2. Academic Validation
  3. Small Molecule-Drug Conjugates Emerge as a New Promising Approach for Cancer Treatment

Small Molecule-Drug Conjugates Emerge as a New Promising Approach for Cancer Treatment

  • Mol Pharm. 2024 Mar 4;21(3):1038-1055. doi: 10.1021/acs.molpharmaceut.3c01049.
Tiansi Wang 1 2,  Meichai Li 1 2,  Ruting Wei 1 2,  Xinyu Wang 1 2,  Zhizhe Lin 2 3,  Jianming Chen 1 2,  Xin Wu 1 2
Affiliations

Affiliations

  • 1 Fujian University of Traditional Chinese Medicine, No. 1, Qiuyang Road, Fuzhou, Fujian 350122, China.
  • 2 Shanghai Wei Er Lab, Shanghai 201799, China.
  • 3 Shandong University of Traditional Chinese Medicine, No.4655, University Road, Jinan, Shandong 250355, China.
PMID: 38344996 DOI: 10.1021/acs.molpharmaceut.3c01049
Abstract

Antibody drug conjugates (ADCs) have emerged as a new promising class of anti- Cancer agents. However, limitations such as higher costs and unavoidable immunogenicity due to their relatively large structures cannot be ignored. Therefore, the development of lightweight drugs such as small molecule-drug conjugates (SMDCs) based on the ADC design idea has become a new option for targeted therapy. SMDCs are derived from the coupling of small-molecule targeting ligands with cytotoxic drugs. They are composed of three parts: small-molecule targeting ligands, cytotoxic molecules, and linkers. Compared with ADCs, SMDCs can be more rapidly and evenly dispersed into tumor tissues, with low cost and no immunogenicity. In this article, we will give a comprehensive review of different types of SMDCs currently under clinical trials to provide ideas and inspirations for the development of clinically applicable SMDCs.

Keywords

cancer; conjugates; linker; small molecule−drug conjugates; target treatment.

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