ebastine / Generic mfg. - LARVOL DELTA

Bactericidal and anti-biofilm activity of ebastine against Staphylococcus aureus. (PubMed, Lett Appl Microbiol) - "Furthermore, safety evaluations showed that ebastine exhibited limited toxicity to mammalian cells, with negligible hemolytic effects and good overall safety profiles. This study provided new insights into the potential applications of ebastine in the field of antimicrobial therapy, highlighting its promise as a non-traditional antibacterial agent."

Journal • Infectious Disease

Development and Optimization of Oral Dissolution Films for Enhanced Delivery of Ebastine-Loaded Solid Lipid Nanoparticles. (PubMed, Int J Nanomedicine) - "The developed system demonstrates enhanced solubility, stability, and bioavailability of ebastine, offering a promising alternative to traditional oral tablets, with potential advantages in patient compliance and rapid drug onset. Therefore, the ODFs containing SLNs can be considered as an efficient approach for EBT administration."

Journal • Allergy • Immunology

EBASTINE INTERRUPTS THE HISTAMINERGIC-NEUROTROPHIN LOOP TO INHIBIT PANCREATIC CANCER PROGRESSION AND MODULATE THE IMMUNE MICROENVIRONMENT UNDER CHRONIC STRESS CONDITIONS (DDW 2025) - No abstract available

Oncology • Pancreatic Cancer • Solid Tumor

5310: Pancreatitis and Pancreatic Cancer: Inflammation, Fibrogenesis and Immunology (DDW 2025) - "Description: This session will explore the complex interplay between inflammation, fibrogenesis, and immunology in the context of pancreatitis and pancreatic cancer. Presentations will cover topics such as the role of TLR2 in acute pancreatitis, the impact of ebastine on pancreatic cancer progression, and the mechanisms driving immune evasion in pancreatic ductal adenocarcinoma.Learning Objectives:• Describe the Role of Inflammation in Pancreatitis and Pancreatic Cancer• Explore Mechanisms of Immune Evasion and Tumor Progression• Discuss Diagnostic and Therapeutic Approaches"

Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Pancreatitis • Solid Tumor • TLR2

Ebastine in combination with low-dose antidepressants for refractory irritable bowel syndrome: A randomized controlled trial. (PubMed, Technol Health Care) - "They were administered with ebastine (Group A) or ebastine combined with flupentixol and melitracen (Group B) for 4 weeks. After treatment, the serum levels of D-LAC and I-FABP were significantly lower in Group B than in Group A.ConclusionRefractory IBS patients showed certain psychological abnormalities. Ebastine combined with antidepressants exhibited more obvious benefits on QOL, sleep quality, and SSS, with significant improvements in psychological status and intestinal permeability in refractory IBS patients."

Journal • CNS Disorders • Depression • Gastrointestinal Disorder • Mood Disorders • Psychiatry

Identification of effective synthetic molecules against viral-induced cytokine release syndrome using in silico and in vitro approaches. (PubMed, Mol Divers) - "Six potential 3-CLpro inhibitors were identified by molecular docking using MOE software, including ebastine (1), orlistat (2), atracurium besylate (3), piperaquine phosphate (4), valsartan (5), and acarbose (6), among which 1-3 binds strongly to the target protein with binding affinity of - 8.22, - 9.12, and - 7.81, kcal/mol, respectively. This study demonstrates the potential of pre-existing drugs to ameliorate the cytokine storm and oxidative damage with simultaneous anti-viral effects. The data provide pre-clinical support to develop these drugs as potential therapeutic agent against ARDS."

Journal • Preclinical • Acute Respiratory Distress Syndrome • Infectious Disease • Inflammation • Novel Coronavirus Disease • Pneumonia • Pulmonary Disease • Respiratory Diseases • CSF2 • IFNG • IL1B • IL2 • IL6 • TNFA

Two Cases of Acquired Reactive Perforating Collagenosis in Hemodialysis Patients. (PubMed, Semin Dial) - "Two patients were treated with oral thalidomide and ebastine, local application of fluticasone propionate cream, and enhanced dialysis. We report for the first time that ARPC in patients with hemodialysis could be improved by oral thalidomide and antihistamines and local application of steroid. This report provides reference for guiding the understanding of ARPC and the new treatment of ARPC in hemodialysis patients."

