Since the landmark 2019 approval of Enhertu, the antibody-drug conjugate (ADC) drug that quickly became a blockbuster breast cancer therapy—with global sales surpassing $1.6 billion in 2022—industry investment in ADC technologies has surged. ADCs marry the precision of antibody targeting with the tumor-killing power of cytotoxic drugs, offering a compelling strategy for delivering potent therapies directly to diseased cells.
Enhertu chemically links deruxtecan, a topoisomerase I (topo I) inhibitor, to trastuzumab, a monoclonal antibody that selectively binds HER2—a protein essential for normal cell growth but overexpressed in many breast cancers. Topo I inhibitors are highly effective at destroying rapidly dividing cells characteristic of tumor progression, yet their lack of selectivity can also harm healthy tissue.
Today’s therapeutic companies are pushing ADC technology further by optimizing payload potency, improving linker chemistry, and even designing antibodies from scratch to transform clinical outcomes.
Cancer smart bomb
Kristen Buck, MD,…
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