Mizollen (mizolastine) / Sanofi, Mitsubishi Tanabe - LARVOL DELTA

Discovery of Non-Steroidal Aldo-Keto Reductase 1D1 Inhibitors through Automated Screening and In Vitro Evaluation. (PubMed, Toxicol Lett) - "Other moderate inhibitors included carbamazepine, larotrectinib, endosulfan II, megastigmatrienone A, and mizolastine. The structural diversity of the identified inhibitors demonstrates that the binding site of AKR1D1 is rather promiscuous and can accommodate a broad range of ligands. These findings underscore the importance of toxicity screening and potential to identify structurally different AKR1D1 inhibitors."

Journal • Preclinical • Metabolic Disorders

In silico Evaluation of H1-Antihistamine as Potential Inhibitors of SARS-CoV-2 RNA-dependent RNA Polymerase: Repurposing Study of COVID-19 Therapy. (PubMed, Turk J Pharm Sci) - "These findings suggested that among all the analyzed drugs, bilastine, fexofenadine, montelukast, zafirlukast, mizolastine, and rupatadine might bind with the best binding energy (< -7.0 kcal/mol) and inhibit RdRp, potentially halting the replication of the virus. This study highlights the potential of H1-antihistamines in combating COVID-19 and underscores the value of computational approaches in rapid drug discovery and repurposing efforts. Finally, experimental studies are required to measure the potency of H1-antihistamines before their clinical use against COVID-19 as RdRp inhibitors."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Preclinical and clinical studies on Qin-Zhu-Liang-Xue decoction: insights from network pharmacology and implications for atopic dermatitis treatment. (PubMed, Front Med) - "The trial demonstrated that patients who received QZLX showed considerable improvements in their Scoring Atopic Dermatitis (SCORAD) and Dermatology Life Quality Index (DLQI) scores compared with those who received mizolastine at week 4...A negative correlation was observed between GRα expression and clinical parameters, including SCORAD, DLQI, and serum IgE levels. QZLX alleviates AD symptoms through the upregulation of GRα and thus presents a novel therapeutic strategy for the prevention of glucocorticoid resistance in AD management."

Clinical • Journal • Preclinical • Atopic Dermatitis • Dermatitis • Dermatology • Immunology

Derivatization-free sustainable spectrofluorimetric estimation of antihistamine drug mizolastine in pharmaceutical and biological matrices. (PubMed, Luminescence) - "Such applications underscore the method's potential applicability within quality control laboratories, preventing the need for sample preparation or laborious extraction steps. Finally, the method's sustainability and practicality were confirmed by applying different greenness and whiteness metrics, yielding excellent results."

Journal • Allergic Rhinitis • Dermatology • Immunology • Inflammation • Urticaria

Comparative Safety Profiles of Individual Second-Generation H1-Antihistamines for the Treatment of Chronic Urticaria: A Systematic Review and Network Meta-Analysis of Randomized Controlled Trials. (PubMed, J Allergy Clin Immunol Pract) - "These findings suggest evidence of variations in safety profiles among sgAHs for CU treatment, particularly in terms of adverse events and CNS side effects."

Clinical • Journal • Retrospective data • Review • Dermatology • Immunology • Urticaria

Formulation and Pathohistological Study of Mizolastine-Solid Lipid Nanoparticles-Loaded Ocular Hydrogels. (PubMed, Int J Nanomedicine) - "Moreover, pretreatment with MZL-SLNs-loaded hydrogel imparted markedly decreased TNF-α and VEGF-expression levels in rabbits conjunctivae compared with post-treatment with the same formula. MZL-SLNs could be considered a promising stable sustained-release nanoparticulate system for preparing ocular hydrogel as effective antiallergy ocular delivery systems."

Journal • Conjunctivitis • Immunology • Marginal Zone Lymphoma • Ocular Infections • Ocular Inflammation • Ophthalmology • TNFA

An in-silico evaluation of COVID-19 main protease with clinically approved drugs. (PubMed, J Mol Graph Model) - "Among the eight studied compounds, Lymecycline and Mizolastine appear as potential inhibitors of this protease. Moreover, the ADMET analysis also indicated drug-likeness properties. Thus it is suggested that the identified compounds can inhibit Chymotrypsin-like protease (3CL) of SARS-CoV-2."

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

Cardiac safety of second-generation H -antihistamines when updosed in chronic spontaneous urticaria. (PubMed, Clin Exp Allergy) - "Blockade of these channels causes QT prolongation leading to torsade de pointes that may possibly degenerate into ventricular fibrillation and sudden death. We considered in detail bilastine, cetirizine, levocetirizine, ebastine, fexofenadine, loratadine, desloratadine, mizolastine and rupatadine and conclude that all these drugs have an excellent safety profile with no evidence of cardiotoxicity even when updosed up to four times their standard licensed dose, provided that the prescribers carefully consider and rule out potential risk factors for cardiotoxicity, such as the presence of inherited long QT syndrome, older age, cardiovascular disorders, hypokalemia and hypomagnesemia, or the use of drugs that either have direct QT prolonging effects or inhibit sgAH metabolism."

Clinical • Journal • Cardiovascular • Dermatology • Pruritus • Urticaria

C reactive protein (CRP) rs3093059C predicts poor mizolastine response in chronic spontaneous urticaria patients with elevated serum CRP level. (PubMed, Exp Dermatol) - "Forty (62.50%) CSU patients were effective when treated with mizolastine, and 55 (72.4%) patients were effective in the desloratadine group. From the ?-Hexosaminidase assay, we observed the inhibiting degranulation effects by mizolastine and this effect is weakened when with a higher dose CRP in RBL-2H3 cells. Our findings suggested that CSU patients carrying the rs3093059C allele may respond poorly to mizolastine with elevated serum CRP level."

Clinical • Journal • Cardiovascular • Dermatology • Dermatopathology • Pruritus • Urticaria

Clinical observation on the therapeutic effect of desloratadine citrate disodium in the treatment of chronic urticaria and changes in IL4, IL18, IL23 and IL-33 levels before and after treatment. (PubMed, Pak J Pharm Sci) - "Desloratadine citrate disodium treatment effect of chronic urticaria is better, and after treatment, IL4, IL18, IL23, IL33 levels decreased significantly."

Journal • Dermatology • Dermatopathology • Immunology

Effects of combination of mizolastine and proteoglycan on chronic urticaria: a randomized controlled trial. (PubMed, Arch Dermatol Res) - "Using ELISA, we found that the IFN-γ (37.88 ± 4.27 pg/mL vs. 21.91 ± 4.95 pg/mL, p = 0.028) levels were specifically increased in the experiment group. The combination of mizolastine plus proteoglycan is effective in treating chronic urticaria with better therapeutic effect and lower relapse rate through promoting IFN-γ production."

Clinical • Journal