Trastuzumab deruxteca (Enhertu)
Antibody-Drug Conjugate · Approved since 2019
Description
Trastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate that targets HER2-positive colorectal cancers, which represent approximately 2-5% of all colorectal cancer cases. This precision medicine combines the HER2-targeting antibody trastuzumab with a potent topoisomerase I inhibitor payload. In colorectal cancer, it is specifically used for patients whose tumors demonstrate HER2 overexpression or amplification, providing a treatment option for this molecularly defined subset of patients.
Mechanism of Action
The drug binds to HER2 receptors on cancer cell surfaces through its trastuzumab component, allowing selective uptake into HER2-positive tumor cells. Once internalized, the linker is cleaved, releasing the cytotoxic deruxtecan payload (a topoisomerase I inhibitor) which causes DNA damage and cell death in both the targeted cell and nearby tumor cells through a bystander effect.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.