Preclinical studies of fluvastatin

Drugs of Today

Volumn 32, Issue 1, 1996, Pages 19-38

  Corsini, Alberto ^a   Fumagalli, Remo ^a   Paoletti, Rodolfo ^a   Bernini, Franco ^b  

^a UNIVERSITY OF MILAN   (Italy)

^b UNIVERSITY OF PARMA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

FLUINDOSTATIN; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; MEVINOLIN; PRAVASTATIN; SIMVASTATIN;

ATHEROSCLEROSIS; CARCINOGENICITY; DRUG METABOLISM; DRUG SCREENING; ENZYME INHIBITION; HUMAN; HYPERCHOLESTEROLEMIA; NONHUMAN; RABBIT; REVIEW;

EID: 0029970426     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.1996.32.1.355120     Document Type: Review

References (94)

1. Neaton, J.D., Wentworth, D. for the Multiple Risk Factor Intervention Trial Research Group. Serum cholesterol, blood pressure, cigarette smoking, and death from coronary heart disease. Overall findings and differences by age for 316,099 white men. Arch Intern Med 1992,152: 56-63.
2. National Cholesterol Education Program. Second report of the Expert Panel on Detection, Evaluation; and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel II). Circulation 1994, 89: 1329-445.
3. Law, M.R., Wald, N.J., Hackshaw, A., Bailey, A. Systematic underestimation of association between serum cholesterol concentration and ischaemic heart disease in observational studies: Data from the BUPA study. Brit Med J 1994, 308: 363-6.
4. Castelli, W.P., Garrison, R.J., Wilson, P.W.F., Abbott, R.D., Kalousdian, S., Kannel, W.B. Incidence of coronary heart disease and lipoprotein cholesterol levels: The Framingham Study. JAMA 1986, 256: 2835-8.
5. Wissler, R.W. Update on the pathogenesis of atherosclerosis. Amer J Med 1991, 91(Suppl. 1B): 1B-3S-1B-9S.
6. Ross, R. The pathogenesis of atherosclerosis: A perspective for the 1990s. Nature 1993, 362: 801-9.
7. Brown, M.S., Goldstein, J.L. A receptor-mediated pathway for cholesterol homeostasis. Science 1986, 232: 34-47.
8. Relationship of atherosclerosis in young men to serum lipoprotein cholesterol concentrations and smoking. A preliminary report from the Pathobiological Determinants of Atherosclerosis in Youth (PDAY) Research Group. JAMA 1990, 264: 3018-24.
9. Brown, B.G., Zhao, X.-Q., Sacco, D.E., Albers, J.J. Lipid lowering and plaque regression. New insights into prevention of plaque disruption and clinical events in coronary disease. Circulation 1993, 87: 1781-91.
10. Watts, G.F., Lewis, B., Brunt, J.N.H. et al. Effects on coronary artery disease of lipid-lowering diet, or diet plus cholestyramine, in the St. Thomas' Atherosclerosis Regression Study (STARS). Lancet 1992, 339: 563-9.
11. Lipid Research Clinics Program. The Lipid Research Clinics Coronary Prevention Trial results. II: The relationship of reduction in incidence of coronary heart disease to cholesterol lowering. JAMA 1984, 251: 365-74.
12. Frick, M.H., Elo, O., Haapa, K. et al. Helsinki Heart Study: Primary-prevention trial with gemfibrozil in middle-aged men with dyslipoproteinemia. Safety of treatment, changes in risk factors, and incidence of coronary heart disease. New Engl J Med 1987, 317: 1237-45.
13. Manninen, V., Tenkanen, L., Koskinen, P. et al. Joint effects of serum trygliceride and LDL cholesterol concentrations on coronary heart disease risk in the Helsinki Heart Study. Circulation 1992, 85: 37-45.
14. Blankenhorn, D.H., Nessim, S.A., Johnson, R.L. Beneficial effects of combined colestipol-niacin therapy on coronary atherosclerosis and coronary venous bypass graft. JAMA 1987. 257: 3233-40.
