication regimen with ranitidine.
- |||||||||| ketamine / Generic mfg.
Outpatient surgery is not always smooth: a case of anaphylaxis. (Channel 1 - ePosters [VIRTUAL]) - Oct 31, 2021 - Abstract #Euroanaesthesia2021Euroanaesthesia_595;
Anesthesia was induced with infusion of remifentanil (0.01 mcg/kg/min) and propofol (6 mg/kg/h)...Immediate therapy was started with rocuronium (70mg IV), adrenaline (1mg IM + 1mg IV), ketamine (100mg IV), magnesium sulfate (2g IV), clemastine (2g IV) and hydrocortisone (200mg IV)...The fact that tryptase levels remain normal may be a factor against anaphylaxis although tryptase level does not always rise (2). In this case, it will be important to clarify differential diagnoses of anaphylaxis, airway manipulation and hereditary and acquired angioedema.
- |||||||||| tamoxifen / Generic mfg.
Preclinical, Journal: Chronic Exposure to Hypoxia Inhibits Myelinogenesis and Causes Motor Coordination Deficits in Adult Mice. (Pubmed Central) - Oct 8, 2021
To understand whether enhancing myelination could protect brain functions against hypoxia, we treated hypoxic mice with the myelination-enhancing drug-clemastine, which resulted in enhanced myelogenesis and improved motor coordination. Taken together, our data indicate that chronic hypoxia inhibits myelinogenesis and causes functional deficits in the brain and that enhancing myelinogenesis protects brain functions against hypoxia-related deficits.
- |||||||||| Tavegil (clemastine) / GSK
Preclinical, Journal: Clemastine Ameliorates Perioperative Neurocognitive Disorder in Aged Mice Caused by Anesthesia and Surgery. (Pubmed Central) - Sep 10, 2021
At the same time, the expression of post-synaptic density protein 95 (PSD95, or DLG4), brain-derived neurotrophic factor (BDNF), synaptosomal-associated protein 25 (SNAP25) and neuronal nuclei (NEUN) were also improved. Our results suggested that clemastine might be a therapy for PND caused by anesthetic and surgical factors in aged patients.
- |||||||||| Tavegil (clemastine) / GSK
Preclinical, Journal: Enhancing myelin renewal reverses cognitive dysfunction in a murine model of Alzheimer's disease. (Pubmed Central) - Aug 11, 2021
Genetically or pharmacologically enhancing myelin renewal, by oligodendroglial deletion of the muscarinic M1 receptor or systemic administration of the pro-myelinating drug clemastine, improved the performance of APP/PS1 mice in memory-related tasks and increased hippocampal sharp wave ripples. Taken together, these results demonstrate the potential of enhancing myelination as a therapeutic strategy to alleviate AD-related cognitive impairment.
- |||||||||| Bosulif (bosutinib) / Pfizer, Tavegil (clemastine) / GSK
Journal: Identification of SARS-CoV-2 entry inhibitors among already approved drugs. (Pubmed Central) - Jul 28, 2021
Three of the drugs were classified as histamine receptor antagonists with clemastine showing the strongest anti-SARS2 activity (EC = 0.95 ± 0.83 µM). Our work suggests that these 7 drugs could enter into further in vivo studies and clinical investigations for COVID-19 treatment.
- |||||||||| cetirizine oral / Generic mfg., loratadine / Generic mfg., desloratadine / Generic mfg.
Journal: Desloratadine and loratadine stand out among common H-antihistamines for association with improved breast cancer survival. (Pubmed Central) - Jun 22, 2021
Based on their safety and current use within the patient population, together with our observations, we suggest the initiation of trials of desloratadine and loratadine as treatment of breast cancer as well as studies of the mechanism behind their possible effect. Further studies on any effects of other H-antihistamines may also be merited, as well as of H-antihistamine use and survival in other malignancies.
- |||||||||| Tavegil (clemastine) / GSK
Preclinical, Journal: Social defeat stress in adolescent mice induces depressive-like behaviors with reduced oligodendrogenesis. (Pubmed Central) - May 15, 2021
To assess whether decreased oligodendrogenesis caused by social defeat stress is related to depressive-like symptoms under stress, clemastine, a drug that induces OL generation, was administered to socially defeated adolescent mice, resulting in the rescue of the behavioral abnormalities accompanied by increased oligodendrogenesis. These findings suggest that oligodendrogenesis in adverse environments during adolescence plays a role in psychiatric disorders, and clemastine may provide a potential therapeutic drug for adolescent mental disorders, targeting OLs.
- |||||||||| clemastine / Generic mfg.
Trial completion date, Trial primary completion date: Assessment of Clemastine Fumarate as a Remyelinating Agent in Acute Optic Neuritis (ReCOVER) (clinicaltrials.gov) - Apr 22, 2021
P2, N=90, Recruiting,
These findings suggest that oligodendrogenesis in adverse environments during adolescence plays a role in psychiatric disorders, and clemastine may provide a potential therapeutic drug for adolescent mental disorders, targeting OLs. Trial completion date: Jan 2022 --> Aug 2022 | Trial primary completion date: Aug 2021 --> Aug 2022
- |||||||||| cetirizine oral / Generic mfg., loratadine / Sedico, Remedica, Generic mfg., Merck (MSD), Bayer, desloratadine / Kaken, Incepta, Merck (MSD), Generic mfg.
Journal, Adverse events: Association of H1-antihistamines with Torsade de Pointes: a pharmacovigilance study of the Food and Drug Administration Adverse Event Reporting System. (Pubmed Central) - Apr 10, 2021
P
Conclusions Our study found the increased torsadogenic potential of new signals compared with previously known old signals, hence necessitating clinical studies to determine the actual torsadogenic potential of newly identified signals. Clinical Trial Registration This study is registered at ClinicalTrials.gov (NCT.gov ID: NCT04293432.
- |||||||||| loratadine / Sedico, Remedica, Generic mfg., Merck (MSD), Bayer, desloratadine / Kaken, Incepta, Merck (MSD), Generic mfg.
Clinical, Journal: Improved survival in several cancers with use of H-antihistamines desloratadine and loratadine. (Pubmed Central) - Feb 9, 2021
Our hypothesis is that our findings result from immune checkpoint inhibition, and we believe both desloratadine and loratadine should be tested in randomized clinical trials as treatment of immunogenic tumors, with priority given to trials of desloratadine as treatment of tumors with few therapy options and dismal prognoses, such as pancreatic cancer. If our results can be confirmed in a clinical setting, new, potentially curative, therapies could result for several tumors, including ones with dire prognoses and limited treatment options.
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