VYNE Therapeutics Inc. announced the clearance of its Investigational New Drug application (?IND?) by the U.S. Food and Drug Administration for VYN202, an oral BD2-selective BET inhibitor. VYNE plans to initiate a first-in-human Phase 1a single ascending dose/multiple ascending dose (?SAD/MAD?) trial in healthy volunteers this quarter and expects to report top line results from the SAD/MAD trial in the second half of this year. The VYN202 Phase 1a trial is a double-blind, placebo-controlled study in healthy volunteers and consists of SAD and MAD components.

The study is expected to enroll approximately 64 healthy adult subjects into five SAD and three MAD cohorts to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of VYN202. If the Phase 1a portion of the trial is successfully completed, VYNE plans to initiate Phase 1b trials in subjects with moderate-to-severe plaque psoriasis and moderate-to-severe adult-onset rheumatoid arthritis, with top line results anticipated in the second half of 2025. About VYN202: VYN202 is an innovative, oral small molecule BD2-selective BET inhibitor that has been designed to achieve class-leading selectivity (BD2 vs.

BD1), maximum potency versus BD2 and optimal oral bioavailability. By maximizing BD2 selectivity, VYNE believes VYN202 has the potential to be a more conveniently administered non-biologic treatment option for both acute control and chronic management of immuno-inflammatory indications, in which the damaging effects of unrestricted inflammatory signaling activity is common. VYN202 is structurally distinct from VYNE?s pan-BET inhibitor (VYN201) and covered by distinct PCT and provisional composition of matter patent applications directed to new chemical entities and their uses.

BET proteins play a key role in regulating gene transcription via epigenetic interactions (?reading?), and recent research has identified a key role for these proteins in regulating B cell and T cell activation and subsequent inflammatory processes. As epigenetic readers, BET proteins regulate the recruitment of transcriptional factors that are key to the production of several pro-inflammatory cytokines. BET inhibitors have the potential to treat a range of immuno-inflammatory and fibrotic diseases by blocking pro-inflammatory cytokine transcription with additional potential in myeloproliferative neoplastic disorders.