VYNE Begins Phase 1a Trial Dosing of BET Inhibitor VYN202

VYNE Therapeutics Inc. has embarked on a significant milestone with the dosing of the first healthy volunteers in their Phase 1a clinical trial of VYN202. This trial will assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of VYN202, an orally administered BD2-selective bromodomain and extra-terminal domain (BET) inhibitor. This promising development in the field of immuno-inflammatory disease treatment has garnered considerable attention, with top-line data anticipated in the latter half of 2024.

David Domzalski, President and CEO of VYNE, expressed his enthusiasm about the commencement of the first-in-human trial of VYN202. He emphasized the potential of VYN202 as a treatment option for a wide array of immune-mediated diseases, citing its consistent performance in preclinical tests. These tests have shown VYN202's ability to reduce disease severity and lower levels of pro-inflammatory biomarkers across various models of inflammation and fibrosis.

The Phase 1a trial is a double-blind, placebo-controlled study that will enroll around 64 healthy adults. These individuals will be divided into five single ascending dose (SAD) cohorts and three multiple ascending dose (MAD) cohorts. The primary goal of the study is to evaluate the safety and tolerability of VYN202, along with its pharmacokinetic and pharmacodynamic profiles.

Dr. Iain Stuart, Chief Scientific Officer at VYNE, noted the limitations of early generation BET inhibitors, which tend to show similar affinities for both BD1 and BD2 bromodomains. This lack of selectivity has led to gastrointestinal and hematologic toxicities. In contrast, VYN202 has been designed to achieve high selectivity and potency specifically for the BD2 bromodomain, which may lead to a better therapeutic profile for treating immuno-inflammatory diseases. Dr. Stuart highlighted the encouraging preclinical data and expressed eagerness to further evaluate VYN202's clinical potential.

VYN202 stands out due to its innovative design and optimal oral bioavailability. It is distinct from VYNE's other pan-BET inhibitor, VYN201. VYN202's selective targeting of BD2 over BD1 is intended to offer a non-biologic treatment option that can be conveniently administered both for acute control and chronic management of conditions characterized by excessive inflammatory signaling.

BET proteins, which include BD1 and BD2 bromodomains, play a crucial role in regulating gene transcription through epigenetic mechanisms. These proteins are instrumental in B cell and T cell activation, which are essential components of the inflammatory response. BET inhibitors like VYN202 have the potential to mitigate a variety of immuno-inflammatory and fibrotic diseases by blocking the transcription of pro-inflammatory cytokines. This approach also holds promise for treating myeloproliferative neoplastic disorders.

VYNE Therapeutics Inc. is dedicated to enhancing patient lives by developing proprietary therapies for immuno-inflammatory diseases. Their InhiBET™ platform includes both VYN201 and VYN202, licensed from Tay Therapeutics Limited. The company continues to innovate in the field, focusing on creating differentiated treatments that address significant unmet medical needs.

With the launch of this Phase 1a trial, VYNE Therapeutics is taking a significant step toward potentially offering a groundbreaking treatment for a range of immune-mediated conditions. The results of this trial are eagerly awaited, as they will provide critical insights into the future clinical development of VYN202.