Journal • Cardiovascular • Chronic Kidney Disease • Dermatology • Diabetes • Endocrine Disorders • Hypertension • Metabolic Disorders • Renal Disease • Type 2 Diabetes Mellitus

Ebastine-mediated destabilization of E3 ligase MKRN1 protects against metabolic dysfunction-associated steatohepatitis. (PubMed, Cell Mol Life Sci) - "This enhances AMPK stability and activity, suppressing lipid accumulation, inflammation, and fibrosis. Moreover, the knockout of Mkrn1 mice decreased the risk of MASH, suggesting that ebastine could be a promising therapeutic agent for the treatment of MASH."

Journal • Fibrosis • Genetic Disorders • Hepatocellular Cancer • Hepatology • Immunology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Metabolic Dysfunction-Associated Steatotic Liver Disease • Obesity • Oncology • Solid Tumor • Targeted Protein Degradation

S6K1 is a Targetable Vulnerability in Tumors Exhibiting Plasticity and Therapy Resistance. (PubMed, Int J Biol Sci) - " We identified a novel derivative of the antihistamine drug ebastine, designated Super-ebastine (Super-EBS), that inhibited the viability of cancer cells representing diverse KRAS and EGFR driver mutations and models of plasticity and treatment resistance...The essential role of S6K1 in the action of Super-EBS was recapitulated in xenografts, and knockout of S6K1 abrogated tumor growth in mice. S6K1 is a therapeutic vulnerability in tumors exhibiting intrinsic and/or acquired resistance to treatment."

Journal • Oncology • CDC42 • EGFR • KRAS • RPS6KB1

Prednisolone versus antihistamine for allergic rhinitis: No significant difference found in randomized trial. (PubMed, Clin Transl Allergy) - "Prednisolone tablets did not show superior efficacy over antihistamine tablets in reducing symptoms or medication usage in tree pollen-induced AR. These results suggest that systemic corticosteroids may not provide additional benefits over antihistamines, and clinicians should prioritize individualized treatment based on patient preferences and tolerability."

Journal • Allergic Rhinitis • Immunology • Inflammation

Exploring α-Lipoic Acid Based Thermoplastic Silicone Adhesive: Towards Sustainable and Green Recycling. (PubMed, Polymers (Basel)) - "The shear strength of the LASA90 presented strong adhesion (up to 88 kPa) on various substrates including steel, aluminum, PET, and PTFE...The rheology, TG-DTA, DSC, and 1H NMR showed that the degradation of the LASA occurred at 150 °C via the retro-ROP of the five-membered disulfide ring, indicating their recyclability after usage. Conclusively, we envision that a silicone adhesive based on α-lipoic acid as a natural linker is more sustainable than conventional silicone thermosets because of its desired properties, strong adhesion, reversibility, and on-demand heat degradation."

Journal

Ebastine Interrupts the Histaminergic Neurons-Pancreatic Cancer Communication Loop to Inhibit Pancreatic Cancer Progression Under Chronic Stress Conditions (APA-JPS-CAP-IAP 2024) - No abstract available

Hepatology • Oncology • Pancreatic Cancer • Solid Tumor

Analyzing the clinical efficacy and safety of levocetirizine based on its receptor occupancy, intraclass comparison and role in the treatment of CSU: an AROG consensus statement. (PubMed, Expert Rev Clin Pharmacol) - "The marked receptor occupancy translates to better efficacy as compared to similarly dosed SGAH and the lower cost of the molecule makes it an appropriate drug for chronic use. Receptor occupancy should serve as the basis of intra-class head-to-head trials for CSU."

