Drug interactions of Acalabrutinib

Strong CYP3A Inhibitors

Clinical Effect: Concomitant use of acalabrutinib with a strong CYP3A inhibitor (e.g., itraconazole) increases the plasma concentration of acalabrutinib. Increased acalabrutinib concentration may lead to increased toxicity.

Prevention or Management: Avoid concomitant use of strong CYP3A inhibitors with acalabrutinib. Alternatively, if the inhibitor will be used short-term, interrupt acalabrutinib therapy.

Moderate CYP3A Inhibitors

Clinical Effect: Concomitant use of acalabrutinib with a moderate CYP3A inhibitor may increase the plasma concentration of acalabrutinib. Increased acalabrutinib concentration may lead to increased toxicity.

Prevention or Management: When acalabrutinib is used concomitantly with a moderate CYP3A inhibitor, reduce the dose of acalabrutinib to 100 mg once daily.

Strong CYP3A Inducers

Clinical Effect: Concomitant use of acalabrutinib with a strong CYP3A inducer (e.g., rifampicin) decreases the plasma concentration of acalabrutinib. Decreased acalabrutinib concentration may reduce the activity of acalabrutinib.

Prevention or Management: Avoid concomitant use of strong CYP3A inducers with acalabrutinib. If use of a strong CYP3A inducer cannot be avoided, increase the dose of acalabrutinib to 200 mg approximately every 12 hours.

Acid-Reducing Agents

Clinical Effect: Concomitant use of acalabrutinib with proton pump inhibitors (PPIs), H2-receptor antagonists, or antacids may decrease the plasma concentration of acalabrutinib. Decreased acalabrutinib concentration may reduce the activity of acalabrutinib. If treatment with an acid-reducing agent is necessary, consider using an H2-receptor antagonist (e.g., ranitidine or famotidine) or an antacid (e.g., calcium carbonate).

Prevention or Management: Administer acalabrutinib and the acid-reducing agent at least 2 hours apart. Take acalabrutinib 2 hours before administering an H2-receptor antagonist.

Proton Pump Inhibitors (PPIs): Avoid concomitant use. Due to the long-lasting effect of PPIs, separating the administration times may not eliminate the interaction with acalabrutinib.

FDA，2025.01