Drug name: Trastuzumab emtansine


Related CSCTT Targets

ERBB2 [ref.1]P04626

Trastuzumab

Cas.no PubChem ID
180288-69-1
Known Target
Receptor tyrosine-protein kinase erbB-2P04626
Structure
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Introduction
Trastuzumab (Herclon, Herceptin) is a monoclonal antibody that interferes with the HER2/neu receptor. Its main use is to treat certain breast cancers. Used in the treatment of HER2-positive breast cancer. HER2 protein overexpression is observed in 25%-30% of primary breast cancers.Trastuzumab has been shown, in both in vitro assays and in animals, to inhibit the proliferation of human tumorcells that overexpress HER2. It is a mediator of antibody dependent cellular cytotoxicity, in that the binding of the antibody to HER2 overexpressing cells leads to preferential cell death.

Mertansine

Cas.no PubChem ID
11343137
Known Target
Structure
...
Introduction
Mertansine is a cytotoxic agent also known as DM1. It is a maytansinoid, linked via 4-mercaptovaleric acid with monoclonal antibodies. Trastuzumab emtansine (CAS: 1018448-65-1) is an antibody-drug conjugate consisting of the monoclonal antibody trastuzumab linked to the cytotoxic agent mertansine (DM1). The conjugate is abbreviated T-DM1. Trastuzumab alone stops growth of cancer cells by binding to the HER2/neu receptor, whereas mertansine enters cells and destroys them by binding to tubulin. Because the monoclonal antibody targets HER2, and HER2 is only over-expressed in cancer cells, the conjugate delivers the toxin specifically to tumor cells.

Reference

  • [1] Targeting of preexisting and induced breast cancer stem cells with trastuzumab and trastuzumab emtansine (T-DM1). Diessner, J., et al. (2014).Cell Death Dis.5:e1149.
    24675467. [ 24675467 ]

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