15. Brown, G., Albers, J.J., Fisher, L.D. et al. Regression of coronary artery disease as a result of intensive lipid-lowering therapy in men with high levels of apolipoprotein B. New Engl J Med 1990, 323: 1289-98.
16. Kane, J.P., Malloy, M.J., Ports, T.A., Phillips, N.R., Diehl, J.C., Havel, R.J. Regression of coronary atherosclerosis during treatment of familial hypercholesterolemia with combined drug regimens. JAMA 1990, 264: 3007-12.
17. Blankenhorn, D.H., Azen, S.P., Kramsch, D.M. et al. Coronary angiographic changes with lovastatin therapy. The Monitored Atherosclerosis Regression Study (MARS). Ann Intern Med 1993, 119: 969-76.
18. MAAS Investigators. Effect of simvastatin on coronary atheroma: The Multicentre Anti-Atheroma Study (MAAS). Lancet 1994, 344: 633-8.
19. Scandinavian Simvastatin Survival Study Group. Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Simvastatin Survival Study (4S). Lancet 1994, 344: 1383-9.
20. Waters, D., Higginson, L., Gladstone, P. et al. Effects of monotherapy with an HMG-CoA reductase inhibitor on the progression of coronary atherosclerosis as assessed by serial quantitative arteriography. The Canadian Coronary Atherosclerosis Intervention Trial. Circulation 1994, 89: 959-68.
21. Furberg, C.D., Adams, H.P., Applegate, W.B. et al. Effect of lovastatin on early carotid atherosclerosis and cardiovascular events. Circulation 1994, 90: 1679-87.
22. Endo, A. The discovery and development of HMG-CoA reductase inhibitors. J Lipid Res 1992, 33: 1569-82.
23. Brown, M.S., Goldstein, J.L. Drugs used in the treatment of hyperlipoproteinemias. In: The Pharmacological Basis of Therapeutics. Gilman, A.G., Rall, T.W., Mies, A.L. et al. (Eds.). Pergamon Press, 1991, 874-96.
24. Illingworth, D.R. Clinical implications of new drugs for lowering plasma cholesterol concentrations. Drugs 1991, 49: 151-61.
25. Catapano, A.L. Mode of action of fibrates. Pharm Res 1992, 26: 331-40.
26. Lee, T.-J. Synthesis, SARs and therapeutic potential of HMG-CoA reductase inhibitors. Trends Pharmacol Sci 1987, 8: 442-6.
27. Illingworth, D.R., Erkelens, D.W., Keller, U., Thompson, G.R., Tikkanen, M.J. Defined daily doses in relation to hypolipidemic efficacy of lovastatin, pravastatin, and simvastatin. Lancet 1994, 343: 1554-5.
28. Blum. C.B. Comparison of properties of four inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. Amer J Cardiol 1994, 73: 30-11D.
29. Alberts, A.W., Chen, J.S., Kuron, G. et al. Mevinolin: A highly potent competitive inhibitor of HMG-CoA reductase and a cholesterol-lowering agent. Proc Natl Acad Sci USA 1980, 77: 3957-61.
30. Tsujita, Y., Kuroda, M., Shimada, Y. CS-514, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase: Tissue selective inhibition of sterol synthesis and hypolipidemic effect on various animal species. Biochim Biophys Acta 1986, 877: 50-60.
31. Stokker, G.E., Huffman, W.F., Alberts, A.W. et al. 3-Hydroxy-3-methylgluraryl-coenzyme A reductase inhibitors. 1. Structural modifications of 5-substituted 3,5-dihydroxypentanoic acids and their lactone derivatives. J Med Chem 1985, 28: 347-58.
32. Kathawala, F.G. HMG-CoA reductase inhibitors: An exciting development in the treatment of hyperlipoproteinemia. Med Res Rev 1991, 11: 121-46.
33. Davidson, M.H. Fluvastatin Long-Term Extension Trial (FLUENT): Summary of efficacy and safety. Amer J Med 1994, 96(Suppl. A): 41S-50S.
