The Effects of the Proton Pump Inhibitor Esomeprazole on the Bioavailability of Regorafenib
Status:
Completed
Trial end date:
2018-02-01
Target enrollment:
Participant gender:
Summary
Regorafenib is a novel oral multi-kinase inhibitor which targets angiogenic, stromal and
oncogenic receptor tyrosine kinases. It is currently registered for GIST and mCRC. When
regorafenib is co-administered with an acid suppressive agent, the intra-gastric pH
increases, and as a result the equilibrium of ionized/non-ionized regorafenib may shift to
the less soluble non-ionized form which reduces regorafenib bioavailability and exposure.
Since proton pump inhibitors (PPIs) are often used during regorafenib therapy, this drug-drug
interaction (DDI) confronts pharmacists and oncologists with challenges in clinical practice.
In this study the investigators will therefore evaluate the impact of PPI-induced
intra-gastric pH elevation on regorafenib pharmacokinetics in patients with GIST and mCRC.