Gastrin receptor antagonist CI-988 inhibits growth of human colon cancer in vivo and in vitro

Aust N Z J Surg. 1996 Apr;66(4):235-7. doi: 10.1111/j.1445-2197.1996.tb01173.x.


Background: Whilst gastrin has been found to be trophic for some colorectal cancer cell lines, and gastrin receptor antagonists are able to block this phenomenon, their potency has been modest.

Methods: The effect of a new, potent and selective CCK B receptor antagonist, CI-988 on the growth of LoVo, a human colon cancer cell line both in vitro and in vivo was instigated.

Results: Basal growth of LoVo in vitro was inhibited by up to 58.93 +/- 7.30% with concentrations of CI-988 as low as 1 X 10(-11) mol/L whereas the addition of gastrin (G17) at 0.5 nmol/L had no effect. LoVo was also grown in vivo for 10 days in nude mice subsequently treated with CI-988 at 10 mg/kg per day orally for 20 days. CI-988 inhibited the growth of xenografts by 53%.

Conclusion: This was the first study in cancer with this potent gastrin receptor antagonist, CI-988. The results suggest that CI-988 may be of use in inhibiting the growth of colorectal cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Analysis of Variance
  • Animals
  • Cell Division / drug effects
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / metabolism
  • Drug Evaluation, Preclinical
  • Hormone Antagonists / pharmacology*
  • Hormone Antagonists / therapeutic use*
  • Humans
  • Indoles / pharmacology*
  • Indoles / therapeutic use*
  • Male
  • Meglumine / analogs & derivatives*
  • Meglumine / pharmacology
  • Meglumine / therapeutic use
  • Mice
  • Mice, Nude
  • Neoplasms, Experimental / drug therapy*
  • Receptors, Cholecystokinin / antagonists & inhibitors*
  • Tumor Cells, Cultured / drug effects


  • Hormone Antagonists
  • Indoles
  • Receptors, Cholecystokinin
  • PD 134308
  • Meglumine