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omeprazole + taletrectinib
- Development stage
- Phase 1
- 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.
- Other names
- taletrectinibomeprazole
02
Targets
Trk (Trk receptor family)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK1 (Tropomyosin-related receptor kinase A)NTRK3 (Tropomyosin receptor kinase C)ATP4A (Potassium–transporting ATPase alpha chain 1)
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