Topline proof-of-concept data in vitiligo patients expected in 1H 2023

BRIDGEWATER, N.J., Nov. 17, 2022 (GLOBE NEWSWIRE) -- VYNE Therapeutics Inc. (Nasdaq: VYNE) ("VYNE" or the "Company"), a biopharmaceutical company developing proprietary, innovative, and differentiated therapies for the treatment of immuno-inflammatory conditions, today announced that the first subjects have been dosed in a Phase 1a/b clinical trial evaluating VYN201 for the treatment of vitiligo. VYN201 is a locally administered, small molecule, pan-bromodomain and extra-terminal domain (BET) inhibitor that is being developed for the treatment of immuno-inflammatory diseases. The clinical trial is a first-in-human study designed to generate safety and pharmacokinetic data in healthy volunteers as well as provide early clinical proof-of-concept data in vitiligo patients.

"We believe BET inhibitors have the potential to become a major new drug class for the treatment of vitiligo and other immuno-inflammatory diseases," said David Domzalski, President and Chief Executive Officer of VYNE. "The initiation of this clinical trial for VYN201, the first of several planned programs for our InhiBET^TM BET inhibitor platform, is a major milestone in our mission to improve the lives of patients suffering from immuno-inflammatory diseases. We look forward to topline data for both the Phase 1a and Phase 1b portions of the study, expected in the first half of 2023."

The Phase 1 study will be conducted in U.S.-based clinical centers. The Phase 1a portion of the study will evaluate single ascending/multiple ascending doses in up to 30 healthy volunteers with VYN201 applied topically once daily for up to two weeks. The primary objective of this portion of the study is to characterize the preliminary safety and pharmacokinetics of VYN201 and to determine the safe starting dose for the Phase 1b portion of the study.

In the Phase 1b portion, up to 30 patients with a clinical diagnosis of non-segmental vitiligo will receive VYN201 once daily in up to three dose cohorts. Patients will receive treatment for an initial 8-week period based on currently available nonclinical safety data. The Company expects to extend the treatment period for up to an additional 12 weeks, subject to ongoing nonclinical safety assessments. The primary objective of the Phase 1b portion of the study will be to evaluate the safety and pharmacokinetics of VYN201. In addition, exploratory efficacy of VYN201 in non-segmental vitiligo patients will also be assessed. Clinical assessments will include safety, pharmacokinetics, local skin tolerance, efficacy, pharmacodynamic biomarkers and photography.

"By utilizing a soft-drug approach, topical VYN201 is designed to maximize target engagement in the skin and minimize systemic exposure. In an ex vivo human tissue model of vitiligo, VYN201 demonstrated a dose-dependent reduction in the loss of melanin pigment in the basal layers of skin and positively impacted key biomarkers that drive dyspigmentation in vitiligo. Further, VYN201 was found to upregulate the WNT signaling pathway which is an important mediator of both melanogenesis and melanocyte differentiation and is known to be dysregulated in patients with vitiligo," said Dr. Iain Stuart, Chief Scientific Officer of VYNE. "Based upon these data, we believe VYN201 could be a promising and differentiated new therapy to address the unmet needs of patients with vitiligo."

About VYN201 and Vitiligo
VYN201 is a locally-administered pan-bromodomain BET inhibitor, designed as a "soft" drug to address diseases involving multiple, diverse inflammatory cell signaling pathways while providing low systemic exposure. To date, VYN201 has produced consistent reductions in pro-inflammatory and disease-related biomarkers, improvements in disease severity and a demonstrated local activity through several preclinical models. The Company believes that these data suggest potential broad utility for VYN201 across multiple routes of administration. 

Vitiligo is a chronic autoimmune depigmenting disorder of the skin, characterized by the loss of pigment producing cells known as melanocytes. Vitiligo is the most common depigmenting skin condition, with a prevalence estimated at 0.5-2% of the world population.¹ There is currently only one FDA-approved product for the treatment of vitiligo.

About BET Inhibitors
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. BET inhibitors have the potential to treat a range of immuno-inflammatory and fibrotic diseases by blocking pro-inflammatory cytokine transcription with additional potential myeloproliferative neoplastic disorders.

1. Rosmarin et al, Lancet (2020);396:110-120 Bergqvist. Dermatol. 2020;236:571-592

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. The Company's unique and proprietary bromodomain & extra-terminal (BET) domain platform includes lead programs VYN201 (pan-BETi) and VYN202 (selective-BETi), and access to a library of small molecule BET inhibitors for the potential treatment of immuno-inflammatory conditions licensed from Tay Therapeutics Limited.

For more information about VYNE Therapeutics Inc. or its investigational products, visit . 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.

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 timing for the receipt of topline results in VYNE's phase 1 trial of VYN201, VYNE's BET inhibitor platform, 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 non-clinical studies and clinical trials; VYNE's ability to enroll patients and successfully progress, complete, and receive favorable results in, clinical trials for its product candidates; VYNE's ability to exercise its exclusive option with respect to an oral BET inhibitor candidate pursuant to the terms of the option agreement with Tay Therapeutics Limited; VYNE's intentions and its ability to obtain additional funding, either through equity or debt financing transactions or collaboration arrangements; disruptions related to COVID-19 or another pandemic, epidemic or outbreak of a contagious disease, on the ability of VYNE's suppliers to manufacture and provide materials for VYNE's product candidates, initiating and retaining patients in clinical trials, operating results, liquidity and financial condition; the regulatory approval process for VYNE's product candidates, including any delay or failure in obtaining requisite approvals; the potential market size of treatments for any diseases and market adoption of products, if approved or cleared for commercial use, by physicians and patients; developments and projections relating to competitors and the pharmaceuticals industry, including competing drugs and therapies; the timing or likelihood of regulatory filings and approvals or clearances for product candidates; VYNE's ability to comply with various regulations applicable to its business, including Nasdaq continued listing rules; VYNE's ability to create intellectual property and the scope of protection it is able to establish and maintain for intellectual property rights covering its product candidates, including the projected terms of patent protection; 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; the timing, costs or results of litigation, including litigation to protect its intellectual property; VYNE's ability to successfully challenge intellectual property claimed by others; estimates of VYNE's expenses, capital requirements, its needs for additional financing and its ability to obtain additional capital on acceptable terms or at all; VYNE's ability to attract and retain key scientific or management personnel; VYNE's defense of any litigation that may be initiated against it; VYNE's expectations regarding licensing, business transactions and strategic operations; VYNE's future financial performance and liquidity; and volatility in VYNE's stock price may result in rapid and substantial increases or decreases in the stock price that may or may not be related to the company's operating performance or prospects. 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, 2021, 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.

Investor Relations:
John Fraunces
LifeSci Advisors, LLC
917-355-2395
jfraunces@lifesciadvisors.com

Tyler Zeronda
VYNE Therapeutics Inc.
908-458-9106
Tyler.Zeronda@vynetx.com