Datopotamab deruxtecan
A novel antibody-drug conjugate for cancer treatment
Datopotamab deruxtecan is an investigational antibody-drug conjugate (ADC) designed for the treatment of various types of cancer. It is being developed by Daiichi Sankyo and AstraZeneca. This ADC is composed of a humanized anti-TROP2 monoclonal antibody linked to a topoisomerase I inhibitor payload, known as deruxtecan.
Mechanism of Action[edit | edit source]
Datopotamab deruxtecan targets the TROP2 protein, which is overexpressed in many epithelial cancers. The ADC binds to TROP2 on the surface of cancer cells, facilitating internalization of the conjugate. Once inside the cell, the linker is cleaved, releasing the cytotoxic deruxtecan, which inhibits topoisomerase I, leading to DNA damage and cell death.
Development and Clinical Trials[edit | edit source]
Datopotamab deruxtecan is currently undergoing clinical trials to evaluate its efficacy and safety in various cancer types, including breast cancer, non-small cell lung cancer (NSCLC), and triple-negative breast cancer (TNBC). Early-phase trials have shown promising results, with significant antitumor activity observed in patients with advanced solid tumors.
Potential Indications[edit | edit source]
The primary focus of datopotamab deruxtecan's development is for cancers that express TROP2. These include:
Safety and Side Effects[edit | edit source]
As with other ADCs, the safety profile of datopotamab deruxtecan is closely monitored. Common side effects observed in clinical trials include nausea, fatigue, and hematological toxicities. The risk of interstitial lung disease (ILD) is also a concern, as seen with other ADCs containing deruxtecan.
Future Directions[edit | edit source]
Ongoing research aims to optimize the use of datopotamab deruxtecan in combination with other therapies, such as immune checkpoint inhibitors and chemotherapy. The goal is to enhance its efficacy and broaden its application across different cancer types.
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