Journal • Review • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

Ebastine Versus Mebeverine in IBS Patients (clinicaltrials.gov) - P3 | N=200 | Recruiting | Sponsor: Guy Boeckxstaens | Trial completion date: Jan 2027 ➔ Jan 2028 | Trial primary completion date: Oct 2026 ➔ Oct 2027

Trial completion date • Trial primary completion date • Gastrointestinal Disorder

Acidic sphingomyelinase interactions with lysosomal membranes and cation amphiphilic drugs: A molecular dynamics investigation. (PubMed, Comput Struct Biotechnol J) - "Our study, leveraging all-atom explicit solvent molecular dynamics simulations, delves into the interaction of glycosylated ASM with the lysosomal membrane and the effects of CAD representatives, i.e., ebastine, hydroxyebastine and loratadine, on the membrane and ASM. CADs also interfere with the association of ASM with the membrane at the level of a loop in the catalytic domain engaging in membrane interactions. Our computational approach, applicable to various CADs or membrane compositions, provides insights into ASM and CAD interaction with the membrane, offering a valuable tool for future studies."

Journal • Oncology

Cost-effectiveness Analysis of Second-Generation Antihistamine 1 Receptor Blockers and Japanese Kampo Shoseiryuto for Treating Perennial Allergic Rhinitis in Outpatient Settings in Japan. (PubMed, Hosp Pharm) - " The most cost- and clinically effective SGAs were determined from a list of 6 SGAs (bepotastine, 10 mg; cetirizine, 10 mg; ebastine, 10 mg; epinastine, 20 mg; loratadine, 10 mg; and olopatadine, 5 mg) together with shoseiryuto, using the overall improvement rate through a model-based analysis. Ebastine (10 mg) was the most cost-effective treatment strategy for PAR among the agents evaluated in this study. This insight could aid in establishing an appropriate formulary for treating PAR in hospitals and communities."

Cost effectiveness • HEOR • Journal • Allergic Rhinitis • Immunology • Inflammation

Cytochrome P450 and UDP-glucuronosyltransferase expressions, activities, and induction abilities in 3D-cultured human renal proximal tubule epithelial cells. (PubMed, Drug Metab Dispos) - "Midazolam 1'-hydroxylation, trifluoperazine N-glucuronidation, serotonin O-glucuronidation, propofol O-glucuronidation, and morphine 3-glucuronidation in the 3D-RPTEC were significantly higher than the 2D-RPTEC and comparable to those in the HepaRG cells, although bupropion, ebastine, and calcitriol hydroxylations were not different between the 2D- and 3D-RPTEC. The results were comparable to that in the human kidney cortex. 3D-RPTEC are useful for evaluating the induction of kidney P450s, UGTs, and human renal drug metabolism in cellulo."

Journal • CYP1A1 • CYP1B1 • CYP2E1 • CYP3A4 • CYP3A5 • UGT1A1 • UGT1A4 • UGT1A6 • UGT1A9

TREATMENT WITH THE HISTAMINE 1 RECEPTOR ANTAGONIST EBASTINE FOR NON-CONSTIPATED IRRITABLE BOWEL SYNDROME: A DOUBLE-BLIND, RANDOMIZED, PLACEBO-CONTROLLED TRIAL (DDW 2024) - "Stool consistency did not significantly differ between placebo (n=68) and ebastine (n=64) in IBS-D patients. Conclusions Our study shows that a 12-week treatment with 20 mg ebastine is superior to placebo and should be further evaluated as novel treatment for non-constipated IBS."

Clinical • Constipation • Gastrointestinal Disorder • Pain

Mast cell degranulation-triggered by SARS-CoV-2 induces tracheal-bronchial epithelial inflammation and injury. (PubMed, Virol Sin) - "Taken together, our findings confirm the essential role of MC degranulation in SARS-CoV-2-induced hyper-inflammation and the subsequent tissue lesions. Furthermore, our results support the use of ebastine or loratadine to inhibit SARS-CoV-2-triggered degranulation, thereby preventing tissue damage caused by hyper-inflammation."