34. Levy, R.I., Troendle, A.J., Fattu, J.M. A quarter century of drug treatment of dyslipoproteinemia, with a focus on the new HMG-CoA reductase inhibitor fluvastatin. Circulation 1993, 87(Suppl. III): III45-III53.
35. Dietschy, J.M., Turley, S.D., Spady, D.K. Role of liver in the maintenance of cholesterol and low density lipoprotein homeostasis in different animal species, including humans. J Lipid Res 1993, 34: 1637-59.
36. Goldstein, J.L., Brown, M.S. Regulation of the mevalonate pathway. Nature 1990, 343: 425-30.
37. Endo, A., Kuroda, M., Tsujita, Y. ML-236A, ML-236B, and ML-236C, new inhibitors of cholesterogenesis produced by Penicillium citrinum. J Antibiot 1976, 29: 1346-8.
38. Endo, A., Kuroda, M., Tazawa, K. Competitive inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase by ML-236A and ML-236B, fungal metabolites, having hypocholesterolemic activity. FEBS Lett 1976, 72: 323-6.
39. Corsini, A., Maggi, F.M., Catapano, A.L. Pharmacology of competitive inhibitors of HMG-CoA reductase. Pharm Res 1995, 31: 9-27.
40. Albers, A.W., MacDonald, J.S., Till, A.E., Tobert, J.A. Lovastatin. Cardiovasc Drug Rev 1989, 7: 89-109.
41. Tsujita, Y., Watanabe, Y. Pravastatin sodium: A novel cholesterol-lowering agent that inhibits HMG-CoA reductase. Cardiovasc Drug Rev 1989, 7: 110-26.
42. Todd, P.A., Goa, K.L. Simvastatin. Drugs 1990, 40: 583-607.
43. Arai, M., Serizawa, N., Terahara, A. Pravastatin sodium (CS-514) a novel cholesterol-lowering agent which inhibits HMG-CoA reductase. Sankyu Kenkyusho Nempo 1988, 40: 1-38.
44. Hoffman, W.F., Alberts, A.W., Cragoe, E.J. Jr. et al. 3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 2. Structural modifications of 7-(substituted aryl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives. J Med Chem 1986, 29: 159-69.
45. Louis-Flamberg, P., Peishoff, C.E., Bryan, D.L. et al. Slow binding inhibition of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. Biochemistry 1990, 29: 4115-20.
46. Parker, R., Clark, R.W., Sit, S., Lanier, T.L., Grosso, R.A., Wright, J. Selective inhibition of cholesterol synthesis in liver versus extrahepatic tissues by HMG-CoA reductase inhibitors. J Lipid Res 1990, 31: 1271-82.
47. Alberts, A.W. HMG-CoA reductase inhibitors - The development. Atherosclerosis Rev 1988, 18: 123-31.
48. Shaw, M.K., Newton, R.S., Sliskovic, D.R., Roth, B.D., Ferguson, E., Krause, R. Hep-G2 cells and primary rat hepatocytes differ in their response to inhibitors of HMG-CoA reductase. Biochem Biophys Res Commun 1990, 170: 726-34.
49. Corsini, A., Mazzotti, M., Raiteri, M. et al. Relationship between mevalonate pathway and arterial myocyte proliferation: In vitro studies with inhibitors of HMG-CoA reductase. Atherosclerosis 1993, 101: 117-25.
50. Sandoz, data on file.
51. Hayashi, K., Kurokawa, J.-I., Nomura, S., Kuga, Y., Ohkura, Y., Kajiyama, G. Effect of fluvastatin sodium (XU62-320). a new inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, on the induction of low-density lipoprotein receptor in HepG2 cells. Biochim Biophys Acta 1993, 1167: 223-5.
52. van Vliet, A.K., van Thiel, G.C.F., Huisman, R.H., Moshage, H., Yap, S.H., Cohen, L.H. Different effects of 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors on sterol synthesis in various human cell types. Biochim Biophys Acta 1995, 1254: 105-11.
