Alomide (lodoxamide tromethamine) / Novartis - LARVOL DELTA

Discovery of Potential Tyrosinase Inhibitors via Machine Learning and Molecular Docking with Experimental Validation of Activity and Skin Permeation. (PubMed, ACS Omega) - "We identified three top-ranking inhibitors, rhodanine-3-propionic acid, lodoxamide, and cytidine 5'-(dihydrogen phosphate), with strong binding affinities mediated by metal ion coordination and π-π interactions at the enzyme's active site. In vitro assays revealed that all three compounds exhibited higher inhibitory activity against mushroom tyrosinase compared to arbutin (IC50 = 38.37 mM), with rhodanine-3-propionic acid displaying the most potent inhibition (IC50 = 0.7349 mM). Furthermore, transdermal permeation experimental results confirmed that these compounds achieved markedly better skin permeability than commercial arbutin-based formulations, highlighting their potential as next-generation agents for inhibiting melanin production in cosmetic applications."

Journal • Tyrosinase

The effect of corticotropin-release hormone on duodenal permeability and immune activation in healthy volunteers in a double-blind placebo-controlled study. (PubMed, Am J Physiol Gastrointest Liver Physiol) - "In addition, CRH was administrated ex-vivo to baseline biopsies pretreated with or without lodoxamide... In-vivo CRH administration reduced tryptase levels in supernatant of duodenal biopsies without affecting permeability, whereas ex-vivo duodenal permeability increased regardless of mast51 cell stabilization. These results suggest the involvement of mast-cells in regulating gut permeability in HVs in response to CRH, possibly influenced by in-vivo compensatory mechanisms."

Journal • CNS Disorders • Dyspepsia • Gastrointestinal Disorder • Inflammation

Treatment of allergic rhinitis and allergic conjunctivitis. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Allergic Rhinitis • Allergy • Conjunctivitis • Immunology • Inflammation • Ocular Infections • Ocular Inflammation • Ophthalmology

Discovery of a novel GPR35 agonist with high and equipotent species potency for oral treatment of IBD. (PubMed, Bioorg Med Chem) - "In this study, structural modifications to lodoxamide provides a series of high and equivalent agonists on human, mouse, and rat GPR35...Oral administration of compound 4b at 20 mg/kg alleviates clinical symptoms of DSS-induced IBD in mice, and is slightly more effective than 5-ASA at 200 mg/kg. In summary, it can serve as a new start point for exploiting more potent GPR35 agonists without species differences for the treatment of IBD, and warrants further study."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease

Insights into divalent cation regulation and G-coupling of orphan receptor GPR35. (PubMed, Cell Discov) - "Here we report a cryo-electron microscopy structure of G-coupled GPR35 bound to an anti-allergic drug, lodoxamide...A featured 'methionine pocket' contributes to the G coupling by GPR35. Together, our findings provide a structural basis for divalent cation modulation, ligand recognition, and subsequent G protein coupling of GPR35 and offer a new opportunity for designing GPR35-targeted drugs for the treatment of IBDs."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease

THE EFFECT OF CORTICOTROPIN-RELEASE HORMONE ON DUODENAL PERMEABILITY IN HEALTHY VOLUNTEERS (UEGW 2022) - " Acutely administered CRH in vivo did not induce anxiety or increase duodenal permeability in healthy subjects. However, ex-vivo administered CRH increased TEER while lodoxamide, decreased paracellular permeability of duodenal biopsies."

Clinical • Dyspepsia • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Mood Disorders • Mucositis • Psychiatry

Autonomic nervous system receptor-mediated regulation of mast cell degranulation modulates the inflammation after corneal epithelial abrasion. (PubMed, Exp Eye Res) - "Inhibition of MC degranulation by the MC stabilizers cromolyn sodium and lodoxamide tromethamine increased the infiltration of neutrophils and delayed healing of abraded corneas...We conclude that normal degranulation of MCs in the corneal limbus and crosstalk between the ANS and MCs are crucial for the appropriate control of inflammation and the repair progress of wounded corneas. This suggests a potential approach for improving defective corneal wound healing by the administration of clinically available autonomic activity-modulating agents."

Journal • Corneal Abrasion • Immunology • Inflammation • Ocular Inflammation

Lack of effect of intravenous corticotropin-release hormone on anxiety scores and duodenal permeability in healthy subjects. (BWG 2022) - "In addition, during a separate baseline endoscopy, CRH was administrated ex vivo at the serosal compartment of the Ussing chambers with or without pretreatment with lodoxamide as a mast cell blocker...Conclusions Acutely administered CRH in vivo did not induce acute anxiety and did not increase duodenal permeability in healthy subjects. However, a trend towards higher permeability was observed after ex vivo exposure of the biopsies to CRH."

Clinical • Dyspepsia • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Mood Disorders • Mucositis • Psychiatry

Candidates for Repurposing as Anti-Virulence Agents Based on the Structural Profile Analysis of Microbial Collagenase Inhibitors. (PubMed, Pharmaceutics) - "A total of 100 compounds were identified as potential BC inhibitors, of which, 10 are human approved drugs. Benzthiazide, entacapone, and lodoxamide were chosen as the best candidates for in vitro testing based on their pharmaco-toxicological profile."

Journal

Drugs for allergic rhinitis and allergic conjunctivitis. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Allergic Rhinitis • Allergy • Conjunctivitis • Immunology • Ocular Infections • Ocular Inflammation • Ophthalmology

"I have the same case, and I want to combine Rituximab and Lenalomide. Is it feasible for a 80 yrs ils patient?" (@smbenlazar)

Clinical

"CD20-. I want to intoduce Lenalomide After neuropathy resolution ( with PN monitoring)." (@smbenlazar)

Pain • CD20

Protective effect of lodoxamide on hepatic steatosis through GPR35. (PubMed, Cell Signal) - "Lodoxamide suppressed high fat diet-induced fatty liver development, which suggested the protective function of GPR35 in liver steatosis. Therefore, the present data suggest that GPR35 may function to protect against fatty liver development."

Journal

Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35? (PubMed, Biomol Ther (Seoul)) - "However, a transforming growth factor α (TGF-α) shedding assay revealed lodoxamide not to be a potent agonist of mouse GPR35 in vitro. Therefore, these results showed anti-fibrotic effects of lodoxamide in mice and raise concerns how lodoxamide protects against liver fibrosis in vivo and whether GPR35 is involved in the action."

Journal • Preclinical