Antibody-Drug Conjugates Use Click Chemistry for Cancer Therapy

Researchers have developed a new method for in vivo ligation of therapeutic antibodies to antibody-drug conjugates (ADCs) using bioorthogonal click chemistry. This technique, published online on July 15, 2026, in Nature, enables the modular assembly of ADCs directly within the body. The approach demonstrated enhanced anti-tumor activity in heterogeneous and treatment-resistant tumors in preclinical models.

The study details how clinically used therapeutic antibodies can be modified to participate in click chemistry reactions. These modified antibodies are then ligated to ADCs, which are designed to deliver cytotoxic drugs specifically to cancer cells. This in vivo conjugation strategy allows for the precise targeting of tumors and the controlled release of therapeutic payloads, potentially overcoming limitations of traditional ADC delivery methods.

This modular approach offers a flexible platform for developing next-generation ADCs. By enabling the rapid assembly of different antibody-drug combinations within the body, researchers can optimize treatment strategies for various cancer types and patient profiles. The enhanced anti-tumor efficacy observed in resistant tumor models suggests a significant advancement in cancer therapy, offering new hope for patients with limited treatment options.