Abemaciclib

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[ CAS NO. ] 1231929-97-7
[ Molecular Formula ] C27H32F2N8
[ Molecular Weight ] 506.606
[ Appearance ] Off-white to Yellow Powder

[ Function ]
1. Targeted inhibition of key proteins: Specifically blocks CDK4 and CDK6 proteins within cancer cells. These proteins play a regulatory role in the growth cycle of both healthy and cancerous cells.
2. Blocking the cell division process: Inhibiting CDK4/6 prevents cancer cells from entering the replication phase (S phase) from the growth phase (G1 phase), a critical step in cell division.
3. Inhibiting cancer cell proliferation: This prevents cancer cells from dividing and proliferating normally, ultimately leading to senescence or death (apoptosis).
4. Tumor shrinkage: In preclinical studies and clinical applications, abemaciclib, used alone or in combination with anti-estrogen drugs, has shown the ability to slow tumor growth and even shrink tumors.

[ Application ]
1. Used as initial endocrine therapy for postmenopausal women.
2. Used in patients who have failed endocrine therapy or whose tumors have progressed.
3. Suitable for patients whose condition has worsened after previous endocrine therapy and chemotherapy.

About Abemaciclib
Abemaciclib is a small-molecule targeted drug that works by selectively inhibiting the activity of CDK4/6 protein kinases. These kinases are responsible for regulating the transition of the cell cycle from the G1 phase to the S phase; their inhibition prevents cancer cell division. In 2017, the U.S. FDA approved it for the treatment of HR+/HER2- advanced breast cancer, and subsequent indications have gradually expanded to include adjuvant therapy for early-stage high-risk breast cancer.
Abemaciclib is primarily used to treat hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. It blocks cancer cell proliferation by inhibiting cyclin-dependent kinases 4/6 (CDK4/6) and is often used in combination with endocrine therapy to extend patients' progression-free survival.