Trastuzumab deruxtecan

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Trastuzumab Deruxtecan

Chemical structure of Trastuzumab Deruxtecan

Trastuzumab deruxtecan is a monoclonal antibody used in the treatment of certain types of cancer. It is a drug that combines a chemotherapy agent with a targeted therapy approach, specifically designed to target HER2-positive cancer cells.

Mechanism of Action

Trastuzumab deruxtecan is an antibody-drug conjugate (ADC) that consists of a humanized monoclonal antibody linked to a topoisomerase I inhibitor. The antibody component targets the HER2 receptor, which is overexpressed in some breast cancer and gastric cancer cells. Upon binding to the HER2 receptor, the conjugate is internalized by the cancer cell, where the cytotoxic agent is released, leading to DNA damage and cell death.

Clinical Use

Trastuzumab deruxtecan is primarily used in the treatment of HER2-positive metastatic breast cancer and has shown efficacy in patients who have previously been treated with other HER2-targeted therapies. It is also being investigated for use in other HER2-expressing cancers, such as gastric cancer and lung cancer.

Side Effects

Common side effects of trastuzumab deruxtecan include nausea, fatigue, vomiting, alopecia, and neutropenia. Serious side effects can include interstitial lung disease and cardiotoxicity. Patients receiving this treatment are closely monitored for these adverse effects.

Development and Approval

Trastuzumab deruxtecan was developed by Daiichi Sankyo in collaboration with AstraZeneca. It received accelerated approval from the U.S. Food and Drug Administration (FDA) for the treatment of HER2-positive metastatic breast cancer in patients who have received two or more prior anti-HER2-based regimens in the metastatic setting.

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Contributors: Prab R. Tumpati, MD