Open Access

Development, efficacy and side effects of antibody‑drug conjugates for cancer therapy (Review)

  • Authors:
    • Te Sun
    • Xueli Niu
    • Qing He
    • Min Liu
    • Shuai Qiao
    • Rui-Qun Qi
  • View Affiliations

  • Published online on: May 4, 2023     https://doi.org/10.3892/mco.2023.2643
  • Article Number: 47
  • Copyright: © Sun et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

Antibody‑drug conjugates (ADCs) are anticancer drugs that combine cytotoxic small‑molecule drugs (payloads) with monoclonal antibodies through a chemical linker and that transfer toxic payloads to tumor cells expressing target antigens. All ADCs are based on human IgG. In 2009, the Food and Drug Administration (FDA) approved gemtuzumab ozogamicin as the initial first‑generation ADC. Since then, at least 100 ADC‑related projects have been initiated, and 14 ADCs are currently being tested in clinical trials. The limited success of gemtuzumab ozogamicin has led to the development of optimization strategies for the next generation of drugs. Subsequently, experts have improved the first‑generation ADCs and have developed second‑generation ADCs such as ado‑trastuzumab emtansine. Second‑generation ADCs have higher specific antigen levels, more stable linkers and longer half‑lives and show great potential to transform cancer treatment models. Since the first two generations of ADCs have served as a good foundation, the development of ADCs is accelerating, and third‑generation ADCs, represented by trastuzumab deruxtecan, are ready for wide application. Third‑generation ADCs are characterized by strong pharmacokinetics and high pharmaceutical activity, and their drug‑to‑antibody ratio mainly ranges from 2 to 4. In the past decade, the research prospects of ADCs have broadened, and an increasing number of specific antigen targets and mechanisms of cytotoxic drug release have been discovered and studied. To date, seven ADCs have been approved by the FDA for lymphoma, and three have been approved to treat breast cancer. The present review explores the function and development of ADCs and their clinical use in cancer treatment.
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June-2023
Volume 18 Issue 6

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Copy and paste a formatted citation
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Spandidos Publications style
Sun T, Niu X, He Q, Liu M, Qiao S and Qi R: Development, efficacy and side effects of antibody‑drug conjugates for cancer therapy (Review). Mol Clin Oncol 18: 47, 2023
APA
Sun, T., Niu, X., He, Q., Liu, M., Qiao, S., & Qi, R. (2023). Development, efficacy and side effects of antibody‑drug conjugates for cancer therapy (Review). Molecular and Clinical Oncology, 18, 47. https://doi.org/10.3892/mco.2023.2643
MLA
Sun, T., Niu, X., He, Q., Liu, M., Qiao, S., Qi, R."Development, efficacy and side effects of antibody‑drug conjugates for cancer therapy (Review)". Molecular and Clinical Oncology 18.6 (2023): 47.
Chicago
Sun, T., Niu, X., He, Q., Liu, M., Qiao, S., Qi, R."Development, efficacy and side effects of antibody‑drug conjugates for cancer therapy (Review)". Molecular and Clinical Oncology 18, no. 6 (2023): 47. https://doi.org/10.3892/mco.2023.2643