Usynova Initiates First-in-Human Phase 1 Clinical Trial of Allosteric TYK2 Inhibitor UA021 in AustraliaUsynova Pharmaceuticals Ltd, a private and clinical stage biotechnology company focused on developing innovative medicines for treatment of cancer and inflammatory diseases, today announced the dosing of first healthy volunteer in Australia in a Phase 1 clinical study of UA021, a potent, selective and allosteric investigational tyrosine kinase 2 (TYK2) inhibitor.“UA021 is an oral small molecule inhibitor that targets the pseudokinase (JH2) domain of TYK2 and has showed superior in vitro and in vivo activities in preclinical studies. The unique PK and superior safety profile of UA021 may provide better in vivo target coverage, and can hopefully translate into differentiated and better efficacy in patients with autoimmune diseases, such as psoriasis and inflammatory bowel disease (IBD). This molecule is ideal for combinational studies for overcoming drug resistance and treatment of hard-to-treat diseases,” commented Shengbin Peng, Ph.D., CSO of Usynova.“UA021 program is an excellent reflection of our R&D effectiveness. It took us approximately 20 months from project initiation, lead identification and optimization to first human dose. We are committed to develop this important molecule in China and globally, and the Phase I clinical study in China will likely occur in first quarter, 2023,” added Tao Hu, Ph.D., CEO of Usynova.The first-in-human Phase 1 trial (ACTRN12622001349730) is designed to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic effects of UA021. The trial is expected to enroll 64 healthy volunteers in Australia, and a separate Phase I study in China is planned in Q1, 2023.
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About UA021
UA021 is a potent, selective, and orally bioavailable TYK2 inhibitor. It allosterically targets the pseudokinase (JH2) domain of TYK2 with strong selectivity against other members of JAK family. Thus, it is expected to overcome the toxicities caused by active site JAK inhibitors due to their pan-inhibition of JAK family members. UA021 has showed similar or superior in vitro and in vivo activities to other competitors in preclinical studies, and demonstrated excellent safety profile in preclinical toxicity evaluation. It has the potential to achieve better in vivo target coverage and efficacy in patients. UA021 is currently being evaluated in a Phase 1 clinical study in Australia.
About TYK2
TYK2 is a member of the JAK family including JAK1, JAK2, JAK3 and TYK2. It is a critical component involved in signaling pathways mediated by many pro-inflammatory cytokines such as IL-12, IL-23, and Type 1 interferons. The dysfunction of these cytokines plays a determinant role in the induction of inflammation which is implicated in many immune-mediated disorders such as psoriasis, IBD and other autoimmune diseases.
About Usynova
Usynova Pharmaceuticals Ltd, located at Zhangjiang Hi-Tech Park, Shanghai, is a private and clinical stage biotechnology company focused on developing innovative medicines for treatment of cancer and autoimmune diseases. The company has established internal drug discovery platforms of small molecules and biologics. It currently has multiple pipeline products at different R&D stages. UA007, the lead asset of the company is currently in phase II clinical studies for two indications, gouty arthritis and chemotherapy-induced diarrhea (CID). The early clinical POC results of UA007 in both indications were achieved in the ongoing phase II studies. Gouty arthritis is one of the most common diseases in China and globally, and the current treatments often have drug resistance or undesirable side effects. CID is one of the main side effects of cancer chemotherapy, and it is also an important reason for cancer patients to withdraw from chemotherapy. However, there is currently no effective medicine for treatment of CID. In addition to UA007 and UA021, the company also has a few small molecules in late stage preclinical development.祐森健恒TYK2别构抑制剂在澳大利亚完成首例受试者给药祐森健恒生物医药（上海）有限公司（“祐森健恒”）的TYK2别构抑制剂UA021再传捷报，继获得国内临床试验申请受理通知书后，澳大利亚I期临床也进展顺利，于2022年12月19日完成首例健康受试者给药。祐森健恒CSO彭生斌博士表示：“UA021此次给药，标志着公司开发的TYK2小分子别构抑制剂治疗银屑病等自身免疫性疾病进入到临床阶段，彰显了公司在该疾病领域中强大的药物研发实力。后续将根据产品的特点和创新的临床开发策略，加速UA021在全球的开发进程”。祐森健恒CEO胡滔博士强调：“UA021项目顺利且快速在中澳两国同步推进，体现了祐森健恒立足国内、放眼国际的发展决心”。近期，武田（Tekeda）以60亿美元从Nimbus收购了后者完成II b阶段临床的在研TYK2别构抑制剂NDI-034858。这一消息再度点燃业界对TYK2别构位点的热情。祐森健恒的TYK2别构抑制剂在澳洲的一期临床，是中国创新药有能力进军国际主流市场的例证。需要特别指出的是，祐森健恒的UA021项目从立项、确认PCC到首次人体给药，只用了不到20个月。这充分体现了公司科研团队对项目的深刻理解和高效的组织和执行能力。
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