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nastorazepide

Development stage: Phase 2
Lead developer: Japan Tobacco
Modality: Small Molecules
Administration: Oral

Overview

Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine derivative that acts as a gastrin/cholecystokinin 2 (CCK-2) receptor antagonist. By binding to the gastrin/CCK-2 receptor, it prevents activation by gastrin—a peptide hormone associated with the proliferation of gastrointestinal and pancreatic tumor cells. This mechanism confers potential antitumor and antineoplastic activity. The drug has been investigated primarily for advanced pancreatic cancer in combination with gemcitabine chemotherapy. Clinical trials have shown it to be safe and well tolerated with some evidence of improved pain control and quality of life when combined with gemcitabine. It is still under clinical development for this indication.

Other names: nastorazepide calcium

Targets

CCK2R (Cholecystokinin 2 Receptor)

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