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TFX06 is a novel, next-generation oral selective estrogen receptor degrader (SERD) and complete estrogen receptor antagonist (CERAN) in clinical development for the treatment of estrogen receptor positive (ER+), human epidermal growth factor receptor 2 negative (HER2-) advanced or metastatic breast cancer. TFX06 acts by potently antagonizing and degrading estrogen receptor alpha (ERα), including both wild-type and mutant forms associated with resistance to endocrine therapy. Preclinical studies have shown that TFX06 inhibits proliferation of ER+ breast cancer cells and demonstrates antitumor activity as a single agent, as well as synergistic effects when combined with palbociclib. In vivo models indicate it does not exhibit agonist activity on uterine tissue. Early clinical data from phase 1/2 trials show favorable safety, pharmacokinetics, and preliminary evidence of extracranial and intracranial antitumor efficacy in patients previously treated with endocrine therapies or chemotherapy[1][2][3][4][5]. It is being developed by Shenzhen Yangli Pharma WuXi AppTec.
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