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Netazepide is a promising new medical treatment for type 1 gastric carcinoids

Treatment of gastric carcinoids type 1 with the gastrin receptor antagonist netazepide results in regression of tumours and normalization of serum chromogranin A, reports the most recent issue of the Alimentary Pharmacology & Therapeutics.

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Patients with chronic atrophic gastritis have long-term gastric hypoacidity, and secondary hypergastrinemia.

Some also develop gastric ECL cells carcinoids.

Most type 1 gastric carcinoids remain indolent, but some metastasise.

Patients undergo surveillance, and some are treated with somatostatin analogues, endoscopic resection or surgery.

Gastrin remained unchanged throughout treatment
Alimentary Pharmacology & Therapeutics

Netazepide (YF476) is a highly selective, potent and orally active gastrin receptor antagonist, which has anti-tumor activity in various rodent models of gastric neoplasia driven by hypergastrinemia.

Netazepide has been studied in healthy volunteers.
 
Dr Fossmark and colleagues from Norway assessed the effect of netazepide on type 1 gastric carcinoids.
 
The team reported that 8 patients with multiple type 1 gastric carcinoids received oral netazepide once daily for 12 weeks, with follow-up at 12 weeks in an open-label, pilot trial.

Upper endoscopy was performed at 0, 6, 12 and 24 weeks, and carcinoids were counted and measured.

Fasting serum gastrin and chromogranin A (CgA) and safety and tolerability were assessed at 0, 3, 6, 9, 12 and 24 weeks.
 
Netazepide was well tolerated.

The research team observed that all patients had a reduction in the number and size of their largest carcinoid.

CgA was reduced to normal levels at 3 weeks and remained so until 12 weeks, but had returned to pre-treatment levels at 24 weeks.

The team noted that gastrin remained unchanged throughout treatment.
 
Dr Fossmark's team concluded, "The gastrin receptor antagonist netazepide is a promising new medical treatment for type 1 gastric carcinoids, which appear to be gastrin-dependent."

"Controlled studies and long-term treatment are justified to find out whether netazepide treatment can eradicate type 1 gastric carcinoids."

Aliment Pharmacol Ther 2012: 36(12): 1067-1075
13 November 2012

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