Full Press Release Details
Lead BET Inhibitor, VYN201, Significantly Reduces
Expression of Several Key Pro-Inflammatory Cytokines in Preclinical Studies
N.J., October 26, 2021 -- VYNE Therapeutics Inc. (Nasdaq: VYNE) ("VYNE" or the "Company") today
announced preclinical data showing that its pan-bromodomain and extra-terminal ("BET") inhibitor, VYN201, significantly reduced
the expression of several key pro-inflammatory cytokines relevant to Th17-mediated autoimmune diseases in an animal model and an ex vivo
human tissue study. The pathogenesis of many autoimmune diseases is linked to the proliferation and activity of Th17 cells, which include
several diseases that VYNE is evaluating for its VYN201 program.
"We are encouraged by the evolving therapeutic profile of our
lead topical BET inhibitor, VYN201," said David Domzalski, VYNE's Chief Executive Officer. "In collaboration with our
newly formed scientific advisory board, we look forward to presenting additional VYN201 data as we continue to advance this promising
and highly differentiated product candidate across our immuno-inflammatory development programs."
As announced in August 2021, VYNE is focusing its R&D capabilities
to advance its proprietary pipeline, featuring the BET inhibitor compounds recently licensed from In4Derm Limited. VYN201 is a first-in-class
topical "soft" pan-bromodomain BET inhibitor that is designed to control multiple pro-inflammatory pathways while mitigating
systemic drug exposure. VYN201 is being developed for topical applications, potentially including rare neutrophilic dermatoses.
Preclinical Model of Th17 Inflammation
VYNE's proprietary formulation of VYN201 was evaluated in a well-established
preclinical model in which dorsal depilated mice are topically dosed with imiquimod cream to induce a Th17 inflammation pathology over
a 7-day induction phase. A further 7-day treatment phase evaluated three doses of VYN201 (0.001%, 0.01% and 0.1% concentrations) compared
to a class 1 super-potent glucocorticosteroid product positive control (clobetasol propionate 0.05% cream) and vehicle control. Further,
an imiquimod-naive control group (healthy control group) was included for VYN201 vehicle treatment.
Key findings from the study:
Ex-vivo Anti-inflammatory Effect on Human Skin Tissue Compared
to Ruxolitinib (JAK1/2 Inhibitor)
An ex vivo human skin tissue study was also conducted. Human skin biopsy
tissue was stimulated to induce a Th17 immuno-phenotype using a method derived from Feghali-Bostwick et al.1 In the study,
the release of several key pro-inflammatory cytokines were substantially reduced when Th17-stimulated human skin tissue was treated with
VYN201, resulting in greater than 95% inhibition of IL-17, IL-36 and CXCL10 release relative to vehicle control. VYN201 also demonstrated
a superior anti-inflammatory effect on these cytokines when compared to the JAK1/2 inhibitor, ruxolitinib, at identical concentrations.
About Bromodomain and Extra-Terminal Domain
BET proteins play a key role in regulating
gene transcription via epigenetic interactions ("reading"), and recent research has determined a key role for these BET proteins
in regulating B cell and T cell activation and subsequent inflammatory processes. As epigenetic readers, BET proteins regulate the recruitment
of transcriptional factors that are key to the production of several pro-inflammatory cytokines. Inhibiting BET proteins blocks cytokine
transcription and therefore may have significant therapeutic potential across a wide variety of immuno-inflammatory/fibrotic and myeloproliferative
neoplastic disorders. A topically applied BET inhibitor product has the possibility to positively impact diseases involving multiple,
diverse inflammatory cell signaling pathways that are active in rare neutrophilic dermatoses. Furthermore, bromodomain 2 selective oral
BET inhibitors may present as more conveniently-administered non-biologic treatment options for both acute control and chronic management
of immuno-inflammatory indications, where the damaging effects of unrestricted inflammatory signaling activity is common.
About VYNE Therapeutics Inc.
VYNE's mission is to improve the lives of patients by developing
proprietary, innovative, and differentiated therapies for the treatment of immuno-inflammatory conditions. VYNE is working to develop
and commercialize a variety of therapies for major immuno-inflammatory conditions and rare skin diseases with high unmet medical need.
The Company's unique and proprietary pipeline includes FMX114 for the treatment of mild-to-moderate atopic dermatitis and access
to a library of bromodomain & extra-terminal (BET) domain inhibitors in both topical and oral forms for the treatment of major
immuno-inflammatory conditions and rare skin diseases.
more information about VYNE Therapeutics Inc. or its investigational products, visit www.vynetherapeutics.com or follow
VYNE on Twitter. 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.
Statement Regarding Forward-Looking Statements
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 development of VYNE's product candidate, VYN201, 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: the outcome and cost of preclinical and clinical trials for current and future
product candidates; determination by the FDA that results from VYNE's preclinical and clinical trials are not sufficient to
support registration or marketing approval of product candidates; adverse events associated with the development of VYN201 or
VYNE's approved products; the COVID-19 pandemic and its impact on our business operations and liquidity including our ability
to progress a preclinical or clinical trial; the potential patient base and commercial potential of VYN201 or any of VYNE's
other product candidates; risks of potential litigation by third-parties regarding infringement of third-party intellectual
property; risks that VYNE's intellectual property rights, such as patents, may fail to provide adequate protection, may be
challenged and one or more claims may be revoked or interpreted narrowly or will not be infringed; risks that any of VYNE's
patents may be held to be narrowed, invalid or unenforceable or one or more of VYNE's patent applications may not be granted
and potential competitors may also seek to design around VYNE's granted patents or patent applications; additional competition
in the markets in which we compete; inability to raise additional capital on favorable terms or at all;
VYNE's ability to recruit and retain key employees; and VYNE's ability to stay in compliance with applicable laws,
rules and regulations. 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, 2020, as well as discussions of
potential risks, uncertainties, and other important factors in VYNE's subsequent filings 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 of future events.