Trastuzumab deruxtecan: Difference between revisions

Revision as of 15:48, 9 February 2025

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

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-'''Trastuzumab deruxtecan''' (also known as DS-8201) is a [[monoclonal antibody]] drug conjugate used in the treatment of certain types of [[breast cancer]]. It is specifically designed for the treatment of patients with [[HER2-positive]] breast cancer that is unresectable or metastatic and who have received two or more prior anti-HER2-based regimens in the metastatic setting. Trastuzumab deruxtecan combines a HER2-targeted antibody, similar to trastuzumab, with a cytotoxic drug, allowing for the direct delivery of the chemotherapy to the cancer cells while minimizing exposure to the rest of the body.
+== Trastuzumab deruxtecan ==
-==Mechanism of Action==
+'''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]].
-Trastuzumab deruxtecan works through a dual mechanism. Firstly, the trastuzumab component binds to the HER2 protein on the surface of cancer cells. HER2 is overexpressed in some breast cancer cells, promoting their growth. By binding to HER2, trastuzumab can inhibit the proliferation of these cancer cells. Secondly, once bound, the conjugate is internalized by the cancer cell, where the cytotoxic agent (deruxtecan) is released. Deruxtecan induces DNA damage, leading to cell death. This targeted approach allows for the delivery of high concentrations of chemotherapy to the cancer cells with reduced systemic toxicity.
-==Clinical Trials==
+=== Mechanism of Action ===
-Clinical trials have demonstrated the efficacy of trastuzumab deruxtecan in patients with HER2-positive metastatic breast cancer. The pivotal phase II trial, known as DESTINY-Breast01, showed a significant improvement in overall response rate and progression-free survival in patients treated with trastuzumab deruxtecan compared to standard therapies. Further studies are ongoing to evaluate its effectiveness in other HER2-expressing cancers, including gastric and non-small cell lung cancers.
+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]].
-==Adverse Effects==
+=== Clinical Use ===
-The use of trastuzumab deruxtecan is associated with several potential adverse effects. The most common include nausea, fatigue, vomiting, alopecia, and constipation. More serious side effects can occur, including interstitial lung disease/pneumonitis, neutropenia, and left ventricular dysfunction. Patients receiving trastuzumab deruxtecan should be monitored for signs of these adverse effects, and treatment should be adjusted accordingly.
+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.
-==Approval==
+=== Side Effects ===
-Trastuzumab deruxtecan received accelerated approval from the [[U.S. Food and Drug Administration]] (FDA) in December 2019 for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens in the metastatic setting. This approval was based on the results of the DESTINY-Breast01 trial. Subsequent approvals in other jurisdictions have followed, reflecting its potential as a significant advancement in the treatment of HER2-positive breast cancer.
+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.
-==Conclusion==
+=== Development and Approval ===
-Trastuzumab deruxtecan represents a significant advancement in the treatment of HER2-positive breast cancer, offering hope to patients who have exhausted other treatment options. Its targeted mechanism of action allows for the delivery of potent chemotherapy directly to cancer cells, improving efficacy while reducing systemic side effects. Ongoing research and clinical trials will further elucidate its role in the treatment of other HER2-expressing cancers.
+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]]
+{{Reflist}}
+[[File:Trastuzumab_deruxtecan.svg|thumb|Structure of trastuzumab deruxtecan]]
-[[Category:Cancer treatments]]
 [[Category:Monoclonal antibodies]]
-[[Category:Breast cancer]]
+[[Category:Antineoplastic drugs]]
+[[Category:HER2-targeted therapy]]
-{{Medicine-stub}}