Usynova 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.
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.
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.
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.