FDA Clears VYNE's IND Application for BD2-Selective BET Inhibitor VYN202

VYNE Therapeutics Inc. has announced that the U.S. Food and Drug Administration (FDA) has cleared its Investigational New Drug (IND) application for VYN202, an oral BD2-selective BET inhibitor. VYNE, a clinical-stage biopharmaceutical company, focuses on developing innovative therapies for immuno-inflammatory conditions. The company plans to initiate a Phase 1a single ascending dose/multiple ascending dose (SAD/MAD) trial in healthy volunteers this quarter, with top-line results expected in the latter half of this year.

David Domzalski, President and CEO of VYNE, emphasized the significance of the IND clearance for VYN202, describing it as a highly selective and potent orally administered BET inhibitor with promising potential for treating autoimmune diseases. The Phase 1a trial aims to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of VYN202.

The Phase 1a trial is designed as a double-blind, placebo-controlled study involving approximately 64 healthy adult participants. The trial will include five SAD cohorts and three MAD cohorts to thoroughly assess the drug's effects. Upon successful completion of the Phase 1a trial, VYNE plans to proceed with Phase 1b trials involving subjects with moderate-to-severe plaque psoriasis and moderate-to-severe adult-onset rheumatoid arthritis. Results from these trials are anticipated in the second half of 2025.

VYN202 is a novel oral small molecule BD2-selective BET inhibitor, designed to achieve high selectivity for BD2 over BD1, maximum potency against BD2, and optimal oral bioavailability. This selectivity is expected to offer a more convenient non-biologic treatment option for both acute control and chronic management of immuno-inflammatory conditions, where unchecked inflammatory signaling is prevalent. Unlike VYNE's pan-BET inhibitor (VYN201), VYN202 is structurally unique and protected by distinct patent applications.

BET proteins are crucial in regulating gene transcription through epigenetic interactions, and recent studies have highlighted their role in B cell and T cell activation, which drives inflammatory processes. By inhibiting BET proteins, it is possible to block the transcription of pro-inflammatory cytokines, offering therapeutic potential for various immuno-inflammatory and fibrotic diseases, as well as myeloproliferative neoplastic disorders.

VYNE’s mission is to enhance patient lives by developing proprietary, innovative, and differentiated therapies for treating immuno-inflammatory conditions. The company’s InhiBET™ platform includes both a locally administered pan-BD BET inhibitor (VYN201) and the orally available BD2-selective BET inhibitor (VYN202), licensed from Tay Therapeutics Limited.

VYNE Therapeutics Inc. continues to focus on groundbreaking treatments to address immuno-inflammatory conditions, reinforcing its commitment to improving patient outcomes through scientific innovation and targeted therapies.