SHANGHAI, February 10, 2025 — BioRay Pharmaceutical Co., Ltd. announced on December 19, 2024, that the National Medical Products Administration (NMPA) has approved its clinical trial application for BR111, a novel, self-developed Class 1 therapeutic biologic. BR111, an antibody-drug conjugate (ADC), targets dual ROR1 epitopes to treat ROR1-positive hematologic malignancies and solid tumors.
ROR1, a transmembrane receptor tyrosine kinase, is minimally expressed in normal tissues but highly expressed in various cancers, including lymphoma, breast, ovarian, and lung cancers. It plays a role in the Wnt5a-mediated non-canonical Wnt signaling pathway, influencing tumor cell growth and invasion. Its link to tumorigenesis and drug resistance makes it an attractive drug target. Currently, no ROR1-targeted therapies are commercially available.
BR111 employs BioRay’s CysX™ irreversible site-specific conjugation technology to link a dual-epitope ROR1-targeting antibody with the small-molecule toxin eribulin. As the world’s first anti-ROR1 Bi-paratopic ADC to enter clinical trials, BR111’s dual-epitope targeting enhances affinity and endocytosis. Following uptake by ROR1-positive tumor cells, the toxin is released within the lysosome, effectively killing the cells. The CysX™ platform ensures BR111’s high homogeneity and circulatory stability, minimizing toxin release in circulation and improving both safety and therapeutic index.
Preclinical studies showed BR111’s superior anti-tumor efficacy and safety profile compared to existing therapies in multiple animal models. Furthermore, BR111’s bystander effect and ability to activate immune responses in the tumor microenvironment suggest potential for combination therapies with other targeted or immunotherapeutic agents.
The NMPA’s approval reflects BioRay’s strong R&D capabilities and validates the CysX™ platform. BioRay remains committed to clinical needs, innovative research, and advancing biopharmaceutical technologies to provide patients with more effective and safer treatments.