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Ribociclib is an oral tablet that is a cyclin-dependent kinase (CDK) 4/6 inhibitor. By selectively inhibiting CDK4/6 activity, it blocks the cell cycle from entering the S phase from G1 phase, thereby inhibiting the proliferation of tumor cells.
1. Generic name: Ribociclib
2. Trade name: Kisqali®
Combined with an aromatase inhibitor (such as letrozole) as initial endocrine therapy, it is used to treat postmenopausal women with hormone receptor (HR) positive and human epidermal growth factor receptor 2 (HER2) negative advanced or metastatic breast cancer.
1. Specifications : 200mg/tablet
2. Properties : Film-coated tablets
1. Active ingredient: Ribociclib succinate.
2. Excipients: Colloidal silica, crospovidone, hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose, etc.
1. Recommended dosage of : 600mg (3 tablets of 200mg) orally, once a day, for 21 consecutive days, followed by 7 days off (28 days is a cycle).
2. How to take : Can be taken with food or on an empty stomach. Swallow the tablet whole (do not chew, crush or split).
3. Combination medication : Needs to be used in combination with letrozole 2.5 mg once a day.
1. Neutropenia : Suspend or reduce the dose according to the grade (if grade ≥3, the treatment needs to be interrupted, and the dose needs to be downgraded after recovery).
2. Hepatotoxicity : ALT/AST>3×ULN is permanently discontinued when accompanied by elevated bilirubin; in other cases, reduce the dose as needed.
3. QT interval prolongation : Suspend and downgrade the dose when QTcF>500ms; if accompanied by arrhythmia symptoms, permanently discontinue the drug.
1. Missed dose/vomiting : If you miss a dose or vomit after taking the medicine, there is no need to take a supplement. Take the medicine at the originally planned time next time.
2. Dietary influence : Not affected by food, but avoid grapefruit, pomegranate and their products (may inhibit CYP3A4).
3. Other : During the medication period, electrocardiogram, liver function, and blood routine must be monitored regularly.
1. Patients with liver damage : Mild to moderate (Child-PughA/B) dosage should be reduced to 400mg/day, severe (Child-PughC) dosage should be used with caution.
2. Pregnancy/breastfeeding : It is embryotoxic and is contraindicated in pregnancy; the drug should be discontinued for at least 3 weeks during lactation.
3. Elderly : No need to adjust the dose.
1. Common (≥20%) : Neutropenia (75%), nausea (52%), fatigue (37%), diarrhea (35%), alopecia (33%).
2. Severe (>2%) : Grade 3/4 neutropenia (60%), elevated liver enzymes (8%), and prolonged QT interval (3%).
There are no absolute contraindications, but the combined use of strong CYP3A4 inhibitors/inducers and QT prolonging drugs should be avoided.
1. CYP3A4 inhibitor (such as ketoconazole): Avoid combined use. If combined use is necessary, reduce ribociclib to 400mg/day.
2. CYP3A4 substrate (such as midazolam): may increase its plasma concentration and the dose needs to be adjusted.
3. QT prolonging drugs (such as amiodarone): Avoid combined use.
It is not clearly stated. It is recommended to refer to conventional drug storage conditions (protect from light, dry, below 25℃).