Bispecific ADC Platform

Antibody-drug conjugates (ADCs) have become a very promising therapeutic modality for antibody drug research and development, due to their ability to deliver a cytotoxic payload in an antigen-specific manner. Through decades of development, ADC technologies- including coupling and linker/payload- have made great breakthroughs. However, because the currently approved targets of ADCs are very limited, identifying safe and effective innovative targets remain the key to the future success of ADC research and development.

Mechanistically, bispecific antibodies can induce effector mechanisms not possible with monospecific antibodies or combination antibody therapy. Thus, bispecific ADCs targeting dual tumor-associated antigens (TAAs) have multiple potential anti-tumor advantages:

1. Simultaneous targeting of dual tumor-driven signaling pathways to overcome drug resistance; 2. Improved specificity for tumor cells co-expressing dual TAAs to reduce off-target toxicity; and 3. Imparting a new synergistic mechanism of dual-target binding and endocytosis, resulting in a more efficient tumor killing.

Overview of Biocytogen’s Bispecific ADC platform

The fully human antibodies produced by RenLite® mice have a common kappa light chain, which can effectively solve the mismatch problem between heavy chain and light chain during the assembly of BsAbs, facilitating drug development.


RenLite® mice can produce fully human antibodies with diverse epitopes and high affinity. In addition, KIH (knobs-into-holes) technology is used to connect the heavy chains of the two parental monoclonal antibodies, ensuring the successful assembly of a BsAb molecule with a stable monoclonal antibody structure. Combinations of TAA-targeting antibodies generated from RenLite mice are subsequently screened in a high-throughput manner. 


As part of Biocytogen’s Project Integrum, bsADCs assembled from TAA-targeting antibodies will be further evaluated by in vivo pharmacologic efficacy and in vitro analyses. The company’s large animal translational platform will further screen out products with better translational properties:

Bispecific ADC Development Progress


AACR 2023: A First-In-Class Anti-HER2/TROP2 Bispecific Antibody-Drug Conjugate (YH012) Exhibits Potent Anti-Tumor Efficacy

AACR 2023: YH013, a Novel Bispecific EGFR x MET Antibody-Drug Conjugate, Exhibits Potent Anti-Tumor Efficacy

AACR 2023: A Novel EGFR x MUC1 Bispecific Antibody-Drug Conjugate, BSA01, Targets MUC1 Transmembrane Cleavage Products and Improves Tumor Selectivity

AACR 2023: BCG022: A Novel Bispecific Antibody-Drug Conjugate Targeting HER3 and MET

AACR 2023: Discovery of BCG033, A Novel Anti-PTK7 x TROP2 Bispecific Antibody-Drug Conjugate with Promising Efficacy Against Triple-Negative Breast Cancer

AACR 2023: A First-In-Class Anti-TROP2/EGFR Bispecific Antibody-Drug Conjugate, DM001, Exhibits Potent Anti-Tumor Efficacy

AACR 2023: A First-In-Class Bispecific Antibody-Drug Conjugate (DM002) Targeting HER3 and the Juxtamembrane Domain of MUC1

AACR 2023: Identification of DM004, A First-In-Class Anti-5T4/MET Bispecific Antibody-Drug Conjugate

IO Summit EU 2023: YH013, a Common Light Chain Bispecific ADC Targeting EGFR and MET, Improves Preclinical Efficacy Over Its Parental Single-Targeting ADCs

AACR 2022: YH012, a Novel Bispecific Anti-HER2 and TROP2 Antibody-Drug Conjugate, Exhibits Potent Antitumor Efficacy

World ADC San Diego2022:YH013, a fully-human EGFR x MET bispecific ADC exhibits outstanding specificity and anti-tumor efficacy

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