VYNE Therapeutics Initiates Phase 1b Trial of VYN202, a Novel BD2-Selective Oral BET Inhibitor, in Plaque Psoriasis
VYNE Therapeutics has initiated a Phase 1b trial for VYN202, its oral BD2-selective BET inhibitor, in patients with moderate-to-severe plaque psoriasis. The trial will evaluate once-daily doses over 12 weeks, focusing primarily on safety assessment, with secondary objectives including pharmacokinetic profile and efficacy measurements through PASI scores.
The company expects to report top-line data from this randomized, placebo-controlled trial by year-end 2025. Previous Phase 1a single ascending dose (SAD) and multiple ascending dose (MAD) trials demonstrated VYN202's favorable safety profile and ability to inhibit multiple inflammatory biomarkers related to Th17, TNF and Th1/myeloid dysregulated activity.
This trial aims to provide insights into VYN202's potential application across various chronic immune-mediated diseases, as psoriasis shares common biological pathways with other inflammatory conditions.
VYNE Therapeutics ha avviato uno studio di Fase 1b per VYN202, il suo inibitore BET selettivo per BD2 per via orale, in pazienti con psoriasi placca da moderata a grave. Lo studio valuterà dosi giornaliere per 12 settimane, concentrandosi principalmente sulla valutazione della sicurezza, con obiettivi secondari che includono il profilo farmacocinetico e le misurazioni di efficacia attraverso i punteggi PASI.
L'azienda prevede di riportare dati preliminari da questo studio randomizzato, controllato con placebo, entro la fine del 2025. Precedenti studi di Fase 1a con dose singola crescente (SAD) e dose multipla crescente (MAD) hanno dimostrato il favorevole profilo di sicurezza di VYN202 e la sua capacità di inibire diversi biomarcatori infiammatori correlati all'attività disregolata di Th17, TNF e Th1/myeloide.
Questo studio mira a fornire approfondimenti sul potenziale utilizzo di VYN202 in diverse malattie croniche mediate dal sistema immunitario, poiché la psoriasi condivide vie biologiche comuni con altre condizioni infiammatorie.
VYNE Therapeutics ha iniciado un ensayo de Fase 1b para VYN202, su inhibidor BET selectivo para BD2 por vía oral, en pacientes con psoriasis en placas de moderada a severa. El ensayo evaluará dosis diarias durante 12 semanas, centrándose principalmente en la evaluación de la seguridad, con objetivos secundarios que incluyen el perfil farmacocinético y las mediciones de eficacia a través de los puntajes PASI.
La empresa espera informar los datos preliminares de este ensayo aleatorizado y controlado con placebo para finales de 2025. Ensayos anteriores de Fase 1a con dosis únicas ascendentes (SAD) y dosis múltiples ascendentes (MAD) demostraron el perfil de seguridad favorable de VYN202 y su capacidad para inhibir múltiples biomarcadores inflamatorios relacionados con la actividad disfuncional de Th17, TNF y Th1/mieloide.
Este ensayo tiene como objetivo proporcionar información sobre la posible aplicación de VYN202 en diversas enfermedades crónicas mediadas por el sistema inmunológico, ya que la psoriasis comparte vías biológicas comunes con otras condiciones inflamatorias.
VYNE Therapeutics는 중등도에서 중증의 판상 건선 환자를 대상으로 하는 경구 BD2 선택적 BET 억제제인 VYN202의 1b상 시험을 시작했습니다. 이 시험은 12주 동안 하루 한 번 복용하는 용량을 평가하며, 주로 안전성 평가에 중점을 두고, 2차 목표로는 약리학적 프로필과 PASI 점수를 통한 효능 측정이 포함됩니다.
회사는 2025년 연말까지 이 무작위, 위약 대조 시험의 주요 데이터를 보고할 것으로 예상하고 있습니다. 이전의 1a상 단일 용량 상승(SAD) 및 다중 용량 상승(MAD) 시험에서는 VYN202의 유리한 안전성 프로필과 Th17, TNF 및 Th1/골수 불균형 활동과 관련된 여러 염증 바이오마커를 억제하는 능력이 입증되었습니다.