Journal • Infectious Disease • Inflammation • Novel Coronavirus Disease • Respiratory Diseases

Efficacy of mast cell directed therapies in irritable bowel syndrome: a systematic review. (PubMed, Acta Gastroenterol Belg) - "This limited evidence suggests a significant overall improvement in the key symptoms after treatment with disodium cromoglycate, ebastine, ketotifen or palmitoylethanolamide-polydatin compared to control groups. Mast cell modulating therapies could be of significant value in therapy for IBS patients. Further high-quality research is needed to establish the therapeutic efficacy of mast cell targeted therapies in order to draw robust conclusions and improve the clinical management of irritable bowel syndrome."

Journal • Review • Gastrointestinal Disorder • Pain

3D-QSAR pharmacophore modeling, virtual screening, molecular docking, MD simulations, in vitro and in vivo studies to identify potential anti-hyperplasia drugs. (PubMed, Biotechnol J) - "Based on MD simulations results, the best two hit molecules, that is, ebastine (Ebs) and mebeverine (Mbv) were selected for in vitro and in vivo antioxidant studies performed in mice. TNF-α and COX pro-inflammatory mediators, biochemical assays, histopathological analyses, and immunohistochemistry observations confirmed the anti-inflammatory response of the selected drugs. Based on these findings, it appeared that Ebs can effectively treat psoriasis-like skin lesions and down-regulate inflammatory responses which was consistent with docking predictions and could potentially be employed for further research on inflammation-related skin illnesses such as psoriasis."

Journal • Preclinical • Dermatitis • Dermatology • Immunology • Inflammation • Psoriasis • TNFA

Drugs of the future for diarrhea-predominant irritable bowel syndrome: an overview of current investigational drugs. (PubMed, Expert Opin Investig Drugs) - "Clinical trial evidence has shown that loperamide, eluxadoline, alosetron, ramosetron, bile acid sequestrants, and rifaximin can modulate GI alterations and benefit patients with IBS-D. Among the potential therapies, ibodutant, ibudilast, blautix, BOS-589, solabegron, vibegron, olorinab, ebastine, and ORP-101 have demonstrated possible effects but remain confirmed...Therefore, we should focus on developing new, efficient, and affordable medications for IBS-D. The government, insurers, and society must recognize this need and collaborate to ensure its fulfillment."

Journal • Review • Gastrointestinal Disorder • Inflammation

Ebastine for the treatment of irritable bowel syndrome: old drug, new tricks? (PubMed, Gut) - No abstract available

Journal • Gastrointestinal Disorder

Treatment of non-constipated irritable bowel syndrome with the histamine 1 receptor antagonist ebastine: a randomised, double-blind, placebo-controlled trial. (PubMed, Gut) - P2, P4 | "Our study shows that ebastine is superior to placebo and should be further evaluated as novel treatment for patients with non-constipated IBS."

Journal • Constipation • Gastrointestinal Disorder • Immunology • Pain

Hypersensitivity reaction to nedaplatin: A case report and literature review. (PubMed, Medicine (Baltimore)) - "Clinical use of nedaplatin should be monitored and managed intensively for prevention and treatment of hypersensitivity reactions. Care should be taken to control the titration rate during infusion while closely monitoring vital signs. Clinical staff should be prepared to treat allergic symptoms as soon as they appear. The acute phase should involve immediate discontinuation of the drug; intravenous saline infusion for volume expansion; rapid assessment of circulation, airway, respiration, state of consciousness, and skin condition; and administration of oxygen, antihistamines, and epinephrine as appropriate for anaphylaxis. More randomized clinical trials are needed to elucidate appropriate preventative and management strategies to improve patient safety and support their successful completion of clinical treatment programs."

Clinical • Journal • Review • Allergy • Immunology • Lung Cancer • Oncology • Pulmonary Disease • Solid Tumor • Squamous Cell Carcinoma