Trastuzumab deruxtecan


Trastuzumab deruxtecan also known as fam-trastuzumab deruxtecan and sold under the brand name Enhertu, is a medication used for the treatment of adults with unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens in the metastatic setting.

Overview

Trastuzumab deruxtecan is an antibody-drug conjugate that includes a human epidermal growth factor receptor 2 -directed antibody trastuzumab and a topoisomerase I inhibitor conjugate deruxtecan. It was approved for use in the United States in December 2019.

Side effects and label warnings

The most common side effects are nausea, fatigue, vomiting, alopecia, constipation, decreased appetite, anemia, decreased neutrophil count, diarrhea, leukopenia, cough and decreased platelet count.
The prescribing information for fam-trastuzumab deruxtecan-nxki includes a boxed warning to advise health care professionals and patients about the risk of interstitial lung disease and embryo-fetal toxicity. Interstitial lung disease and pneumonitis, including cases resulting in death, have been reported with fam-trastuzumab deruxtecan-nxki.

History

The U.S. Food and Drug Administration approved fam-trastuzumab deruxtecan-nxki in December 2019. The application for fam-trastuzumab deruxtecan-nxki was granted accelerated approval, fast track designation, and breakthrough therapy designation.
The FDA approved fam-trastuzumab deruxtecan-nxki based on the results of one clinical trial enrolling 184 female patients with HER2-positive, unresectable and/or metastatic breast cancer who had received two or more prior anti-HER2 therapies in the metastatic setting. These patients were heavily pretreated in the metastatic setting, receiving between two and 17 therapies prior to receiving fam-trastuzumab deruxtecan-nxki. Patients in the clinical trial received fam-trastuzumab deruxtecan-nxki every three weeks and tumor imagining was obtained every six weeks. The overall response rate was 60.3%, which reflects the percentage of patients that had a certain amount of tumor shrinkage with a median duration of response of 14.8 months.
The FDA granted the approval of Enhertu to Daiichi Sankyo.