Rujianing Lerociclib Hydrochloride Tablets

1. Indications and Usage
Investigational Use:
Lerociclib is an investigational drug being studied for the treatment of adults with solid tumors, including triple-negative breast cancer (TNBC) and other CDK4/6 pathway-driven malignancies.
Current Status:
Not currently approved for commercial use in the United States or the European Union.
2. Dosage and Administration
Recommended Dosage (Clinical Trial Context):
Standard Dose: The recommended dose in clinical trials has been 200 mg to 400 mgadministered orally once daily or twice daily, in combination with other agents (e.g., paclitaxel or endocrine therapy).
Note: Dosing schedules are subject to change based on Phase 2/3 trial protocols.
Administration Instructions:
Administer orally with or without food.
Swallow tablets whole; do not crush or chew.
3. Mechanism of Action
CDK4/6 Inhibitor:
Lerociclib is a potent, highly selective, and orally bioavailable inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6).
Physiological Effect:
It binds to the ATP-binding pocket of CDK4 and CDK6, inhibiting their activity. This prevents the phosphorylation of the retinoblastoma protein (pRb), leading to cell cycle arrest at the G1 phase and inhibition of tumor cell proliferation.
4. Safety and Warnings
Neutropenia:
Decreases in neutrophil counts have been observed. Monitor complete blood counts (CBC) prior to starting treatment and periodically during treatment. Dose reductions or interruptions may be required.
Fatigue and Asthenia:
Patients may experience significant fatigue.
Embryo-Fetal Toxicity:
Based on its mechanism of action, lerociclib can cause fetal harm when administered to a pregnant woman.
5. Adverse Reactions
Most Common (Based on Clinical Trials):
Neutropenia, leukopenia, fatigue, nausea, vomiting, diarrhea, decreased appetite, and hair color changes.
6. Drug Interactions
CYP3A Substrates:
Lerociclib is metabolized primarily by CYP3A4. Co-administration with strong CYP3A inhibitors (e.g., ketoconazole) or inducers (e.g., rifampin) may significantly alter lerociclib exposure.
7. Pharmaceutical Information
Chemical Description:
Lerociclib Hydrochloride is a small molecule selective CDK4/6 inhibitor.
Storage:
Store at controlled room temperature. Keep in the original package to protect from moisture.