VYN202 / Vyne Therap, Tay Therap - LARVOL DELTA

VYNE Therapeutics Provides Program Update on Oral BET inhibitor VYN202 (GlobeNewswire) - "Following the clinical hold, VYNE made the decision to unblind the clinical data from the subjects who were enrolled in the study (VYN202 treated: n=6 across 0.25 mg, 0.5 mg and 1 mg doses; Placebo treated: n=1), the results of which are described below...The Company believes that the totality of the data from this study, together with promising results from multiple preclinical models, support the continued advancement of VYN202 into serious, immune-mediated diseases with limited effective treatment options. Based on this assessment, the Company will no longer enroll patients in the Phase 1b psoriasis study, extending the Company’s expected cash runway into the fourth quarter of 2026. VYNE expects to provide further updates on its plans for the VYN202 program following the release of top-line results from the ongoing Phase 2b study of its lead candidate repibresib gel (formerly VYN201), a pan-BD BET inhibitor, for the treatment of non-segmental vitiligo."

Enrollment closed • P2b data • Psoriasis • Vitiligo

Preliminary Data from Phase 1b Trial (GlobeNewswire) - P1b | N=7 | "(n=7 enrolled: VYN202: n=6 across 0.25 mg, 0.5 mg and 1 mg doses; Placebo: n=1)...No TESAEs or discontinuations due to a clinical TEAE...All subjects treated with VYN202 had an improvement in signs and symptoms of disease, including scalp psoriasis; Improvement in PASI scores ranged from ~27% reduction after 1 week of treatment to ~90% reduction at week 8; Improvements (reduction) in serum cytokine levels involved in the pathogenesis of plaque psoriasis were observed in subjects treated with VYN202 for greater than 1 week, including IL17A, IL17F, IL19 and IL22 ranging from -17% to -83%. There was no change in these serum cytokines for the subject receiving placebo...Subject treated with VYN202 0.5 mg reported a four-point improvement in joint pain NRS scale by week 2 which corresponded with a -48% reduction in serum c-reactive protein level, a biomarker associated with psoriatic arthritis and other rheumatic diseases."

P1 data • Psoriasis

EFFICACY OF A BD2-SELECTIVE BET INHIBITOR IN ANIMAL MODELS OF RHEUMATOID ARTHRITIS BY INHIBITION OF NF-KB DRIVEN INFLAMMATORY PATHWAYS (EULAR 2025) - "Antagonists to these cytokines (e.g. adalimumab, anakinra, tocilizumab) are known to be effective in the treatment of RA...Objectives: To evaluate the efficacy of orally administered VYN202 in collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) models in rats compared to vehicle and reference compounds, dexamethasone (glucocorticoid), GSK620 (a less potent, earlier generation BD2-selective BET inhibitor), and upadacitinib (a Janus kinase inhibitor approved in RA)... BD2-selective BET inhibition with VYN202 represents a novel approach to treatment of NF-κB–mediated diseases such as RA. A phase 1b study of VYN202 in RA is planned."

Preclinical • Cardiovascular • Immunology • Inflammation • Inflammatory Arthritis • Rheumatoid Arthritis • Rheumatology • IL17A • IL23A • IL6

Inhibition of Th17 and NF-κB pathways with an oral, BD2-selective BET inhibitor in a phase 1 study (EULAR 2025) - "VYN202 represents a novel approach to treatment of Th17 and NF-kB–mediated diseases. A Phase 1b study of the agent in rheumatoid arthritis is planned."

