VYNE Therapeutics Reports Positive Phase 1a SAD Data for VYN202
VYNE Therapeutics reports positive phase 1a SAD data for VYN202, a novel BD2-selective BET inhibitor
Overview
VYNE Therapeutics Inc., a clinical-stage biopharmaceutical company, announced positive data from the single ascending dose (SAD) portion of its ongoing phase 1a trial of VYN202. The phase 1a trial is a two-part, double-blind, placebo-controlled dose-escalation study in healthy volunteers consisting of SAD and multiple ascending dose (MAD) components to evaluate the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics of VYN202.
Findings from the SAD Portion of The Phase 1a Trial to Date are:
VYN202 Dose Tolerance
- Single ascending doses of VYN202 across all cohorts were generally well tolerated up to and including the highest planned dose level.
- There were no serious adverse events, drug-related adverse events, or clinically significant abnormalities in clinical laboratory results or electrocardiogram findings.
VYN202 Demonstrated Dose-Dependent PK:
VYN202 also met expected PK parameters, with plasma and urine drug concentrations of VYN202 increasing in a dose-dependent manner across all doses tested.
VYN202 Demonstrat ed Pharmacodynamic Effects:
- Participant blood samples were stimulated ex-vivo to assess the pharmacodynamic impact of single doses of VYN202 on key target-engagement and inflammatory biomarkers.
- Results demonstrated an increase in marker protein HEXIM1, indicative of target engagement of VYN202 with BET proteins.
- Additionally, exploratory data from the SAD arm showed that single doses of VYN202 demonstrated biological activity and an inhibitory effect on select inflammatory biomarkers relevant to psoriasis and rheumatoid arthritis.
Phase 1a MAD Portion of Trial Initiated:
The primary objectives of the MAD portion of the phase 1a trial are to assess safety, tolerability, PK and pharmacodynamics of VYN202 over 14 days at different dose levels. Results are expected in Q4 2024.
Statement from CEO: VYNE
- These results from our SAD trial mark the first clinical data for our BD2-selective BET inhibitor, VYN202, and represent an important milestone for our company and the development of our BET inhibitor platform,” said David Domzalski, president and chief executive officer of VYNE.
- We look forward to further assessing safety and PK as well as VYN202’s potential to impact several relevant biomarkers following multiple doses, which we expect to disclose next quarter. These data would inform the design of our planned studies in psoriasis and rheumatoid arthritis.
About VYN202
- VYN202 is an innovative, oral small molecule BET inhibitor that has potential class-leading selectivity and potency for BD2 vs. BD1.
- 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 Patent Cooperation Treaty and provisional composition of matter patent applications directed to new chemical entities and their uses.
BET Proteins
- BET proteins play a key role in regulating gene transcription via epigenetic interactions (reading).
- Recent research has identified a key role for these proteins in regulating activation of immune cells, including T and B cells, and subsequent inflammatory and fibrotic 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.
About VYNE
- VYNE is a clinical-stage biopharmaceutical company focused on developing differentiated therapies to treat chronic inflammatory and immune-mediated conditions with high unmet need.
- VYNE’s unique and proprietary BET inhibitors, which comprise its InhiBET platform, are designed to overcome limitations of early generation BET inhibitors by leveraging alternative routes of administration and enhanced selectivity.
