VYNE Therapeutics Reports Positive Top-line Phase 1a MAD Data for VYN202, its Novel BD2-Selective BET Inhibitor

Core Insights - VYN202 shows promising results as a novel, once-daily oral treatment for various immune-mediated disorders, demonstrating a favorable safety and tolerability profile [1][3] - The Phase 1a trial results indicate robust pharmacodynamic activity, including significant inhibition of inflammatory biomarkers [1][2] Safety and Tolerability - VYN202 exhibited no drug-related adverse events historically associated with earlier generation BET inhibitors, such as thrombocytopenia and gastrointestinal toxicity [2][4] - All treatment-emergent adverse events (TEAEs) were mild or moderate, with no serious adverse events reported [2][3] Pharmacokinetics (PK) - VYN202 supports a once-daily dosing regimen, achieving steady-state after 7 doses [2][4] - Blood levels of VYN202 remained within key inhibitory thresholds for at least 24 hours across all doses [2][4] - No drug-drug interactions were observed when co-administered with methotrexate [2][4] Pharmacodynamics - VYN202 induced a dose-dependent increase in the target engagement biomarker HEXIM-11, with maximal effects at doses of 0.5mg to 1.0mg [2][5] - The drug inhibited multiple inflammatory biomarkers related to Th17 and Th1/myeloid dysregulated activity, consistent with preclinical models [2][6] Development and Future Plans - The positive results from the Phase 1a trial support further development of VYN202 as a treatment option for immune-mediated diseases [3][9] - The company plans to finalize clinical trial plans for VYN202 based on these encouraging results [3][9] About VYN202 - VYN202 is an innovative oral small molecule BET inhibitor designed for enhanced selectivity and potency, particularly for BD2 versus BD1 [6][9] - It aims to provide a differentiated, non-biologic treatment option for chronic inflammatory conditions [6][9]