이 시험은 건선이 다른 염증 상태와 공통 생물학적 경로를 공유하므로, VYN202의 다양한 만성 면역 매개 질환에 대한 잠재적 적용에 대한 통찰력을 제공하는 것을 목표로 합니다.
VYNE Therapeutics a lancé un essai de phase 1b pour VYN202, son inhibiteur BET sélectif pour BD2 par voie orale, chez des patients atteints de psoriasis en plaques modéré à sévère. L'essai évaluera des doses quotidiennes pendant 12 semaines, en se concentrant principalement sur l'évaluation de la sécurité, avec des objectifs secondaires incluant le profil pharmacocinétique et les mesures d'efficacité à travers les scores PASI.
L'entreprise prévoit de communiquer des données préliminaires de cet essai randomisé, contrôlé par placebo, d'ici la fin de l'année 2025. Des essais précédents de phase 1a avec doses uniques ascendantes (SAD) et doses multiples ascendantes (MAD) ont démontré le profil de sécurité favorable de VYN202 et sa capacité à inhiber plusieurs biomarqueurs inflammatoires liés à l'activité dysrégulée de Th17, TNF et Th1/myéloïde.
Cet essai vise à fournir des informations sur l'application potentielle de VYN202 dans diverses maladies chroniques médiées par le système immunitaire, car le psoriasis partage des voies biologiques communes avec d'autres conditions inflammatoires.
VYNE Therapeutics hat eine Phase-1b-Studie für VYN202, seinen oral verabreichbaren BD2-selektiven BET-Inhibitor, bei Patienten mit moderater bis schwerer Plaque-Psoriasis initiiert. Die Studie wird tägliche Dosen über einen Zeitraum von 12 Wochen evaluieren, wobei der Schwerpunkt hauptsächlich auf der Sicherheitsbewertung liegt. Sekundäre Ziele umfassen das pharmakokinetische Profil und die Wirksamkeitsmessungen anhand der PASI-Werte.
Das Unternehmen erwartet, bis Ende 2025 erste Ergebnisse dieser randomisierten, placebokontrollierten Studie zu berichten. Frühere Phase-1a-Studien mit einmaligen und mehrfachen aufsteigenden Dosen (SAD und MAD) haben das günstige Sicherheitsprofil von VYN202 und dessen Fähigkeit zur Hemmung mehrerer entzündlicher Biomarker in Bezug auf Th17, TNF und Th1/myeloide Dysregulation gezeigt.
Diese Studie zielt darauf ab, Einblicke in das potenzielle Anwendungsspektrum von VYN202 bei verschiedenen chronischen, immunvermittelten Krankheiten zu geben, da Psoriasis gemeinsame biologische Wege mit anderen entzündlichen Erkrankungen teilt.
- Successful initiation of Phase 1b trial for VYN202
- Previous Phase 1a trials showed favorable safety profile
- Demonstrated ability to inhibit multiple inflammatory biomarkers
- Results not expected until year-end 2025
- Still in early clinical development phase
Insights
The initiation of VYN202's Phase 1b trial represents a strategic advancement in the development of selective BET inhibitors for immune-mediated diseases. The BD2-selective approach is particularly noteworthy as it potentially offers improved safety compared to first-generation BET inhibitors, which often faced toxicity challenges due to broader targeting.
The trial's design reveals several key strategic elements:
- The focus on moderate-to-severe plaque psoriasis provides a well-defined patient population with established endpoints (PASI scores), enabling clear efficacy measurements
- The oral, once-daily administration could offer a significant advantage over injectable biologics, potentially improving patient compliance and quality of life
- The 12-week duration is sufficient to demonstrate both safety and preliminary efficacy signals
The previous Phase 1a results showing inhibition of Th17, TNF, and Th1/myeloid inflammatory biomarkers are particularly significant. These pathways are implicated not only in psoriasis but also in numerous other inflammatory conditions, suggesting broader therapeutic potential. This positions VYN202 as a potential platform therapy for multiple indications.
