VYNE Therapeutics Announces Positive Phase 1a SAD Data for VYN202, a Novel BD2-Selective BET Inhibitor

Core Insights - VYNE Therapeutics Inc. announced positive results from the single ascending dose (SAD) portion of its Phase 1a trial for VYN202, a novel BET inhibitor targeting chronic inflammatory and immune-mediated conditions [1][6] Group 1: Trial Results - VYN202 was generally well tolerated across all dose groups, with no serious or drug-related adverse events reported [2] - Pharmacokinetic results showed a dose-dependent increase in plasma and urine concentrations of VYN202 [3] - Pharmacodynamic analysis indicated an increase in the HEXIM1 protein, suggesting effective target engagement, along with a biological activity that inhibited inflammatory biomarkers relevant to psoriasis and rheumatoid arthritis [4] Group 2: Future Developments - The multiple ascending dose (MAD) portion of the trial has commenced, with results anticipated in Q4 2024 [5] - The MAD trial aims to further assess safety, tolerability, pharmacokinetics, and pharmacodynamics over a 14-day period at varying dose levels [5] Group 3: Product Overview - VYN202 is an innovative oral small molecule BET inhibitor with potential class-leading selectivity for BD2 over BD1, aiming to provide a non-biologic treatment option for immuno-inflammatory conditions [7] - The compound is distinct from VYNE's previous pan-BET inhibitor, VYN201, and is protected by unique patent applications [7] Group 4: Industry Context - BET inhibitors are recognized for their role in regulating gene transcription and immune cell activation, presenting opportunities for treating various immuno-inflammatory and fibrotic diseases [8][9]