Inhibiting cholesterol absorption with CP-88,818 (β-tigogenin cellobioside; tiqueside): Studies in normal and hyperlipidemic subjects

Journal of Cardiovascular Pharmacology

Volumn 30, Issue 1, 1997, Pages 55-60

  Harris, William S ^a,c   Dujovne, Carlos A ^a   Windsor, Sheryl L ^a   Colle Gerrond, Linda L ^a   Newton, Fran A ^b   Gelfand, Robert A ^b  

^a UNIVERSITY OF KANSAS MEDICAL CENTER   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

^c ST LUKE S HOSPITAL   (United States)

Author keywords

Cholesterol absorption; Fecal sterols; Hypercholesterolemia; Hypolipidemic drugs; Saponins

Indexed keywords

BETA TIGOGENIN CELLOBIOSIDE; CHOLESTEROL; LOW DENSITY LIPOPROTEIN CHOLESTEROL; SAPONIN; TIQUESIDE; UNCLASSIFIED DRUG;

ADULT; ARTICLE; BILIARY EXCRETION; CHOLESTEROL BLOOD LEVEL; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG EFFICACY; DRUG MECHANISM; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; HYPERCHOLESTEROLEMIA; HYPERLIPIDEMIA; LIPID ABSORPTION; LIPID BLOOD LEVEL; LIPOPROTEIN BLOOD LEVEL; MALE; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; STEROL EXCRETION; VITAMIN INTAKE;

ADOLESCENT; ADULT; ANTICHOLESTEREMIC AGENTS; APOLIPOPROTEINS; CHOLESTEROL, DIETARY; CHOLESTEROL, LDL; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; FECES; HUMANS; HYPERCHOLESTEROLEMIA; INTESTINAL ABSORPTION; LIPIDS; LIPOPROTEINS; MALE; MIDDLE AGED; POSTPRANDIAL PERIOD; SAPONINS; VITAMINS;

EID: 0030657967     PISSN: 01602446     EISSN: None     Source Type: Journal    
DOI: 10.1097/00005344-199707000-00008     Document Type: Article

References (25)

1. Dujovne CA, Harris WS. The pharmacological treatment of dyslipidemia. Annu Rev Pharmacol Toxicol 1989;29:265-88.
2. Parthasarathy S, Young SG, Witztum JL. Probucol inhibits oxidative modification of low density lipoproteins. J Clin Invest 1986; 77: 641-4.
3. Wilson MD, Rudel LL. Review of cholesterol absorption with emphasis on dietary and biliary cholesterol. J Lipid Res 1994;35:943-55.
4. Connor WE, Stone DB, Hodges RE. The interrelated effects of dietary cholesterol and fat upon human serum lipid levels. J Clin Invest 1964;43:1691-6.
5. Mattson FH, Grundy SM, Crouse JR. Optimizing the effect of plant sterols on cholesterol absorption in man. Am J Clin Nutr 1982;35:697-700.
6. Heinemann T, Kullak-Ublick GA, Pietruck B, von Bergmann K. Mechanisms of action of plant sterols on inhibition of cholesterol absorption: comparison of sitosterol and sitostanol. Eur J Clin Pharmacol 1991;40:859-63.
7. Kesaniemi YA, Grundy SM. Turnover of low density lipoproteins during inhibition of cholesterol absorption by neomycin. Arteriosclerosis 1984;4:41-8.
8. Harwood HJ Jr, Chandler CE, Pellarin LD, et al. Pharmacologic consequences of cholesterol absorption inhibition: alteration in cholesterol metabolism and reduction in plasma cholesterol concentration induced by the synthetic saponin β-tigogenin cellobioside (CP-88818; tiqueside). J Lipid Res 1993;34:377-95.
9. Crouse JR, Grundy SM. Evaluation of a continuous isotope feeding method for measurement of cholesterol absorption in man. J Lipid Res 1978;19:967-71.
10. Jandacek RJ, Ramirez MM, Crouse JRI. Effects of partial replacement of dietary fat by olestra on dietary cholesterol absorption in man. Metabolism 1990;39:848-52.
11. Grundy SM, Ahrens EH Jr, Salen G. Dietary beta-sitosterol as an internal standard to correct for cholesterol losses in sterol balance studies. J Lipid Res 1968;9:374-87.
12. Warnick GR, Albers JJ. A comprehensive evaluation of the heparin manganese precipitation procedure for estimating high density lipoprotein cholesterol. J Lipid Res 1978;19:65-76.
13. Friedewald WT, Levy RI, Fredrickson DS. Estimation of the concentration of low-density lipoprotein cholesterol in plasma, without use of the preparative ultracentrifuge. Clin Chem 1972;19: 499-502.
14. Czubayko F, Beumers B, Lammsfuss S, Lutjohann D, von Bergmann K. A simplified micro-method for quantification of fecal excretion of neutral and acidic sterols for outpatient studies in humans. J Lipid Res 1991;32:1861-70.
15. Catignani GL, Bieri JG. Simultaneous determination of retinol and α-tocopherol in serum or plasma by liquid chromatography. Clin Chem 1983;29:708-12.
16. Lo CW, Paris PW, Clemens TL, Nolan J, Holick MF. Vitamin D absorption in healthy subjects and in patients with intestinal malabsorption syndromes. Am J Clin Nutr 1985;42:644-9.
17. Lutjohann D, Meese CO, Crouse JR, von Bergmann K. Evaluation of deuterated cholesterol and deuterated sitostanol for measurement of cholesterol absorption in humans. J Lipid Res 1993;34: 1039-46.
18. Miettinen TA. Inhibition of cholesterol absorption by HMG CoA reductase inhibitor. Eur J Clin Pharmacol 1991;40:S19-21.
19. McNamara DJ, Davidson NO, Samuel P, Ahrens EH. Cholesterol absorption in man: effect of administration of clofibrate and/or cholestyramine. J Lipid Res 1980;21:1058-64.
20. Gylling H, Vanhanen H, Miettinen TA. Hypolipidemic effect and mechanism of ketoconazole without or with cholestyramine in familial hypercholesterolemia. Metabolism 1991;40:35-41.
21. Harris WS, Dujovne CA, von Bergmann K, et al. Effects of the ACAT inhibitor CL 277,082 on cholesterol metabolism in humans. Clin Pharmacol Ther 1990;48:189-94.
22. Hainer JW, Terry JG, Connell JM, et al. Effect of the acyl-CoA:cholesterol acyltransferase inhibitor DuP 128 on cholesterol absorption and serum cholesterol in humans. Clin Pharmacol Ther 1994;56:65-74.
23. Jones PJH, Pappu A, Hatcher L, Li Z, Illingworth DR, Connor WE. Dietary cholesterol feeding suppresses human cholesterol synthesis measured by deuterium incorporation and urinary mevalonic acid levels. Arterioscler Thromb Vasc Biol 1996;16:1222-8.
24. Brown MS, Goldstein J. How LDL receptors influence cholesterol and atherosclerosis. Sci Am 1984;251:58-66.
25. McCarthy PA, DeNinno MP, Morehouse LA, et al. 11-Ketotigogenin cellobioside (pamaqueside): a potent cholesterol absorption inhibitor in the hamster. J Med Chem 1996;39:100-2.