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Endocrine treatment may be beneficial for patients with hormone receptor positive breast tumors. [5] There are two ways for treating these kind of tumors: Lowering systemic levels of estrogen, achieved by the use of drugs from the aromatase inhibitor category. [6] [7] These drugs target one of the enzymes that takes part in the biosynthesis of ...
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.
If a patient with ER+ breast cancer develops endocrine resistance, the endocrine therapy used to treat the cancer will no longer be effective. Approximately 30-50% of ER+ breast cancer patients will relapse as a result of endocrine resistance, proving it to be a predominant challenge in the treatment of ER+ breast cancer patients. [19]
Another remaining question surrounding CDK inhibitors as a therapy is if certain cancers will evade or be resistant to treatment. One study showed that 20% of the patients being treated for metastatic ER+ HER2-breast cancer did not respond at all to treatment with a CDK4/6 inhibitor due to preexisting mutations allowing the cancer cells to continue proliferating despite treatment with the drug ...
Palazestrant is an investigational new drug which is being evaluated for the treatment of estrogen receptor-positive (ER+) breast cancer, with a dual mechanism of action as both a complete estrogen receptor antagonist (CERAN) and a selective estrogen receptor degrader (SERD). This orally bioavailable small molecule has demonstrated potent ...
[4] [5] The first clinical study of vosilasarm, a small (n=22) phase 1 study in women with metastatic breast cancer, was started in 2017 and completed in 2020, with results published in 2019, 2020, and 2022. [10] [3] [2] [17] [15] As of March 2023, vosilasarm is in phase 1/2 clinical trials for the treatment of breast cancer. [4] [18]
Staging breast cancer is the initial step to help physicians determine the most appropriate course of treatment. As of 2016, guidelines incorporated biologic factors, such as tumor grade, cellular proliferation rate, estrogen and progesterone receptor expression, human epidermal growth factor 2 (HER2) expression, and gene expression profiling into the staging system.
Tamoxifen is currently first-line treatment for nearly all pre-menopausal women with hormone receptor-positive breast cancer. [1] Raloxifene is another partial agonist SERM which does not seem to promote endometrial cancer, and is used primarily for chemoprevention of breast cancer in high-risk individuals, as well as to prevent osteoporosis. [1]
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