Fam-Trastuzumab Deruxtecan-Nxki

Drug

Drug Profile

Enhertu is the brand name of trastuzumab deruxtecan, an antibody-drug conjugate combining trastuzumab with a topoisomerase I inhibitor payload. It is used in HER2-expressing cancers including breast, NSCLC, and gastric/GEJ adenocarcinoma settings. It has approvals in the U.S., Japan, EU, and other regions with multiple later indication expansions.

Drug Class
Antibody-drug conjugate; antineoplastic
Approval Status
Approved in the United States in December 2019, Japan in March 2020, European Union in January 2021, and Australia in October 2021, with additional subsequent indication expansions
Mechanism of Action
Binds HER2 and, after receptor-mediated internalization, delivers deruxtecan payload to interfere with DNA replication and induce tumor cell death
Brand Names
  • Enhertu
Indications
  • \Unresectable or metastatic HER2-positive breast cancer in specified prior-treatment settings\
  • \HER2-low breast cancer in unresectable/metastatic setting\
  • \Locally advanced or metastatic HER2-positive gastric or gastroesophageal junction adenocarcinoma after prior trastuzumab-based regimen\
  • \Additional HER2-positive solid tumor settings per expanded approvals\

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