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netazepide
- Development stage
- Phase 2
- Lead developer
- Trio Medicines
- Modality
- Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Netazepide is an orally active, small molecule, benzodiazepine-type, selective antagonist of the cholecystokinin B receptor (CCKBR; also known as CCK2R or gastrin receptor). It acts by competitively inhibiting the binding of gastrin and cholecystokinin to CCKBR on enterochromaffin-like (ECL) cells in the stomach lining. This inhibition reduces histamine release from ECL cells and subsequently decreases gastric acid secretion from parietal cells. Netazepide has demonstrated antiproliferative effects on ECL cells and can reduce or eradicate type 1 gastric neuroendocrine tumors (g-NETs) associated with hypergastrinaemia, such as those seen in autoimmune chronic atrophic gastritis. The drug has been investigated for indications including dyspepsia, hypergastrinaemia, Barrett's esophagus, ECL-cell hyperplasia, rebound hyperacidity, and especially for type 1 gastric NETs[1][2][3][4][5][6].
- Brand names
- Netazepide
- Other names
- sograzepide
02
Targets
CCK2R (Cholecystokinin 2 Receptor)
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