The development timeline, with top-line data expected by year-end 2025, indicates a well-planned clinical program. However, investors should note that this is still an early-stage trial, and success in Phase 1b trials doesn't guarantee efficacy in larger Phase 2/3 studies. The small market cap of
- Oral, once-daily doses of VYN202 being evaluated in subjects with moderate-to-severe plaque psoriasis
- Top-line data from the 12-week double-blind trial expected by year-end 2025
- Phase 1b trial designed to provide key insights into VYN202’s potential across a range of chronic, immune-mediated diseases
BRIDGEWATER, N.J., Feb. 19, 2025 (GLOBE NEWSWIRE) -- 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 that the first subject has been dosed in a Phase 1b trial evaluating VYN202 in moderate-to-severe plaque psoriasis. VYN202 is an oral small molecule BD2-selective bromodomain and extra-terminal domain (BET) inhibitor that is being developed for the treatment of immune-mediated diseases. The Phase 1b trial will primarily evaluate the safety of VYN202, administered orally once a day for 12 weeks, with secondary objectives to evaluate the pharmacokinetic profile and preliminary evidence of efficacy, including improvement from baseline in psoriasis area and severity index (PASI) scores. Top-line data from the 12-week randomized, placebo-controlled trial are expected by year-end 2025.
“The initiation of the Phase 1b trial in subjects with moderate-to-severe plaque psoriasis represents a major step forward in advancing our novel and highly selective oral BET inhibitor, VYN202,” said David Domzalski, President and Chief Executive Officer of VYNE. “Psoriasis shares common underlying biological pathways with several other chronic inflammatory conditions, and we believe results from this trial will provide key insights into VYN202’s potential use as a novel, once-daily oral treatment for chronic immune-mediated diseases.”
“Our Phase 1a single ascending dose (SAD) and multiple ascending dose (MAD) trial showed that VYN202 had a favorable safety profile and also demonstrated VYN202’s potential to inhibit the production of multiple inflammatory biomarkers related to Th17, TNF and Th1/myeloid dysregulated activity,” said Iain Stuart, PhD, Chief Scientific Officer of VYNE. “We look forward to reporting results from this robust Phase 1b trial by the end of this year.”
About the Phase 1b Trial for VYN202
The Phase 1b trial is a randomized, double-blind, placebo-controlled trial evaluating the safety, tolerability and pharmacokinetics of once-daily VYN202 in three dosing cohorts (0.25 mg, 0.5 mg, 1 mg doses), compared to placebo, for 12 weeks in subjects with moderate-to-severe plaque psoriasis. Exploratory efficacy of VYN202 will also be evaluated including measures of PASI, Static Physician Global Assessment (sPGA), scalp disease, quality of life, and biomarker analyses. Subjects will be randomized equally (1:1:1:1 ratio) across the active drug cohorts or placebo (~20 subjects in each arm). Following the 12-week treatment period, all subjects will be followed for a 4-week safety period.
About Plaque Psoriasis
Plaque psoriasis is a chronic immune-mediated disease resulting in overproduction of skin cells, which causes inflamed, scaly plaques that may be itchy or painful.1 It is estimated that eight million Americans and more than 125 million people worldwide live with the disease.2 Plaque psoriasis is believed to share common inflammatory pathways involving IL-23/IL-17, TNF, among others, which drive other chronic immune mediated diseases such as psoriatic arthritis (PsA), hidradenitis suppurativa (HS), inflammatory bowel disease (IBD), and axial spondyloarthritis (AxSpA).
About VYN202
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 are common.
About BET Inhibitors
BET proteins play a key role in regulating gene transcription via epigenetic interactions (“reading”) in the nucleus of the cell. Recent research has identified a key role for these proteins in regulating activation of immune cells, including T cells 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 National Psoriasis Foundation. About Psoriasis. Available at: https://www.psoriasis.org/about-psoriasis. Accessed January 2025.
2 National Psoriasis Foundation. Psoriasis Statistics. Available at: https://www.psoriasis.org/content/statistics. Accessed January 2025.
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 (“SEC”), 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 statements regarding the clinical development of VYNE’s product candidates, including VYN202, the timing of results from VYNE’s Phase 1b trial, and the potential benefits of VYNE’s product candidates, including 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: 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 of future events.
Investor Relations:
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Tyler Zeronda
VYNE Therapeutics Inc.
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Tyler.Zeronda@vynetx.com
Media Relations:
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FAQ
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