Trastuzumab emtansine

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A drug used in cancer treatment


Trastuzumab emtansine
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Trastuzumab emtansine, also known as ado-trastuzumab emtansine, is a monoclonal antibody used in the treatment of HER2-positive breast cancer. It is a conjugate of the monoclonal antibody trastuzumab and the cytotoxic agent DM1, a derivative of maytansine.

Mechanism of action

Trastuzumab emtansine works by targeting the HER2 receptor, which is overexpressed in some breast cancer cells. The trastuzumab component binds to the HER2 receptor, inhibiting the proliferation of cancer cells. Once bound, the conjugate is internalized by the cancer cell, where the emtansine component is released, disrupting microtubule function and leading to cell death.

Clinical use

Trastuzumab emtansine is primarily used for the treatment of patients with HER2-positive metastatic breast cancer who have previously received trastuzumab and a taxane. It is administered intravenously and has been shown to improve progression-free survival and overall survival in clinical trials.

Side effects

Common side effects of trastuzumab emtansine include fatigue, nausea, muscle pain, and thrombocytopenia. Serious side effects can include liver toxicity, heart problems, and lung disease. Patients are monitored for these adverse effects during treatment.

Approval and regulation

Trastuzumab emtansine was approved by the FDA in 2013 for the treatment of HER2-positive metastatic breast cancer. It is marketed under the brand name Kadcyla.

Research and development

Ongoing research is exploring the use of trastuzumab emtansine in other types of HER2-positive cancers and in combination with other therapies. Clinical trials are investigating its efficacy in earlier stages of breast cancer and in combination with other targeted therapies.

Related pages

References


Trastuzumab emtansine

  • Trastuzumab emtansine

  • Emtansine mab structure

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Contributors: Prab R. Tumpati, MD