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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Bruton's tyrosine kinase (BTK) inhibitors
orelabrutinib
L01EL04
Adult Dosing
- Mantle cell lymphoma (MCL): 150 mg orally once daily until disease progression or unacceptable toxicity
- Chronic lymphocytic leukemia (CLL) / Small lymphocytic lymphoma (SLL): 150 mg orally once daily until disease progression or unacceptable toxicity
- Hepatic impairment (mild/moderate): No adjustment needed; monitor closely
- Hepatic impairment (severe): Avoid use
- Renal impairment (mild to severe): No adjustment needed
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of adult patients with relapsed or refractory mantle cell lymphoma (MCL) who have received at least one prior therapy
- Treatment of adult patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)
Mechanism of Action
- Small-molecule, highly selective covalent inhibitor of Bruton's tyrosine kinase (BTK)
- Forms a covalent bond with a cysteine residue (Cys481) in the BTK active site, leading to irreversible inhibition of BTK enzymatic activity
- Blocks B-cell receptor signaling pathways and inhibits malignant B-cell proliferation, trafficking, and adhesion
Contraindications
- Hypersensitivity to orelabrutinib or any of its excipients
Adverse Reactions
- Thrombocytopenia
- Neutropenia
- Anemia
- Infections (upper respiratory tract infection, pneumonia)
- Hemorrhage and bleeding events
- Atrial fibrillation and flutter
- Musculoskeletal pain
- Fatigue
- Diarrhea
- Second primary malignancies
Drug Interactions
- Strong CYP3A inhibitors (e.g., ketoconazole, clarithromycin): Avoid coadministration or reduce orelabrutinib dose if unavoidable
- Strong or moderate CYP3A inducers (e.g., rifampin, carbamazepine): Avoid coadministration as they may significantly decrease orelabrutinib plasma concentrations
- Anticoagulants and antiplatelet agents: Increased risk of bleeding; monitor closely for signs of hemorrhage
- Gastric acid-reducing agents (PPIs, H2-receptor antagonists): Generally well-tolerated due to high solubility, but monitor for altered absorption if coadministered
Curated Content: Needs Vetting Before Put to Clinical Use