Enhertu trastuzumab deruxtecan

Drug Class

HER2-directed antibody and topoisomerase inhibitor conjugate

Mechanism

Trastuzumab deruxtecan binds to HER2 on cancer cells, undergoes receptor-mediated endocytosis, and releases a topoisomerase I inhibitor that damages DNA and induces cell death.

Approved Indication

Treatment of adult patients with unresectable or metastatic HER2-low (IHC 1+ or IHC 2+/ISH-) breast cancer; HER2-positive breast cancer; and HER2-mutant non-small cell lung cancer (NSCLC) or HER2-positive gastric cancer.

What This Means For Patients

Enhertu (trastuzumab deruxtecan) is a targeted antibody-drug conjugate (ADC) used to treat HER2-positive or HER2-low breast cancers, gastric cancer, and lung cancer. It delivers a chemotherapy agent directly into HER2-expressing cancer cells. It is approved in mainland China and also clinically available under early access programs in Hainan's Boao Lecheng pilot zone.

Regulatory Approvals

• FDA — approved (2019) — label
• EMA — approved (2021) — source
• NMPA — approved (2023) — source

Pivotal Clinical Evidence

• DESTINY-Breast04 — Modi et al., N Engl J Med 2022 (NCT03734029) — DOI

Sources

• https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/761139s022lbl.pdf
• https://www.ema.europa.eu/en/medicines/human/EPAR/enhertu
• https://doi.org/10.1056/NEJMoa2203690