Airuikang Dalpiciclib Isethionate Tablets

1. Indications and Usage
Combination with Aromatase Inhibators: Indicated in combination with an aromatase inhibitor for the initial endocrine-based treatment of patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer.
Combination with Fulvestrant: Indicated in combination with fulvestrant for the treatment of patients with HR-positive, HER2-negative locally advanced or metastatic breast cancer with disease progression following endocrine therapy.
2. Dosage and Administration
Route of Administration: Oral administration.
Recommended Dosage: 150 mg orally once daily.
Administration Details: Administer at approximately the same time each day. The patient must fast for 1 hour before and 1 hour after taking the dose.
Schedule: Take continuously for 21 days, followed by a 7-day break, constituting a 28-day cycle. If a dose is missed, do not make up the dose on the same day; resume with the next scheduled dose.
3. Mechanism of Action
CDK4/6 Inhibition: Dalpiciclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6).
Cell Cycle Blockade: It inhibits the phosphorylation of the retinoblastoma protein (Rb) downstream of CDK4/6 signaling, inducing G1 phase cell cycle arrest and thereby inhibiting the proliferation of Rb-positive tumor cells.
4. Safety and Warnings
Neutropenia: Severe neutropenia is very common based on clinical trial data. Complete blood counts (CBC) must be monitored before starting, at the beginning of each cycle, and on day 15 of the first two cycles.
Embryo-Fetal Toxicity: Can cause fetal harm. Effective contraception is required for females during treatment and for 1 week after the final dose, and for males with female partners during treatment and for 3 months after.
Hepatic and Renal Impairment: The safety and efficacy in patients with moderate or severe hepatic or renal impairment have not been established.
QT Prolongation: Monitor electrocardiogram (ECG) in patients with risk factors for arrhythmias.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Neutrophil count decreased, leukopenia, anemia, thrombocytopenia, fatigue, nausea, musculoskeletal pain, and rash.
Clinical Research Highlights: Clinical trials (e.g., SHR6390-III-301, III-302) demonstrated significant improvements in progression-free survival when used in combination with endocrine therapies.
6. Drug Interactions
CYP3A4 Inhibitors: Strong CYP3A4 inhibitors should be avoided during treatment. If co-administration is necessary, consider withholding dalpiciclib.
CYP3A4 Inducers: Strong CYP3A4 inducers should be avoided as they may reduce the efficacy of dalpiciclib.
P-gp/Middle-Sensitive Substrates: Caution is advised when co-administering sensitive substrates of P-gp or other transporters.
7. Pharmaceutical Information
Chemical Composition: Active ingredient: Dalpiciclib (as Isethionate).
Appearance: White film-coated tablets.
Packaging: Available in 125 mg strength in blister packs.
Storage: Store at controlled room temperature; protect from moisture.