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Palazestrant is an investigational small molecule drug being developed for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. It acts as both a complete estrogen receptor antagonist (CERAN) and a selective estrogen receptor degrader (SERD), providing dual activity against both wild-type and mutant forms of the estrogen receptor. Palazestrant is orally bioavailable and has demonstrated promising clinical activity in combination with CDK4/6 inhibitors such as ribociclib and palbociclib. The drug has shown tumor responses, prolonged disease stabilization, and progression-free survival in patients previously treated with endocrine therapy plus CDK4/6 inhibitors[3][5][6].
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