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Abemaciclib is a kinase inhibitor that selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4/6) and blocks the phosphorylation of Rb protein, thereby inhibiting the transition of the cell cycle from the G1 phase to the S phase and inducing cell senescence and apoptosis.
1. Generic name: Abemaciclib;
2. Trade name: VERZENIO™.
1. Combined with fulvestrant to treat female patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. It is suitable for patients with disease progression after endocrine therapy.
2. Monotherapy for adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer. It is suitable for patients with disease progression after endocrine therapy and chemotherapy for metastatic disease.
1. Specifications: 150mg
2. Properties: Tablets
Active ingredient: Abemaciclib, a CDK4/6 kinase inhibitor.
1. Recommended dosage:
Combined with fulvestrant: 150 mg orally, twice a day.
Monotherapy: 200 mg orally, twice daily.
2. How to take the medicine: Swallow the whole tablet before or after meals.
3. Treatment of missed doses: If you miss a dose, take it at the original time next time, no need to make up for it.
4. Treatment of vomiting: If you vomit after taking the medicine, there is no need to take more.
1. Diarrhea : Start antidiarrheal treatment (such as loperamide) when loose stools appear for the first time. If the diarrhea is not relieved to level ≤ 1 within 24 hours, the administration must be suspended.
2. Neutropenia :
Grade 3: Suspend until recovery to ≤Grade 2.
Grade 4 or recurrent grade 3: Withhold and reduce dose.
3. Hepatotoxicity : If ALT/AST is persistent or repeated ≥ grade 3, it is necessary to suspend and reduce the dose.
4. Other toxicities : Persistent or recurrent grade 2 or ≥ grade 3 toxicity requires suspension and dose reduction.
1. Diarrhea management : Start antidiarrheal drugs and increase fluid replenishment when loose stools occur for the first time.
2. Blood monitoring : Regularly check blood routine before treatment and during treatment (every 2 weeks × 2 months, and every month × 2 months thereafter).
3. Liver function monitoring : Check ALT/AST regularly before and during treatment (the frequency is the same as blood routine).
4. Risk of thrombosis : Be alert to symptoms of deep vein thrombosis or pulmonary embolism.
1. Pregnant women : Contraindicated as it may cause fetal malformation.
2. During lactation : Discontinue medication or stop breastfeeding.
3. Liver insufficiency : Severe liver damage (Child-PughC) needs to be reduced to once a day.
1. Common (≥20%): Diarrhea (86%), neutropenia (46%), nausea (45%), fatigue (46%), infection (43%), anemia (29%), etc.
2. Serious reactions: Neutropenic fever (1%), hepatotoxicity (ALT/AST elevation), venous thrombosis (5%).
There are no clear contraindications.
1. Strong CYP3A4 inhibitors (such as ketoconazole) : Avoid combined use, and the dosage of other strong inhibitors needs to be reduced.
2. Strong CYP3A4 inducer (such as rifampin) : Avoid combined use.
1. Storage temperature: 20-25°C (short-term 15-30°C allowed).
2. Keep the original packaging and avoid moisture.