Datopotamab deruxtecan: Difference between revisions

Latest revision as of 21:21, 5 March 2025

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]

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]

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]

The primary focus of datopotamab deruxtecan's development is for cancers that express TROP2. These include:

Safety and Side Effects[edit]

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]

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.

Related pages[edit]

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-{{Short description|Antibody-drug conjugate for cancer treatment}}
+{{Short description|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]]. The drug is currently undergoing clinical trials to evaluate its efficacy and safety in treating [[solid tumors]].
+'''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==
-Datopotamab deruxtecan is composed of a humanized monoclonal antibody targeting [[TROP2]] (trophoblast cell-surface antigen 2), which is a protein overexpressed in several types of cancer cells. The antibody is linked to a cytotoxic agent, deruxtecan, which is a topoisomerase I inhibitor. This linkage is achieved through a cleavable tetrapeptide-based linker.
+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.
-[[File:Deruxtecan_ADCs.svg|thumb|right|Diagram of Deruxtecan ADCs]]
+==Development and Clinical Trials==
+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.
-Upon binding to TROP2 on the surface of cancer cells, the ADC is internalized, and the linker is cleaved, releasing the cytotoxic agent inside the cell. The released deruxtecan then inhibits topoisomerase I, leading to DNA damage and ultimately cell death. This targeted delivery allows for higher concentrations of the cytotoxic agent to be delivered directly to cancer cells, minimizing damage to normal tissues.
+==Potential Indications==
+The primary focus of datopotamab deruxtecan's development is for cancers that express TROP2. These include:
-==Clinical Development==
+* [[Breast cancer]]
-Datopotamab deruxtecan is being evaluated in several clinical trials for its potential to treat different types of cancers, including [[breast cancer]], [[non-small cell lung cancer]] (NSCLC), and [[triple-negative breast cancer]] (TNBC). The drug has shown promise in early-phase trials, demonstrating significant antitumor activity and a manageable safety profile.
+* [[Non-small cell lung cancer]]
+* [[Gastric cancer]]
+* [[Prostate cancer]]
-===Breast Cancer===
+==Safety and Side Effects==
-In patients with breast cancer, particularly those with TNBC, datopotamab deruxtecan is being studied for its ability to target TROP2-expressing tumors. TNBC is a subtype of breast cancer that lacks [[estrogen receptor]], [[progesterone receptor]], and [[HER2/neu]] expression, making it difficult to treat with traditional hormone therapies.
+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.
-===Non-Small Cell Lung Cancer===
+==Future Directions==
-For NSCLC, datopotamab deruxtecan is being tested in patients with advanced or metastatic disease. NSCLC is the most common type of lung cancer, and new treatment options are needed for patients who have progressed on standard therapies.
+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.
-==Safety and Efficacy==
+==Related pages==
-The safety profile of datopotamab deruxtecan is being closely monitored in clinical trials. Common adverse effects observed include nausea, fatigue, and decreased appetite. Serious adverse events are also being evaluated to ensure the drug's safety for future use.
-==Related Pages==
 * [[Antibody-drug conjugate]]
 * [[TROP2]]
 * [[Topoisomerase inhibitor]]
-* [[Breast cancer]]
+* [[Cancer treatment]]
-* [[Non-small cell lung cancer]]
+[[File:Deruxtecan_ADCs.svg|Diagram of Deruxtecan ADCs|thumb|right]]
 [[Category:Antibody-drug conjugates]]
 [[Category:Experimental cancer drugs]]