BioRay's ROR1-Targeting Dual-Epitope ADC Drug BR111 Receives Formal Clinical Trial Approval from NMPA

SHANGHAI,Feb. 10,2025 -- On December 19,2024,BioRay Pharmaceutical Co.,Ltd. ("BioRay") announced that the National Medical Products Administration (NMPA) has accepted the clinical trial application for its self-developed Class 1 innovative therapeutic biological product,BR111 for injection. BR111 is an antibody-drug conjugate (ADC) targeting dual epitopes of ROR1,intended for the treatment of ROR1-positive hematological malignancies and solid tumors.

ROR1 is a transmembrane receptor tyrosine kinase protein that is either not expressed or expressed at low levels in normal tissues,but is highly expressed in various hematological malignancies and solid tumors,such as lymphoma,breast cancer,ovarian cancer,and lung cancer. ROR1 is involved in the non-canonical Wnt signaling pathway mediated by Wnt5a,regulating the growth and invasion of tumor cells. It is closely associated with tumorigenesis and drug resistance,making it a potential target for oncology drug development. To date,no ROR1-targeting drugs have been marketed.

BR111 utilizes BioRay's next-generation CysX™ irreversible site-specific conjugation technology platform to conjugate an antibody targeting dual epitopes of ROR1 with the small-molecule toxin eribulin. It is the world's first anti-ROR1 Bi-paratopic ADC to enter clinical trials. BR111 can recognize two non-overlapping epitopes of ROR1 on the surface of tumor cells,and dual-epitope recognition brings stronger affinity and endocytosis. Once endocytosed into ROR1-positive tumor cells,BR111 releases the small-molecule toxin in the lysosome,effectively killing tumor cells. Developed using the CysX™platform,BR111 has higher homogeneity and circulating stability,significantly reducing toxin release in circulation,which enhances safety and optimizes the therapeutic window.

In preclinical studies,BR111 demonstrated superior in vivo anti-tumor efficacy compared to its clinical counterparts in multiple animal models and exhibited better safety. Additionally,BR111 can induce a bystander effect and activate immune response in the tumor microenvironment,showing potential for combination therapy with various drugs,including targeted therapies and immunotherapies.

The acceptance of this project application is a testament to BioRay's R&D capabilities and a validation of the CysX™ platform technology. Moving forward,BioRay will continue to focus on clinical needs,drive innovative research,and advance biopharmaceutical technology,with the goal of delivering more effective and safer treatment options to patients through innovative drugs.