Drug intelligence / Profile preview

acalabrutinib + rabeprazole

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Acalabrutinib + rabeprazole refers to the combined administration of acalabrutinib, a potent, covalent **Bruton tyrosine kinase (BTK) inhibitor** used primarily in certain B-cell malignancies, with rabeprazole, a **proton pump inhibitor (PPI)** used to reduce gastric acid. This combination is clinically relevant due to prior concerns that acid-reducing agents (PPIs, antacids, H2 antagonists) could significantly reduce acalabrutinib exposure when administered in capsule form, but recent studies confirm that the **tablet formulation** of acalabrutinib can be co-administered with rabeprazole without clinically significant alteration in pharmacokinetics, efficacy, or safety. Acalabrutinib acts by irreversibly inhibiting BTK in B-cells, thereby blocking B-cell activation, proliferation, and survival pathways. Rabeprazole increases gastric pH by inhibiting the proton pump in gastric parietal cells.

Other names
acalabrutinib maleate tablet + rabeprazoleacalabrutinib capsule + rabeprazole
02

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)BTK (Bruton tyrosine kinase)

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