Abstract
The experience of synthesising a novel gastrin receptor antagonist gastrazole and
taking it into 3 small clinical studies in pancreatic cancer in man is described.
The need for such a compound is illustrated by the observation that inhibition of
gastric acid secretion by H2 receptor antagonists results in hypergastrinaemia. A
large number of cell types have gastrin receptors including pancreatic cancer cells
which have been shown to be stimulated by gastrin. Small numbers of pancreatic cancer
patients given gastrazole by continuous intravenous infusion showed prolonged survival
compared with best supportive care or placebo, and equivalent survival to those given
5 fluouracil. The results suggest a greater benefit for patients with early stage
disease. An alternative gastrin receptor antagonist YF 476 is also described which
has the advantage of efficacy given by the oral route. This new compound requires
to be studied in pancreatic cancer and other diseases associated with hypergastrinaemia.
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Article info
Publication history
Published online: January 09, 2009
Accepted:
November 18,
2008
Received:
November 18,
2008
Identification
Copyright
© 2008 Elsevier Ltd. Published by Elsevier Inc. All rights reserved.
