Drug intelligence / Profile preview

omeprazole + taletrectinib

Development stage
Unknown
Lead developer
Nuvation Bio
Modality
Small Molecules
Administration
Oral
01

Overview

This combination refers to the co-administration of omeprazole, a proton pump inhibitor (PPI), and taletrectinib (AB-106), a next-generation, potent, and CNS-active tyrosine kinase inhibitor (TKI) targeting ROS1 and TRK fusions. The combination is primarily evaluated in clinical pharmacology studies to determine the effect of gastric pH elevation, induced by omeprazole, on the pharmacokinetics and bioavailability of taletrectinib. Taletrectinib is being developed by Nuvation Bio for the treatment of ROS1-positive non-small cell lung cancer (NSCLC) and other solid tumors, specifically designed to overcome resistance mutations such as ROS1 G2032R. Omeprazole is a widely used PPI that inhibits the H+/K+-ATPase enzyme system in gastric parietal cells.

Brand names
IBTROZIPrilosec
Other names
taletrectinibomeprazole
02

Targets

ROS1 (Proto-oncogene tyrosine-protein kinase ROS)Trk (Trk receptor family)CYP3A4 (Cytochrome P450 3A4)

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