Resistance to antibody-drug conjugates: A review.
10.1016/j.apsb.2024.12.036
- Author:
Sijia LI
1
;
Xinyu ZHAO
1
;
Kai FU
1
;
Shuangli ZHU
1
;
Can PAN
1
;
Chuan YANG
1
;
Fang WANG
1
;
Kenneth K W TO
2
;
Liwu FU
1
Author Information
1. State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, Guangdong Esophageal Cancer Institute, Guangdong Provincial Clinical Research Center for Cancer, Sun Yat-sen University Cancer Center, Guangzhou 510060, China.
2. School of Pharmacy, the Chinese University of Hong Kong, Hong Kong 999077, China.
- Publication Type:Review
- Keywords:
Antibody–drug conjugates;
Cancer;
Combination therapy;
Cytotoxic therapy;
Drug resistance;
Oncotherapy;
Predictive biomarker;
Targeted therapy
- From:
Acta Pharmaceutica Sinica B
2025;15(2):737-756
- CountryChina
- Language:English
-
Abstract:
Antibody-drug conjugates (ADCs) are antitumor drugs composed of monoclonal antibodies and cytotoxic payload covalently coupled by a linker. Currently, 15 ADCs have been clinically approved worldwide. More than 100 clinical trials at different phases are underway to investigate the newly developed ADCs. ADCs represent one of the fastest growing classes of targeted antitumor drugs in oncology drug development. It takes advantage of the specific targeting of tumor-specific antigen by antibodies to deliver cytotoxic chemotherapeutic drugs precisely to tumor cells, thereby producing promising antitumor efficacy and favorable adverse effect profiles. However, emergence of drug resistance has severely hindered the clinical efficacy of ADCs. In this review, we introduce the structure and mechanism of ADCs, describe the development of ADCs, summarized the latest research about the mechanisms of ADC resistance, discussed the strategies to overcome ADCs resistance, and predicted biomarkers for treatment response to ADC, aiming to contribute to the development of ADCs in the future.
