HGR4113 / Glaceum - LARVOL DELTA

Therapeutic effects of a synthetic glabridin derivative on metabolic immuno-regulation and salivary gland functional restoration in experimental Sjögren's syndrome. (PubMed, Exp Mol Med) - "Finally, treatment with HGR4113 promoted the development of 3D salivary epithelial structures in vitro. HGR4113 improves salivary gland hypofunction by inhibiting lymphocyte infiltration and inflammation in the salivary glands and restoring damaged salivary tissue in SS-like NOD/ShiLtJ mice."

Journal • Cardiovascular • Conjunctivitis • Dental Disorders • Dry Eye Disease • Genetic Disorders • Immunology • Inflammation • Metabolic Disorders • Obesity • Ocular Infections • Ocular Inflammation • Ophthalmology • Sjogren's Syndrome • Xerostomia • CD4 • CDH1 • IL10 • IL17A • LEP • STAT3

A Study to Investigate the Safety, Tolerability, Pharmacokinetic/Pharmacodynamic Characteristics and Food Effect of HGR4113 in Healthy Subjects (clinicaltrials.gov) - P1 | N=40 | Recruiting | Sponsor: Glaceum | Trial completion date: Jun 2024 ➔ Jan 2025

Trial completion date • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Synthetic Glabridin Derivatives Improves Sjogren’s Syndrome by Inducing Salivary Secretion and Salivary Gland Regeneration (ACR Convergence 2023) - "These results show that HGR4113 can improve salivary gland hypofunction by inhibiting lymphocyte infiltration and inflammation in the salivary gland and restoring the damaged salivary gland in SS-Like NOD mice. HGR4113 attenuates the severity of SS in NOD/ShiLtJ mice Treatment with HGR4113 promotes the generation of salivary gland organoids in vitro Treatment with HGR4113 regulates the frequency of inflammatory cells in humans"

Genetic Disorders • Immunology • Inflammation • Obesity • Sjogren's Syndrome • CDH1 • IL17A

Preclinical Bioavailability Assessment of a Poorly Water-Soluble Drug, HGR4113, Using a Stable Isotope Tracer. (PubMed, Pharmaceutics) - "By eliminating the differences in clearance between intravenous and oral dosages at different levels, acquired data showed that the current method reduced measurement errors in bioavailability when compared to the conventional approach. The present study suggests a prominent method for evaluating the bioavailability of drugs with poor aqueous solubility in preclinical studies."

Journal • Preclinical

Synthetic Glabridin Derivatives Inhibit LPS-Induced Inflammation via MAPKs and NF-κB Pathways in RAW264.7 Macrophages. (PubMed, Molecules) - "In the previous study, we synthesized glabridin derivatives-HSG4112, (S)-HSG4112, and HGR4113-based on the structure-activity relationship study of glabridin to improve its biological efficacy and chemical stability. In addition, the compounds increased the expression of antioxidant protein heme oxygenase (HO-1) by inducing nuclear translocation of nuclear factor erythroid 2-related factor 2 (Nrf2) through ERK and p38 MAPKs. Taken together, these results indicate that the synthetic glabridin derivatives exert strong anti-inflammatory effects in LPS-stimulated macrophages through MAPKs and NF-κB pathways, and support their development as potential therapeutics against inflammatory diseases."

Journal • Inflammation • Oncology • IL1B • IL6 • NF-κβ • PTGS2 • TNFA

A Study to Investigate the Safety, Tolerability, Pharmacokinetic/Pharmacodynamic Characteristics and Food Effect of HGR4113 in Healthy Subjects (clinicaltrials.gov) - P1 | N=48 | Recruiting | Sponsor: Glaceum

New P1 trial • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • PON1