Drug intelligence / Profile preview

ibrutinib + omeprazole

Development stage
Unknown
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of **ibrutinib** and **omeprazole** is primarily utilized in clinical pharmacology and drug-drug interaction (DDI) studies. Ibrutinib is a first-in-class, irreversible inhibitor of **Bruton's tyrosine kinase (BTK)**, used to treat various B-cell malignancies. Omeprazole is a **proton pump inhibitor (PPI)** that increases gastric pH. Because ibrutinib exhibits pH-dependent solubility—being more soluble at lower pH—co-administration with acid-reducing agents like omeprazole can significantly alter its pharmacokinetics. Clinical studies have demonstrated that omeprazole can reduce the peak plasma concentration (Cmax) and the area under the curve (AUC) of ibrutinib. These investigations are critical for establishing clinical guidelines regarding the use of PPIs in patients receiving ibrutinib therapy, often concluding that while exposure is reduced, the interaction may not necessitate dose adjustments in all clinical settings, though monitoring or alternative acid-reducing strategies may be considered.

Brand names
Imbruvica + PrilosecImbruvica + Losec
Other names
ibrutinib and omeprazoleibrutinib/omeprazole
02

Targets

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

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