P1 data • Ankylosing Spondylitis • Cardiovascular • Dermatology • Hematological Disorders • Immunology • Inflammation • Inflammatory Arthritis • Neutropenia • Psoriasis • Psoriatic Arthritis • Rheumatoid Arthritis • Rheumatology • Seronegative Spondyloarthropathies • Spondylarthritis • Thrombocytopenia • IL23A • IL6

VYNE Therapeutics Reports 2025 First Quarter Financial Results and Provides Business Update (GlobeNewswire) - "Research and development expenses. VYNE’s research and development expenses for the quarter ended March 31, 2025 and 2024 were $6.1 million and $3.7 million, respectively. The increase was primarily driven by increased expenses of $1.5 million for VYN202, increased expenses of $0.7 million for repibresib, and an increase in employee-related expenses of $0.3 million following the hiring of additional research and development personnel."

Commercial • Psoriasis

VYNE shares tumble after FDA clinical hold on psoriasis drug study (Investing.com) - "VYNE Therapeutics...stock plummeted 20.2% following the company’s announcement that the U.S. Food and Drug Administration (FDA) has placed a clinical hold on their Phase 1b study of VYN202, a treatment for moderate-to-severe plaque psoriasis."

Stock price • Psoriasis

VYNE Therapeutics Provides Update on VYN202 Program (GlobeNewswire) - "VYNE Therapeutics Inc...today announced that the U.S. Food and Drug Administration (FDA) verbally informed the Company that it placed a clinical hold on the Company’s Phase 1b study evaluating VYN202 for the treatment of moderate-to-severe plaque psoriasis. The clinical hold determination was made following a recent observation of testicular toxicity in dogs from a non-clinical toxicology study with VYN202....VYNE has suspended all screening, enrollment and patient dosing in the Phase 1b trial of VYN202 and intends to work diligently with the FDA to resolve the clinical hold as soon as possible. To date, there have been no serious adverse events observed in subjects that have been enrolled in the Phase 1b study."

Trial status • Psoriasis

Treatment of psoriasis by inhibition of NF-kB and Th17 pathways with an oral, BD2-selective, BET-inhibitor: preclinical evaluation (AAD 2025) - "Skin inflammation resembling psoriasis was induced in mice with topical application of an NF-kB activating agent, imiquimod (IMI), for 14 days (d). Mice were treated (n=8/group) i.p. with vehicle, 3 mg/kg of VYN202, or 3 mg/kg of the TYK2 inhibitor, deucravacitinib, once-daily on d8-d14...VYN202 is currently being evaluated in healthy volunteers at multiple doses prior to a proof-of-concept study in psoriasis. Results from the healthy volunteer study will be presented."

Preclinical • Dermatitis • Dermatology • Immunology • Inflammation • Psoriasis • IL17A • IL1B • IL22 • IL23A • IL6 • TNFA • TYK2

VYNE Therapeutics Initiates Phase 1b Trial of VYN202, a Novel BD2-Selective Oral BET Inhibitor, in Plaque Psoriasis (GlobeNewswire) - "VYNE Therapeutics...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."

P1 data • Trial status • Psoriasis

VYNE Therapeutics Reports Positive Top-line Phase 1a MAD Data for VYN202, its Novel BD2-Selective BET Inhibitor (GlobeNewswire) - P1a | N=NA | "VYNE Therapeutics Inc...today announced positive results from the multiple ascending dose ('MAD') portion of its Phase 1a SAD/MAD trial of VYN202...No serious adverse events (AEs), discontinuations due to an AE or clinically meaningful treatment emergent adverse events (TEAEs). All TEAEs were considered mild or moderate in severity. No drug-related adverse events associated with laboratory results. There were no AEs of any severity grade relating to thrombocytopenia, which is a known dose-limiting toxicity associated with earlier generations of BET inhibitors...Data supports once-daily dosing regimen. VYN202 demonstrated dose dependent exposure that reached steady-state after 7 once-daily doses. VYN202 blood levels were within key inhibitory thresholds of IC50 to IC90 against BD2 BRD4 for at least 24 hours at all doses."

