• Journal of Pharmaceutical Investigation
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• v.34 no.6
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• pp.459-463
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• 2004

CR 2945, a $gastrin/CCK_B$ receptor antagonist, was conjugated to liposome and tested for the targeting of pancreatic cancer cells in vitro. Successful conjugation was confirmed by FTIR and NMR. The size of CR 2945-conjugated liposome was about 500 nm in diameter, with the zeta-potential being -16.5 mV. In vitro anti-cancer activity of this formulation with or without gemcitabine encapsulated was tested on human pancreatic cancer cells, PANC-1. The growth inhibitory effect of gemcitabine-encapsulating CR 2945-conjugated liposome was found to be 10-fold more potent than that of gemcitabine-encapsulating non-conjugated liposome, suggesting that CR 2945 could be used as a potential cancer targeting moiety by conjugating into liposome.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.416.3-417
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• 2002

Among the promising cancer therapy is targeting of the drug to tumor cells via receptor specific ligands. CR2945, $\beta$-2-( ［2-(8-azaspiro ［4.5］ dec-8-ylcarbony!)-4.6-dimethylphenyl］amino-2-oxoethyl］ -(R)-1-naphthalenepropanoic acid. is known to have an inhibitory effect on a gastrin receptor of colorectal cancer cells. As the human pancreatic cancer cells (BxPC-3) express gastrin receptors. interruption of binding of gastrin with gastrin receptor of human pancreatic cancer cells by CR2945 inhibits the growth of human pancreatic cancer cells. (omitted)