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TYK-00540 + fulvestrant is a combination therapy under clinical investigation for advanced or metastatic hormone receptor positive and HER2-negative breast cancer, particularly in patients who have progressed after prior endocrine therapy or are resistant to CDK4/6 inhibitors. TYK-00540 is a next-generation, highly potent, oral small molecule inhibitor targeting cyclin-dependent kinases 2, 4, and 6 (CDK2/4/6). Fulvestrant is a well-established selective estrogen receptor degrader (SERD) that inhibits estrogen signaling by binding, blocking, and inducing degradation of the estrogen receptor. The combination aims to provide synergistic inhibition of cell cycle progression and estrogen signaling, thus overcoming primary or acquired resistance to prior hormonal or CDK4/6 targeted therapies. TYK-00540 is independently developed by TYK Medicines, Inc.
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