Journal
BIOCONJUGATE CHEMISTRY
Volume 33, Issue 7, Pages 1241-1253Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.2c00177
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Funding
- Intramural Research Program of the National Institutes of Health, National Cancer Institute (NCI), Center for Cancer Research
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Antibody-drug conjugates (ADCs) are a rapidly growing class of cancer therapeutics that aim to overcome the limitations of conventional cytotoxic agents. This review describes different ADCs combinations and technologies, with a focus on the anti-HER-2 antibody trastuzumab and its variants.
Antibody-drug conjugates (ADCs) are a rapidly growing class of cancer therapeutics that seek to overcome the low therapeutic index of conventional cytotoxic agents. However, realizing this goal has been a significant challenge. ADCs comprise several independently modifiable components, including the antibody, payload, linker, and bioconjugation method. Many approaches have been developed to improve the physical properties, potency, and selectivity of ADCs. The anti-HER-2 antibody trastuzumab, first approved in 1998, has emerged as an exceptional targeting agent for ADCs, as well as a broadly used platform for testing new technologies. The extensive work in this area enables the comparison of various linker strategies, payloads, drug-to-antibody ratios (DAR), and mode of attachment. In this review, these conjugates, ranging from the first clinically approved trastuzumab ADC, ado-trastuzumab emtansine (Kadcyla), to the latest variants are described with the goal of providing a broad overview, as well as enabling the comparison of existing and emerging conjugate technologies.
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