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First Patients Dosed with VYN202 for Inflammatory Diseases


VYNE Therapeutics Inc. shared that top-line data from the trial is expected in the second half of 2024.

Girl with burst capillaries on face | Image Credit: © Angelina - stock.adobe.com.

Image Credit: © Angelina

VYNE Therapeutics Inc. announced that the first healthy volunteers have been dosed in its phase 1a trial of VYN202, an oral molecule BD2-selective bromodomain and extra-terminal domain (BET) inhibitor that is being developed for the treatment of immuno-inflammatory diseases. They noted that top-line data is expected in the second half of 2024.1

“We are pleased to announce the initiation of the first-in-human clinical trial of VYN202, a highly selective and potent orally administered BET inhibitor. In preclinical testing, VYN202 achieved consistent improvements in disease severity across a variety of inflammatory and fibrotic models as well as reductions in pro-inflammatory and disease-related biomarkers,” said David Domzalski, president and CEO of VYNE. “We believe VYN202 has significant potential as a treatment option for a broad range of immune-mediated diseases, and we look forward to reporting top-line data from the Phase 1a trial in the second half of this year.”

The phase 1a trial is a first-in-human double-blind, placebo-controlled study, according to a press release from VYNE, that consists of single ascending dose (SAD) and multiple ascending dose (MAD) components. The company said the trial is currently expected to consist of roughly 64 healthy adult subjects, split into 5 SAD and 3 MAD cohorts to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of VYN202.

“Early generation BET inhibitors show similar affinity to both BD1 and BD2 bromodomains of BET proteins that has been implicated in both gastrointestinal and hematologic dose limiting toxicities,” said Iain Stuart, PhD, chief scientific officer of VYNE, in the release. “We believe VYN202’s high potency and selectivity towards the BD2 bromodomain of BET proteins may result in an improved benefit-risk profile when treating immuno-inflammatory diseases. Following highly encouraging preclinical data, we are eager to evaluate the clinical safety, tolerability, pharmacokinetics and pharmacodynamics of VYN202 to further inform our future clinical development plans.”

According to VYNE, if the phase 1a trial is successfully completed, VYNE will initiate phase 1b trials in patients with moderate to severe plaque psoriasis and moderate to severe adult-onset rheumatoid arthritis, with top-line results expected in the second half of 2025.2,3

“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,” VYNE wrote in a previous news release.3

The company also recently announced the initiation of the phase 2b trial of the BET inhibitor VYN201 for vitiligo. They anticipate releasing top-line data from the study’s 24-week treatment period by mid-2025.

“The vast majority of drugs that are currently in development for vitiligo are JAK inhibitors and come along with all the associated safety precautions that come along with that class of molecule. There's a tremendous unmet need in vitiligo in general, and within the therapeutic space, there'sbasically no differentiation. We really think that there's a space here for VYN201,” Stuart told Dermatology Times in a recent interview. “We think the potential for BET inhibition could be very broad, and not just in vitiligo, but into all the dermatologic and immunologic diseases. The very fact that we have shown the very first clinical dataset in an autoimmune disease, and it happened to be vitiligo, was particularly encouraging."5


  1. VYNE therapeutics announces dosing of first participants in phase 1a trial of novel BD2-selective BET inhibitor VYN202. News release. VYNE Therapeutics. June 13, 2024. Accessed June 13, 2024. https://vynetherapeutics.com/press-releases/vyne-therapeutics-announces-dosing-of-first-participants-in-phase-1a-trial-of-novel-bd2-selective-bet-inhibitor-vyn202/ 
  2. VYNE reports first quarter 2024 financial results and provides business update. News release. GlobeNewswire. May 9, 2024. Accessed June 13, 2024. https://www.globenewswire.com/news-release/2024/05/09/2878712/0/en/VYNE-Reports-First-Quarter-2024-Financial-Results-and-Provides-Business-Update.html
  3. VYNE Therapeutics announces FDA clearance of IND application for VYN202, a novel BD2-selective BET inhibitor. News release. VYNE Therapeutics. May 6, 2024. Accessed June 13, 2024. https://vynetherapeutics.com/press-releases/vyne-therapeutics-announces-fda-clearance-of-ind-application-for-vyn202-a-novel-bd2-selective-bet-inhibitor/ 
  4. VYNE therapeutics announces dosing of first subject in phase 2b vitiligo trial of novel BET inhibitor VYN201. News release. VYNE Therapeutics. June 5, 2024. Accessed June 13, 2024. https://vynetherapeutics.com/press-releases/vyne-therapeutics-announces-dosing-of-first-subject-in-phase-2b-vitiligo-trial-of-novel-bet-inhibitor-vyn201/ 
  5. Andrus E, Stuart I. VYN201 for vitiligo: promising data showcases potential of BET inhibition. Dermatology Times. May 22, 2024. Accessed June 13, 2024. https://www.dermatologytimes.com/view/vyn201-for-vitiligo-promising-data-showcases-potential-of-bet-inhibition 
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