What is Abemaciclib, what does it treat, and how effective is its treatment
Abemaciclib is an oral CDK4/6 inhibitor, which is mainly used for the treatment of advanced or metastatic breast cancer with hormone receptor positive (HR+) and human epidermal growth factor receptor negative (HER2-), and plays an anti-tumor role by blocking cell cycle progression. Its efficacy has been validated in multiple clinical trials, particularly showing significant survival benefits for patients who have failed endocrine therapy.
1. Basic information of drugs
(1) Drug category: Selective cyclin dependent kinase 4/6 (CDK4/6) inhibitor, which inhibits tumor cell proliferation by blocking Rb protein phosphorylation.
(2) Research and Development Background: Developed by Eli Lilly and Company, it was approved for market by the FDA in 2017 and has been approved for use in multiple countries around the world.
2. Main therapeutic indications
(1) Combined endocrine therapy: combined with aromatase inhibitor or fluoxetine to treat HR+/HER2 postmenopausal advanced breast cancer.
(2) Monotherapy: used for patients with metastatic breast cancer who have received endocrine therapy and chemotherapy before.
3. Clinical treatment effect
(1) Progression free survival: The MONARCH-2 study showed a median PFS of 16.4 months with the combination of fluvoxetine, which was 7.1 months higher than the control group.
(2) Overall survival benefit: The MONARCH-3 trial confirmed that the combination of letrozole extended OS to 46.7 months and reduced the risk of death by 31%.
(3) Objective response rate: The ORR of monotherapy is 19.7%, while the ORR of combination therapy can reach 48.1%.
4. Special treatment advantages
(1) Continuous inhibition: Twice daily administration can maintain a stable CDK4/6 inhibitory effect.
(2) Central infiltration: Its unique pharmacokinetic properties may have certain therapeutic effects on brain metastases.
(3) Tolerance: Diarrhea is the main dose limiting toxicity, but most are grade 1-2 manageable adverse reactions.
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