Full Press Release Details
Reports Positive Top-line Phase 1a MAD Data for VYN202, its Novel BD2-Selective BET Inhibitor
BRIDGEWATER, NJ, December 23, 2024 -- VYNE Therapeutics
Inc. (Nasdaq: VYNE) ("VYNE" or the "Company"), a clinical-stage biopharmaceutical company focused on developing
differentiated therapies to treat chronic inflammatory and immune-mediated conditions with high unmet need, today announced positive results
from the multiple ascending dose ("MAD") portion of its Phase 1a SAD/MAD trial of VYN202. The Phase 1a trial was a two-part,
double-blind, placebo-controlled dose-escalation study in healthy volunteers consisting of single ascending dose ("SAD") and
MAD components to evaluate the safety, tolerability, pharmacokinetics ("PK") and pharmacodynamics of VYN202.
Key Findings from the Top-line Phase 1a MAD
"We are very excited by the PK, pharmacodynamic
and safety data generated in this trial which not only support the further development of VYN202 but also give us increased confidence
that VYN202 has the potential to become a novel treatment option for immune-mediated diseases," said David Domzalski, President
and Chief Executive Officer of VYNE. "VYN202 has been designed to address the adverse events that have been historically associated
with early generation BET inhibitors. We believe the data from this Phase 1a SAD/MAD trial validates our drug design thesis for VYN202.
Based on these positive results, we look forward to finalizing our clinical trial plans for VYN202 in patients over a longer duration
For more information on the Phase 1a trial
results, please visit the investor section of VYNE's website.
About the MAD Portion of the Phase 1a Trial
The MAD portion of the trial was designed to evaluate
multiple ascending doses of VYN202 given to healthy volunteers for 14 days. Four study cohorts evaluated VYN202 dosed at 0.5mg QOD, 0.5mg
QD, 1mg QD and 1mg QD in combination with methotrexate 7.5mg QWK. The 0.5mg QOD cohort was intended to approximate 0.25mg QD dosing and
the methotrexate combination cohort evaluated potential drug-drug interactions with methotrexate, a treatment commonly used in the management
of chronic inflammatory conditions.
The trial evaluated safety, tolerability, PK and
exploratory pharmacodynamics of VYN202. Participant blood samples were stimulated ex-vivo to assess the pharmacodynamic impact of VYN202
on target engagement and inflammatory biomarkers.
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 differentiated, 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.
About BET Inhibitors
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.
1 Lin, Xiaoyu et al. "HEXIM1
as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues."
Molecular Cancer Therapeutics vol. 16,2 (2017): 388-396. doi:10.1158/1535-7163.MCT-16-0475.
About VYNE Therapeutics Inc.
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.
For more information about VYNE Therapeutics
Inc. or its product candidates, visit www.vynetherapeutics.com. VYNE may use its website to comply with its disclosure obligations
under Regulation FD. Therefore, investors should monitor VYNE's website in addition to following its press releases, filings with
the U.S. Securities and Exchange Commission, public conference calls, and webcasts.
LifeSci Advisors, LLC
VYNE Therapeutics Inc.
Cautionary Statement Regarding Forward-Looking Statements
This release includes forward-looking statements
within the meaning of the Private Securities Litigation Reform Act of 1995, including, but not limited to, statements regarding the clinical
development of VYNE's product candidates, including VYN202, the potential benefits of VYNE's product candidates, including
VYN202, and other statements regarding the future expectations, plans and prospects of VYNE. All statements in this press release which
are not historical facts are forward-looking statements. Any forward-looking statements are based on VYNE's current knowledge and
its present beliefs and expectations regarding possible future events and are subject to risks, uncertainties and assumptions that could
cause actual results to differ materially and adversely from those set forth or implied by such forward-looking statements. These risks
and uncertainties include, but are not limited to: VYNE's ability to successfully develop its product candidates; the timing of
commencement of future preclinical studies and clinical trials; VYNE's ability to complete and receive favorable results
from clinical trials of its product candidates; VYNE's ability to obtain additional funding, either through equity or debt financing
transactions or collaboration arrangements; and VYNE's ability to comply with various regulations applicable to its business. For
a discussion of other risks and uncertainties, and other important factors, any of which could cause VYNE's actual results to differ
from those contained in the forward-looking statements, see the section titled "Risk Factors" in VYNE's Annual Report
on Form 10-K for the year ended December 31, 2023, and VYNE's other filings from time to time with the U.S. Securities and Exchange
Commission. Although VYNE believes these forward-looking statements are reasonable, they speak only as of the date of this announcement
and VYNE undertakes no obligation to update publicly such forward-looking statements to reflect subsequent events or circumstances, except
as otherwise required by law. Given these risks and uncertainties, you should not rely upon forward-looking statements as predictions
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