TJ101 is a bispecific antibody-drug conjugate (ADC) targeting EGFR and B7-H3, currently in a Phase 1 clinical trial in patients with advanced solid tumors. TJ101 is designed to use bispecific targeting to improve tumor selectivity and reduce off-tumor toxicity relative to conventional monospecific ADCs.

EGFR is a clinically validated oncology target that drives tumor growth and metastasis. B7-H3 is a B7-family immunoregulatory protein associated with tumor progression, with limited protein expression in normal tissue. EGFR and B7-H3 are frequently co-expressed in solid tumors, including lung and head and neck cancers, making them a well-matched pair for bispecific ADC targeting.

TJ101 comprises a humanized IgG1 bispecific antibody engineered using knobs-into-holes (KIH) technology, conjugated via a cleavable linker to a proprietary topoisomerase I inhibitor, at a drug-to-antibody ratio (DAR) of 8. Following internalization by tumor cells, the linker is enzymatically cleaved in the lysosome to release the payload, enabling both direct tumor cell killing and a potent bystander effect against neighboring tumor cells. In preclinical studies, TJ101 bound selectively to EGFR/B7-H3 co-expressing tumor cells, induced potent cytotoxicity, and produced robust antitumor activity in mouse xenograft models.

Phase 1 trial: NCT07181473

TJ101 is a bispecific antibody-drug conjugate (ADC) targeting EGFR and B7-H3, currently in a Phase 1 clinical trial in patients with advanced solid tumors. TJ101 is designed to use bispecific targeting to improve tumor selectivity and reduce off-tumor toxicity relative to conventional monospecific ADCs.

EGFR is a clinically validated oncology target that drives tumor growth and metastasis. B7-H3 is a B7-family immunoregulatory protein associated with tumor progression, with limited protein expression in normal tissue. EGFR and B7-H3 are frequently co-expressed in solid tumors, including lung and head and neck cancers, making them a well-matched pair for bispecific ADC targeting.

TJ101 comprises a humanized IgG1 bispecific antibody engineered using knobs-into-holes (KIH) technology, conjugated via a cleavable linker to a proprietary topoisomerase I inhibitor, at a drug-to-antibody ratio (DAR) of 8. Following internalization by tumor cells, the linker is enzymatically cleaved in the lysosome to release the payload, enabling both direct tumor cell killing and a potent bystander effect against neighboring tumor cells. In preclinical studies, TJ101 bound selectively to EGFR/B7-H3 co-expressing tumor cells, induced potent cytotoxicity, and produced robust antitumor activity in mouse xenograft models.

Phase 1 trial: NCT07181473