On August 6, 2018, the National Medical Products Administration (NMPA) of China approved the listing of Pfizer's Pembrolizumab in China. This is the first approved CDK4/6 inhibitor in China and was included in the national medical insurance catalog in October 2021.

1、 Drug name

1. Common name: Palbociclib

2. Product Name: IBRANCE ®

2、 Indications

Combined letrozole is used to treat postmenopausal women with estrogen receptor (ER) positive and human epidermal growth factor receptor 2 (HER2) negative advanced breast cancer as the initial endocrine therapy for metastatic diseases.

3、 Specifications and characteristics

1. 125mg capsules: opaque hard capsules.

2. 100mg capsules: opaque hard capsules.

4、 Main components

Active ingredient: Pabosenil (chemical name: 6-Acetyl-8-Cyclopentyl-5-methyl-2- {[5- (piperazin-1-yl) pyridin-2-yl] amino} pyrido [2,3-d] pyrimidin-7 (8H) - one).

5、 Usage and dosage

1. Standard dose: 125mg once daily, taken continuously for 21 days, then discontinued for 7 days, forming a 28 day cycle. Should be taken with food.

2. Combination therapy: Letrozole 2.5mg should be taken simultaneously once daily.

6、 Dose adjustment

1. Hematological toxicity: When grade 3 neutropenia (accompanied by fever/infection) or grade 4 neutropenia occurs, administration should be suspended until it returns to ≤ grade 2, and subsequent doses should be reduced to 100mg or 75mg.

2. Non hematological toxicity: Grade 3 or above toxicity requires temporary suspension of administration and dose reduction after recovery.

3. Combination use of strong CYP3A inhibitors: The dosage should be reduced to 75mg once daily.

7、 Medication precautions

1. Medication time: Take together with food, swallow the whole pill, do not chew or open the capsule.

2. Missed/Vomiting: No need to take additional medication on the same day, follow the original plan for the next dose.

3. Dietary taboos: Avoid grapefruit and its products.

8、 Medication for special populations

1. Pregnancy/lactation: May cause fetal injury, contraception is necessary during treatment and 2 weeks after discontinuation of medication; Prohibited during lactation.

2. Liver/kidney dysfunction: Mild to moderate without adjustment, tablets are contraindicated for severe liver injury.

3. Elderly individuals: No special adjustments are required, but individualized monitoring is necessary.

9、 Adverse reactions

1. Common reactions (≥ 10%): Neutropenia (75%), leukopenia, fatigue, anemia, upper respiratory tract infection, nausea, stomatitis, hair loss, diarrhea, thrombocytopenia.

2. Serious reactions: Pulmonary embolism (5%), infection (5%), QT interval prolongation.

10、 Contraindications

There are no absolute contraindications, but it is contraindicated for individuals who are allergic to truncated ear canal drugs.

11、 Drug interactions

1. CYP3A strong inhibitors (such as ketoconazole): Avoid combination therapy and reduce to 75mg if necessary.

2. CYP3A strong inducers (such as rifampicin): Avoid combination therapy as it may reduce efficacy.

3. Sensitive CYP3A substrates (such as midazolam): dose reduction is required.

12、 Storage method

Store at room temperature between 20 ° C and 25 ° C, avoiding moisture and direct sunlight.

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