PH46A / Trino Therapeutics - LARVOL DELTA

Bioactive Indanes: Design, synthesis and bioactivity investigation of 2,2-substituted Indane derivatives, a new bioactive Indane scaffold. (PubMed, Bioorg Chem) - "Our group developed a series of 1,2-indane dimers, including PH46A (9), for inflammatory and autoimmune diseases...In lipoxygenase (LOX) assays, 18a, 18d, and 18c exhibited significant 5-LOX inhibition, with 18d comparable to zileuton...Subsequent to molecular docking, molecular docking simulations predicted stable binding of 18c and 18d to 5-LOX under mimicked physiological conditions. These findings offer insights into indane-based therapeutic drug development for IBD, highlighting cost reductions by minimising stereochemistry complexity."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • CXCL8 • IFNG • IL1B • IL6 • TNFA

Bioactive indanes: insight into the bioactivity of indane dimers related to the lead anti-inflammatory molecule PH46A. (PubMed, J Pharm Pharmacol) - "The observed profile of cytokine modulation (IL-6/ TNF-α, IL-8) and inhibition of release of NO and 5-LOX may contribute to the in vivo effects demonstrated by indane dimers and PH46A (1) in murine models of colitis."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • CXCL8 • IFNG • IL1B • IL6 • TNFA

Bioactive indanes: Development and validation of an LC-MS/MS bioanalytical method for the determination of PH46A, a new potential anti-inflammatory agent, in dog and rat plasma and its application to a pharmacokinetic study in dog. (PubMed, J Pharm Biomed Anal) - "The highest C was observed in animal 003 M. The rapid absorption and high plasma concentration observed for animal 003 M compared to the data for animals 001 M and 002 M may account for the sickness observed in this animal; however, the reasons for this have not been investigated."

Journal • PK/PD data • Preclinical • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease