Antibody-drug Conjugate Targets, Drugs, and Linkers

Beverly   A.   Teicher; Joel      Morris
doi:10.2174/1568009622666220224110538
Abstract

Antibody-drug conjugates offer the possibility of directing powerful cytotoxic agents to a malignant tumor while sparing normal tissue. The challenge is to select an antibody target expressed exclusively or at highly elevated levels on the surface of tumor cells and either not all or at low levels on normal cells. The current review explores 78 targets that have been explored as antibody-drug conjugate targets. Some of these targets have been abandoned, 9 or more are the targets of FDA-approved drugs, and most remain active clinical interest. Antibody-drug conjugates require potent cytotoxic drug payloads, several of these small molecules are discussed, as are the linkers between the protein component and small molecule components of the conjugates. Finally, conclusions regarding the elements for the successful antibody-drug conjugate are discussed.
Keywords: Antibody-drug conjugates, ADCs, cell surface targets, auristatins, maytansines, cytotoxic drugs.
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Graphical Abstract

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DOI https://dx.doi.org/10.2174/1568009622666220224110538	Print ISSN 1568-0096
Publisher Name Bentham Science Publisher	Online ISSN 1873-5576
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