Netazepid

Structural formula
General
Non-proprietary name	Netazepid
other names	YF476; 1 - [(3 R ) -1- (3,3-dimethyl-2-oxobutyl) -2-oxo-5- (pyridin-2-yl) -2,3-dihydro-1 H -1,4-benzodiazepine -3-yl] -3- [3- (methylamino) phenyl] urea;
Molecular formula	C 28 H 30 N 6 O 3
External identifiers / databases
PubChem	9870520
ChemSpider	8046211
DrugBank	DB12355
Wikidata	Q2297773
Drug information
Drug class	Cytostatic
Mechanism of action	CCK-2 inhibitor
properties
Molar mass	498.585 g · mol -1
safety instructions
GHS hazard labeling ; no classification available
GHS hazard labeling ; no classification available
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Netazepid is a potential drug for the treatment of tumors of the gastrointestinal tract . It is made by the Japanese pharmaceutical company Yamanouchi Pharma Co. Ltd. developed. Netazepid is currently in the clinical trial .

Mechanism of action

Netazepid is an antagonist at the cholecystokinin 2 receptor, a gastrin receptor. Gastrin stimulates gastric acid - secretion directly through the stimulation of CCK-2 receptor of the gastric epithelial cells . The inhibition of CCK-2 receptors by netazepid inhibits gastric acid secretion. However, the histamine- dependent gastric acid secretion is not influenced. The approaches to treating tumors of the gastrointestinal tract with netazepid are based on the assumption that gastrin promotes tumor growth by means of CCK-2 receptors. The plasma half-life is around 8 hours.

literature

Agent for preventing or treating pancreas cancer, ovary cancer or liver cancer containing novel water-soluble prodrug. PCT Int. Appl. , 2007, 108pp
L. Evilevitch, BR. Weström and SG. Pierzynowski. CCK-B receptor antagonist YF476 inhibit spancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol , 39: 886-890, 2004
Y.Takinami, H.Yuki, A.Nishida, S.Akuzawa, A.Uchida, Y.Takemoto, M.Otha, M.Satoh, G.Semple, K.Miyata. YF476 is a new potent and selective gastrin / cholecystokinin-B receptor antagonist in vitro and in vivo. Alimentary Pharmacology and Therapeutics , 11 (1): 113-120, 1997

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[NV-1] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.