Enhertu Enhertu

Generic name:

FAM-TRASTUZUMAB DERUXTECAN-NXKI

Company:

DAIICHI SANKYO

FDA approval date:

12/20/2019

Specific treatment:

ENHERTU is a HER2-directed antibody and topoisomerase inhibitor
conjugate indicated for the treatment of adult patients with
unresectable or metastatic HER2-positive breast cancer who have
received two or more prior anti-HER2-based regimens in the
metastatic setting. 

Mechanism of Action:

Fam-trastuzumab deruxtecan-nxki is a HER2-directed antibody-drug conjugate. The antibody is a humanized anti-HER2
IgG1. The small molecule, DXd, is a topoisomerase I inhibitor attached to the antibody by a cleavable linker. Following
binding to HER2 on tumor cells, fam-trastuzumab deruxtecan-nxki undergoes internalization and intracellular linker
cleavage by lysosomal enzymes. Upon release, the membrane-permeable DXd causes DNA damage and apoptotic cell
death. 

Dosage Form/Route:

For injection: 100 mg lyophilized powder in a single-dose vial 

Side Effects:

The most common adverse reactions (≥20%) were nausea, fatigue,
vomiting, alopecia, constipation, decreased appetite, anemia,
neutropenia, diarrhea, leukopenia, cough, and thrombocytopenia.