Full Press Release Details
VYNE Therapeutics Announces Positive Phase 1a SAD Data
for VYN202, a Novel BD2-Selective BET Inhibitor
BRIDGEWATER, N.J., September 12, 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 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 as follows:
VYN202 Was Generally Well Tolerated Across All Dose Groups
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 Demonstrated 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 proteins1. 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.
"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."
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.
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.
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 ("SEC"), public conference calls,
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 related to VYNE's ability to successfully complete the Phase 1a SAD/MAD trial of VYN202 and to receive
favorable results from such trial, as well as the timing of results from the MAD portion of the trial, the role of trial results in
informing the design of planned studies in psoriasis and rheumatoid arthritis and the potential benefits of VYN202. 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 enroll
patients in its clinical trials and successfully develop its product candidates; 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 SEC. 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 of future events.
LifeSci Advisors, LLC
VYNE Therapeutics Inc.