VYNE Therapeutics Reports Positive Phase 1a Data for VYN202, a New BD2-Selective BET Inhibitor

VYNE Therapeutics Inc., a clinical-stage biopharmaceutical company, has released promising data from the single ascending dose (SAD) portion of its ongoing Phase 1a trial of VYN202. VYN202 is an innovative, oral small molecule BET inhibitor aiming to treat chronic inflammatory and immune-mediated conditions. The Phase 1a trial, which is double-blind and placebo-controlled, aims to evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics of VYN202. This study includes both SAD and multiple ascending dose (MAD) components.

The results from the SAD portion showed that VYN202 was generally well tolerated across all dose groups, with no serious or drug-related adverse events. Clinical laboratory results and electrocardiogram findings did not reveal any significant abnormalities. The pharmacokinetic analysis indicated a dose-dependent increase in plasma and urine concentrations of the drug, suggesting that VYN202 met expected PK parameters.

Furthermore, pharmacodynamic data showed that blood samples from participants demonstrated target engagement and biological activity on inflammatory biomarkers. Specifically, the increase in the marker protein HEXIM1 indicated effective target engagement of VYN202 with BET proteins. Exploratory data also revealed that VYN202 had an inhibitory effect on certain inflammatory biomarkers relevant to conditions such as psoriasis and rheumatoid arthritis.

The MAD portion of the trial has commenced, focusing on assessing the safety, tolerability, PK, and pharmacodynamics of VYN202 over a 14-day period at different dose levels. Results from this phase are anticipated in the fourth quarter of 2024.

David Domzalski, President and CEO of VYNE, emphasized that the results from the SAD trial represent a significant milestone for the company and the development of its BET inhibitor platform. The next steps involve further evaluating VYN202’s safety and PK profiles, along with its potential to impact relevant biomarkers following multiple doses. These insights will guide the design of future studies targeting psoriasis and rheumatoid arthritis.

VYN202 is distinguished by its high selectivity and potency for BD2 over BD1, which VYNE believes could make it a more convenient, non-biologic treatment option for managing immuno-inflammatory conditions. The drug is structurally different from VYNE’s pan-BET inhibitor VYN201 and has distinct patent applications covering new chemical entities and their uses.

BET inhibitors function by regulating gene transcription through epigenetic interactions, particularly in immune cell activation and inflammatory processes. These inhibitors can potentially treat various immuno-inflammatory and fibrotic diseases by blocking the transcription of pro-inflammatory cytokines, and they also show promise in managing myeloproliferative neoplastic disorders.

VYNE Therapeutics Inc. is committed to developing innovative therapies to address unmet needs in chronic inflammatory and immune-mediated conditions. The company’s proprietary BET inhibitors, part of its InhiBET™ platform, aim to improve upon the limitations of early-generation BET inhibitors through enhanced selectivity and alternative routes of administration.