Orelabrutinib – Chronic Lymphocytic Leukemia | DengYueMed

Orelabrutinib Application Scope

Orelabrutinib is an oral, highly selective, irreversible Bruton’s tyrosine kinase (BTK) inhibitor used in B‑cell malignancies.

Characteristics

• Ingredients: Orelabrutinib

• Properties:

  • Mechanism: Covalent, irreversible inhibition of BTK → blocks B‑cell receptor signaling and malignant B‑cell survival

  • Selectivity: High BTK specificity; minimal off‑target kinase activity

• Packaging Specification:

  • Typically supplied as film‑coated tablets

  • Strengths in clinical use: 50 mg, 80 mg, 100–150 mg (study‑dependent)

• Storage:

  • Store at room temperature (20–25 °C)

  • Protect from moisture and light (standard for oral BTK inhibitors)

• Expiry Date: As indicated on packaging, typically 24–36 months from manufacture (standard practice).

• Executive Standard:

  • Chinese NMPA approval standards (with Phase II/III clinical data)

  • Internationally held to ICH‑GCP guidelines in clinical trials

• Approval Number: NMPA-approved in China for CLL/SLL, MCL, MZL (2020)

  • Specific Chinese drug approval codes not found in the retrieved sources

• Date of Revision:

  • Major clinical updates published in 2023 for Waldenström’s macroglobulinemia;

  • Phase II MS data in 2023

• Manufacturer: InnoCare Pharma (developer in China)

Guidelines for the Use of Orelabrutinib

• Dosage and Administration:

  • Typical dosing in oncology studies: 150 mg once daily until disease progression or unacceptable toxicity

  • Doses of 50–100 mg QD used in autoimmune and MS studies

• Adverse Reactions:

  • Mostly grade 1–2;

    • Common events include neutropenia, thrombocytopenia, and pneumonia

    • Liver enzyme elevations, atrial fibrillation, and mild liver dysfunction

  • Serious AEs in ~8.5%; treatment discontinuation in ~6–8%

• Contraindications:

  • Known hypersensitivity to orelabrutinib or excipients

  • Use caution or avoidance with strong CYP3A inhibitors or inducers

• Precautions:

  • Monitor CBC, liver function, ECG (for atrioventricular effects), infections

  • Use contraception during treatment and for a period after

  • Adjust dose or interrupt in case of AEs such as cytopenias or atrial arrhythmias

Orelabrutinib Interactions

• Drug Interactions:

  • Substrate of CYP3A; avoid strong CYP3A inducers/inhibitors

  • Monitor for altered exposure with co‑administered drugs

Note:

• If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
• It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.