VYNE Therapeutics Inc. (Nasdaq: VYNE) announced today that the U.S. Food and Drug Administration has cleared its Investigational New Drug application (IND) for VYN202, an oral BD2-selective BET inhibitor. This marks a significant advancement in the company's efforts to develop therapies for autoimmune diseases.

VYNE Therapeutics Inc.（纳斯达克代码：VYNE）今天宣布，美国食品和药物管理局（FDA）已批准VYN202（一种口服BD2选择性BET抑制剂）的研究性新药申请（IND）。这标志着该公司开发自身免疫性疾病治疗方法的努力取得了重大进展。

David Domzalski, President and CEO of VYNE, expressed excitement about the potential of VYN202 as a treatment option.The company plans to initiate a Phase 1a trial to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of VYN202 in healthy volunteers. This trial will include single ascending dose/multiple ascending dose (SAD/MAD) components and is expected to enroll approximately 64 subjects.

VYNE总裁兼首席执行官大卫·多姆扎尔斯基（DavidDomzalski）对VYN202作为一种治疗选择的潜力表示兴奋。该公司计划启动1a期试验，以评估VYN202在健康志愿者中的安全性，耐受性，药代动力学和药效学。该试验将包括单次递增剂量/多次递增剂量（SAD/MAD）成分，预计将招募大约64名受试者。

Pending successful completion of Phase 1a, VYNE intends to move forward with Phase 1b trials targeting moderate-to-severe plaque psoriasis and adult-onset rheumatoid arthritis, with results anticipated in the latter half of 2025.VYN202 is an oral small molecule BD2-selective BET inhibitor designed to offer high selectivity, potency, and oral bioavailability.

在1a期成功完成之前，VYNE打算推进针对中度至重度斑块状牛皮癣和成人发作性类风湿性关节炎的1b期试验，预计将在2025年下半年取得结果。VYN202是一种口服小分子BD2选择性BET抑制剂，旨在提供高选择性，效力和口服生物利用度。

It differs structurally from VYNE's pan-BET inhibitor, VYN201, and is covered by distinct patent applications.BET proteins play a crucial role in gene transcription regulation through epigenetic interactions, particularly in modulating B and T cell activation and inflammation. BET inhibitors hold promise for addressing various immuno-inflammatory and fibrotic diseases by blocking pro-inflammatory cytokine transcription, with potential applications in myeloproliferative neoplastic disorders. Source: vynetherapeutics.com.

它在结构上不同于VYNE的泛BET抑制剂VYN201，并被不同的专利申请所涵盖。BET蛋白通过表观遗传相互作用在基因转录调控中起着至关重要的作用，特别是在调节B和T细胞活化和炎症方面。BET抑制剂有望通过阻断促炎细胞因子转录来解决各种免疫炎症和纤维化疾病，并在骨髓增生性肿瘤疾病中具有潜在的应用。来源：vynetherapeutics.com。