BeiGene Initiates First-in-Human Phase 1 Clinical Trial of Investigational TYK2 Inhibitor BGB-23339

Expanding portfolio with first internally discovered asset in Inflammation and Immunology with internally discovered asset

A highly selective, allosteric TYK2 inhibitor that has shown potent inhibition against pro-inflammatory cytokines in preclinical studies

CAMBRIDGE, Mass. & BEIJING–(BUSINESS WIRE)– BeiGene (NASDAQ: BGNE; HKEX: 06160), a global, science-driven biotechnology company focused on developing innovative and affordable medicines, today announced that the first patient has been dosed in a Phase 1 clinical trial of BGB-23339, a potent, allosteric investigational tyrosine kinase 2 (TYK2) inhibitor internally developed by BeiGene scientists.

TYK2 is a member of the JAK family and functions as a critical mediator in cytokine signaling pathways implicated in multiple immune-mediated disorders, such as psoriasis and inflammatory bowel disease. BGB-23339 is a potent, highly selective, investigational TYK2 inhibitor targeting the regulatory pseudokinase (JH2) domain.

“Discovered and developed by BeiGene, BGB-23339 is a highly selective, potent, allosteric TYK2 inhibitor that has shown promising activity in preclinical evaluation,” commented Lai Wang, Ph.D., Global Head of R&D at BeiGene. “Building on our proven track record in oncology, BeiGene is expanding its clinical focus to discover new modalities and platforms in areas of high unmet need, including inflammation and immunology, to bring innovative, impactful medicines to patients.”

The first-in-human Phase 1 trial (NCT05093270) is designed to evaluate the safety, tolerability, pharmacokinetics, and preliminary activity of BGB-23339. The trial is expected to enroll up to 115 healthy volunteers in Australia and/or China.

In addition to its broad portfolio focused on hematological malignancies and solid tumors, BeiGene is applying its research excellence and clinical expertise to address inflammation and immunology, an area of high unmet medical need. BeiGene’s internally developed, highly selective next-generation BTK inhibitor BRUKINSA® (zanubrutinib) is currently being evaluated in a Phase 2 trial in patients with active proliferative lupus nephritis.