Kisqali Ribociclib Succinate Film coated Tablets

1. Indications and Usage
HR+/HER2- Advanced or Metastatic Breast Cancer:
Indicated for the treatment of pre/perimenopausal and postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer.
Combination Therapy:
In combination with an aromatase inhibitor as initial endocrine-based therapy.
In combination with fulvestrant in patients with disease progression following endocrine therapy.
2. Dosage and Administration
Recommended Dosage:
Dose: 600 mg (three 200 mg tablets) orally once daily.
Cycle: Continue for 21 consecutive days, followed by a 7-day rest period (28-day cycle).
Administration: Administer with or without food at approximately the same time each day (preferably in the morning). Swallow tablets whole; do not crush, split, or chew.
Monitoring:
Perform complete blood counts (CBC) and liver function tests (LFTs) prior to starting treatment and monitor periodically. Obtain an ECG prior to initiation.
3. Mechanism of Action
CDK4/6 Inhibition:
Ribociclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6).
Cell Cycle Arrest:
CDK4/6 bind to cyclin D1 to phosphorylate the retinoblastoma protein (Rb), leading to cell cycle progression. Ribociclib inhibits this phosphorylation, resulting in G1 phase cell cycle arrest and suppression of tumor cell proliferation.
4. Safety and Warnings
QTc Prolongation:
Ribociclib can prolong the QT interval. It is contraindicated in patients with congenital long QT syndrome. ECG monitoring is required.
Severe Neutropenia:
Severe neutropenia (Grade 3 or 4) is a common adverse reaction. Monitor CBC regularly.
Hepatobiliary Toxicity:
Increases in transaminases (AST/ALT) have been observed. Monitor LFTs regularly.
Pulmonary Toxicity:
Interstitial lung disease (ILD)/pneumonitis has been reported. Monitor for pulmonary symptoms.
5. Adverse Reactions
Most Common:
Nausea, fatigue/asthenia, diarrhea, headache, insomnia, vomiting, abdominal pain, and pyrexia.
Laboratory Abnormalities:
Neutropenia, leukopenia, lymphopenia, anemia, increased AST/ALT, increased creatinine.
6. Drug Interactions
Strong CYP3A Inhibitors:
Avoid concomitant use with strong CYP3A inhibitors (e.g., itraconazole, clarithromycin, ritonavir) as they significantly increase Ribociclib plasma concentrations.
CYP Substrates:
May increase exposure to CYP2D6 and P-gp substrates.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Ribociclib Succinate.
Storage:
Store at 20°C to 25°C (68°F to 77°F). Keep in the original package to protect from moisture.