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Giredestrant is an investigational oral selective estrogen receptor degrader (SERD) being developed for the treatment of estrogen receptor-positive (ER+) breast cancer. [1] [2] It is a potent, nonsteroidal compound that antagonizes estrogen effects by competitively binding to both wild-type and mutant estrogen receptors with nanomolar potency.
Another receptor that often plays a role in breast cancer, although it is not a hormone receptor, is the human epidermal growth factor receptor 2 (HER2). The overexpression of HER2 is determined by immunohistochemistry (IHC), or with fluorescent in situ hybridization in those equivocal cases where IHC does not provide a clear result.
Fulvestrant, sold under the brand name Faslodex among others, is an antiestrogenic medication used to treat hormone receptor (HR)-positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced breast cancer in combination with abemaciclib or palbociclib in women with disease progression after endocrine therapy. [2]
The mechanism of action of SERDs involves binding to the estrogen receptor, leading to a conformational change that facilitates recruitment of cellular machinery to degrade the receptor protein. By promoting degradation of the estrogen receptor, SERDs effectively inhibit estrogen signaling within cancer cells, thereby suppressing tumor growth.
Imlunestrant is an experimental selective estrogen receptor degrader developed by Eli Lilly and Company for the treatment of some types of breast cancer. [ 1 ] [ 2 ] [ 3 ] References
Vepdegestrant is an experimental estrogen receptor degrader that works via proteolysis targeting chimera. It is developed for advanced estrogen receptor positive breast cancer. [ 1 ] [ 2 ]
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