Yinuokai Orelabrutinib Tablets

1. Indications and Usage
Mantle Cell Lymphoma (MCL):
Indicated for the treatment of adult patients with MCL who have received at least one prior therapy.
Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL):
Indicated for the treatment of adult patients with CLL/SLL who have received at least one prior therapy.
2. Dosage and Administration
Route of Administration:
Oral Use ONLY.
Recommended Dosage:
Dose: 150 mg (three 50 mg tablets) administered orally once daily.
Duration: Continue until disease progression or unacceptable toxicity.
Administration Instructions:
Swallow tablets whole with water; do not split, crush, or chew.
Can be taken with or without food.
Maintain a fixed dosing time each day.
Missed Dose:
If a dose is missed, take it as soon as possible within 8 hours prior to the next scheduled dose. Otherwise, skip the missed dose and resume at the regular schedule. Do not take extra tablets to make up for a missed dose.
3. Mechanism of Action
BTK Inhibition:
Orelabrutinib is a next-generation, highly selective BTK inhibitor.
Immunomodulation:
It covalently binds to cysteine-481 in the ATP binding pocket of BTK, blocking B-cell antigen receptor (BCR) signaling pathways, which inhibits tumor cell proliferation and induces apoptosis.
4. Safety and Warnings
Bleeding Events:
Major hemorrhagic events, including fatal intracranial hemorrhage, have been reported. Monitor patients for signs of bleeding. Temporarily withhold prior to surgery.
Infections:
May cause severe and fatal infections (e.g., pneumonia). Monitor for signs of infection.
Cytopenias:
Grade ≥ 3 neutropenia, thrombocytopenia, and anemia have been observed. Monitor complete blood counts regularly.
Arrhythmias:
Atrial fibrillation and flutter have been reported. Monitor patients with cardiac history.
Hepatic Impairment:
Contraindicated in patients with severe hepatic impairment.
5. Adverse Reactions
Most Common:
Upper respiratory tract infections, thrombocytopenia, neutropenia, anemia, hemorrhage (bruising, petechiae), rash, and fatigue.
6. Drug Interactions
CYP3A Modulators:
Orelabrutinib is primarily metabolized by CYP3A4. Avoid concomitant use with strong or moderate CYP3A4 inhibitors or inducers.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Orelabrutinib (50 mg per tablet).
Storage:
Store in the original package to protect from moisture. Store below 30°C.