Trastuzumab deruxtecan: Difference between revisions

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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==
[[File:Trastuzumab_deruxtecan.svg|thumb|right|Chemical structure of Trastuzumab Deruxtecan]]
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==
'''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.
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.


==Adverse Effects==
=== Mechanism of Action ===
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 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.


==Approval==
=== Clinical Use ===
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.
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]].


==Conclusion==
=== Side Effects ===
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.
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.
 
== Related Pages ==
* [[Monoclonal antibody therapy]]
* [[HER2/neu]]
* [[Breast cancer treatment]]
* [[Antibody-drug conjugate]]
 
{{Antineoplastic agents}}


[[Category:Cancer treatments]]
[[Category:Monoclonal antibodies]]
[[Category:Monoclonal antibodies]]
[[Category:Breast cancer]]
[[Category:Antineoplastic drugs]]
 
[[Category:HER2-targeted therapies]]
{{Medicine-stub}}

Latest revision as of 16:31, 16 February 2025

Trastuzumab Deruxtecan[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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.

Related Pages[edit]