Abemaciclib is a kinase inhibitor that selectively inhibits cyclin dependent kinases 4 and 6 (CDK4/6), blocks the phosphorylation of Rb protein, and inhibits the transition of the cell cycle from G1 phase to S phase, inducing cell aging and apoptosis.

1、 Drug name

1. Common name: Abemaciclib;

2. Product Name: VERZENIO ™。

2、 Indications

1. The combination of fluoxetine and hormonal receptor (HR) positive, human epidermal growth factor receptor 2 (HER2) negative women with advanced or metastatic breast cancer is suitable for patients with disease progression after endocrine therapy.

2. The single drug therapy is applicable to adult patients with advanced or metastatic breast cancer with HR positive, HER2 negative, and is applicable to patients with disease progression after endocrine therapy and chemotherapy of metastatic diseases.

3、 Specifications and characteristics

1. Specification: 150mg

2. Appearance: Tablets

4、 Main components

Active ingredient: Abemaciclib, a CDK4/6 kinase inhibitor.

5、 Usage and dosage

1. Recommended dosage:

Combination Fluvustat: 150mg orally, twice daily.

Single drug treatment: 200mg orally, twice daily.

2. Medication method: Take the whole tablet orally, before or after meals.

3. Omission treatment: If missed, take according to the original time next time without the need for supplementation.

4. Vomiting treatment: If vomiting occurs after taking medication, there is no need to take additional medication.

6、 Dose adjustment

1. Diarrhea: Stop diarrhea treatment (such as loperamide) immediately upon the first appearance of loose stools. If the condition does not improve to ≤ grade 1 within 24 hours, discontinue administration.

2. Neutropenia:

Level 3: Pause until restored to ≤ Level 2.

Grade 4 or Recurrent Grade 3: Suspend and reduce dosage.

3. Hepatotoxicity: ALT/AST levels ≥ 3 should be paused and the dose reduced if sustained or repeated.

4. Other toxicities: Prolonged or recurrent grade 2 or ≥ 3 toxicities require a pause and dose reduction.

7、 Medication precautions

1. Diarrhea management: Start taking antidiarrheal medication and increasing fluid replacement as soon as loose stools appear for the first time.

2. Blood monitoring: Regular blood routine checks before and during treatment (every 2 weeks x 2 months, and every month x 2 months thereafter).

3. Liver function monitoring: Regularly check ALT/AST (frequency same as blood routine) before and during treatment.

4. Thrombosis risk: Be alert to symptoms of deep vein thrombosis or pulmonary embolism.

8、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal malformation.

2. Breastfeeding period: Stop taking medication or breastfeeding.

3. Liver dysfunction: Severe liver injury (Child Pugh C) requires reduction to once daily.

9、 Adverse reactions

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%).

10、 Contraindications

There are no clear contraindications.

11、 Drug interactions

1. Strong CYP3A4 inhibitors (such as ketoconazole): Avoid combination therapy, and reduce the dosage of other strong inhibitors.

2. Strong CYP3A4 inducers (such as rifampicin): Avoid combination use.

12、 Storage method

1. Storage temperature: 20-25 ° C (short-term 15-30 ° C allowed).

2. Keep the original packaging and avoid moisture.

Abemaciclibinformation