P1 data • Immunology

VYNE Therapeutics Announces Granting of Composition of Matter Patent for VYN202, a Novel BD2-Selective BET Inhibitor (GlobeNewswire) - "VYNE Therapeutics Inc...announced GB Patent No. 2621505 entitled 'Pyrrolopyridone derivatives useful in the treatment of inflammatory disorders, immune disorders and cancer' has been granted by the United Kingdom’s Intellectual Property Office. This granted patent covers the compound in VYNE’s VYN202 program and has a 20-year term that will expire in June 2042....This newly issued patent is derived from Tay Therapeutics Limited’s Patent Cooperation Treaty (PCT) application No. WO 2023/275542 A1, which was filed nationally in multiple jurisdictions, and is exclusively licensed to VYNE. This patent is the first of the national filed applications to be granted."

Patent • Oncology

VYNE Therapeutics Announces Dosing of First Participants in Phase 1a Trial of Novel BD2-Selective BET Inhibitor VYN202 (GlobeNewswire) - "VYNE Therapeutics...announced that the first healthy volunteers have been dosed in the Phase 1a trial of VYN202. VYN202 is an oral small molecule BD2-selective bromodomain and extra-terminal domain (BET) inhibitor that is being developed for the treatment of immuno-inflammatory diseases. Top-line data are expected in the second half of 2024....The Phase 1a trial is a first-in-human double-blind, placebo-controlled study in healthy volunteers and consists of single ascending dose (SAD) and multiple ascending dose (MAD) components. The trial is currently expected to enroll approximately 64 healthy adult subjects into five SAD and three MAD cohorts to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of VYN202."

P1 data • Trial status • Immunology

VYNE Therapeutics gets FDA nod for new drug trial (Investing.com) - "VYNE Therapeutics Inc...announced today that the U.S. Food and Drug Administration (FDA) has cleared their Investigational New Drug (IND) application for VYN202. The company is poised to commence a Phase 1a single ascending dose/multiple ascending dose (SAD/MAD) trial for the drug, an oral BD2-selective BET inhibitor, within this quarter...The upcoming trial is a double-blind, placebo-controlled study involving approximately 64 healthy adult volunteers. The study is designed to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of VYN202. If the initial Phase 1a trial yields successful results, VYNE plans to initiate Phase 1b trials in patients with moderate-to-severe plaque psoriasis and adult-onset rheumatoid arthritis, expecting top-line results by the second half of 2025."

IND • New P1 trial • P1 data • Rheumatoid Arthritis

VYNE Reports 2023 Fourth Quarter and Year-End Financial Results and Provides Business Update (GlobeNewswire) - "VYN202, an oral small molecule BD2-selective BET inhibitor: Phase 1a trial expected to start in Q2– Assuming the IND is cleared by the FDA,VYNE expects to initiate its Phase 1a single ascending dose/multiple ascending dose (SAD/MAD) trial in healthy volunteers in the second quarter of 2024, with top line results from the trial anticipated in the second half of 2024. If the Phase 1a portion of the trial is successfully completed, VYNE plans to initiate Phase 1b trials in subjects with moderate-to-severe plaque psoriasis and moderate-to-severe adult-onset rheumatoid arthritis, with top line results anticipated in the second half of 2025."

New P1 trial • P1 data • Psoriasis • Rheumatoid Arthritis

VYNE Therapeutics Reports Positive Results from Preclinical Models for Oral BD2-Selective BET Inhibitor VYN202 (GlobeNewswire) - "Treatment with VYN202 resulted in significant inhibition of key inflammatory biomarkers and substantial resolution of the signs and symptoms of psoriasis and rheumatoid arthritis....VYNE expects to submit its IND for VYN202 by year-end 2023 and commence a first-in-human Phase 1a single ascending dose/multiple ascending dose trial in the first quarter of 2024. If successful, VYNE anticipates commencing Phase 1b trials in moderate-to-severe plaque psoriasis and in moderate-to-severe adult-onset rheumatoid arthritis in the second half of 2024."

IND • New P1 trial • Preclinical • Immunology • Psoriasis • Rheumatoid Arthritis