Trastuzumab deruxtecan

Trastuzumab deruxtecan

Trastuzumab deruxtecan is a monoclonal antibody used in the treatment of certain types of cancer. It is a conjugate of the monoclonal antibody trastuzumab and a topoisomerase inhibitor, deruxtecan. This drug is primarily used for the treatment of HER2-positive breast cancer and gastric cancer.

Mechanism of Action

Trastuzumab deruxtecan works by targeting the HER2 receptor, which is overexpressed in some cancer cells. The trastuzumab component binds to the HER2 receptor, and the deruxtecan component, a cytotoxic agent, is then internalized into the cancer cell, where it induces DNA damage and apoptosis.

Clinical Use

Trastuzumab deruxtecan is approved for use in patients with HER2-positive breast cancer who have received prior anti-HER2-based regimens. It is also used in the treatment of HER2-positive gastric cancer. The drug has shown efficacy in patients with metastatic disease, providing an option for those who have exhausted other treatments.

Side Effects

Common side effects of trastuzumab deruxtecan include nausea, fatigue, vomiting, alopecia, and neutropenia. Serious side effects can include interstitial lung disease and pneumonitis, which require careful monitoring and management.

Development and Approval

Trastuzumab deruxtecan was developed by Daiichi Sankyo and AstraZeneca. It received accelerated approval from the U.S. Food and Drug Administration (FDA) in December 2019 for the treatment of HER2-positive breast cancer. Subsequent approvals have expanded its use to other indications based on ongoing clinical trials.

Research

Ongoing research is exploring the use of trastuzumab deruxtecan in other HER2-expressing cancers, including lung cancer and colorectal cancer. Clinical trials are also investigating its efficacy in combination with other therapies.

Related pages

• Monoclonal antibody therapy
• HER2/neu
• Breast cancer treatment

Structure of trastuzumab deruxtecan