53. Komai, T., Shigehara, E., Tokui, T. et al. Carriermediated uptake of pravastatin by rat hepatocytes in primary culture. Biochem Pharmacol 1992, 43: 667-70.
54. Corsini, A., Granata, A., Fumagalli, R., Paoletti, R. Calcium antagonists and low density lipoproteins metabolism by human fibroblasts and by human hepatoma cell line Hep G2. Pharmacol Res Commun 1986, 18: 1-16.
55. Brown, M.S., Goldstein, J.L. Lowering plasma cholesterol by raising LDL receptors. New Engl J Med 1981, 305: 515-7.
56. Bernini, F., Didoni, G., Bonfadini, G., Bellosta, S., Fumagalli, R. Requirement for mevalonate in acetylated LDL induction of cholesterol esterification in macrophages. Atherosclerosis 1993, 104: 19-26.
57. Furukawa, S., Hirano, T. Rapid stimulation of apolipoprotein B secretion by oleate is not associated with cholesteryl ester biosynthesis in HepG2 cells. Biochim Biophys Acta 1993, 1170: 32-7.
58. Soma, M.R., Donetti, E., Parolini, C. et al. HMG-CoA reductase inhibitors: In vivo effects on carotid intimai thickening in normocholesterolemic rabbits. Arterioscl Thromb 1993, 13: 571-8.
59. Shiomi, M., Shiraishi, M., Yata, T., Ito, T. Effect of fluvastatin sodium on secretion of very low density lipoprotein and serum cholesterol levels. Arzneim-Forsch-Drug Res 1994, 44: 1154-6.
60. Fujioka, T., Nara, F., Tsujita, Y., Fukushige, J., Fukami, M., Kuroda, M. The mechanism of lack of hypocholesterolemic effects of pravastatin sodium, a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, in rats. Biochim Biophys Acta 1995, 1254: 7-12.
61. Endo, A., Tsujita, Y., Kuroda, M., Tanzaka, K. Effects of ML-236B on cholesterol metabolism in mice and rats: Lack of hypocholesterolemic activity in normal animals. Biochim Biophys Acta 1979, 576: 266-76.
62. Habenicht, A.J.R., Glomset, J.A., Ross, R. Relation of cholesterol and mevalonic acid to the cell cycle in smooth muscle and Swiss 3T3 cells stimulated to divide by platelet-derived growth factor. J Biol Chem 1980, 255: 5134-40.
63. Maltese, W.A. Posttranslational modification of proteins by isoprenoids in mammalian cells. FASEB J 1990, 4: 3319-28.
64. Hidaka, Y., Eda, T., Yonemoto, M., Kamei, T. Inhibition of cultured vascular smooth muscle cell migration by simvastatin (MK-733). Atherosclerosis 1992, 95: 87-94.
65. Corsini, A., Raiteri, M., Soma, M.R., Bernini, F., Fumagalli, R., Paoletti, R. Pathogenesis of atherosclerosis and the role of drug intervention: Focus on HMG-CoA reductase inhibitors. Amer J Cardiol 1995 (in press).
66. Jackson, C.L., Schwartz, S.M. Pharmacology of smooth muscle cell replication. Hypertension 1992, 20: 713-36.
67. Ip, J.H., Fuster, V., Badimon, L., Badimon, J., Taubman, M.B., Chesebro, J.H. Syndromes of accelerated atherosclerosis: Role of vascular injury and smooth muscle cell proliferation. J Amer Coll Cardiol 1990, 15: 1667-87.
68. O'Brien, E.R., Alpers, C.E., Stewart, D.K. et al. Proliferation In primary and restenotic coronary atherectomy tissue. Implications for antiproliferative therapy. Circ Res 1993, 73: 223-31.
69. Katsuda, S., Coltrera, M.D., Ross, R., Gown, A.M. Human atherosclerosis. IV. Immunocytochemical analysis of cell activation and proliferation in lesions of young adults. Amer J Pathol 1993, 142: 1787-93.
70. Pickering, J.G., Weir, L., Jekanowski, J., Kearney, M.A., Isner, J.M. Proliferative activity in peripheral and coronary atherosclerotic plaque among patients undergoing percutaneous revascularization. J Clin Invest 1993, 91: 1469-80.
71. Gordon, D., Reidy, M.A., Benditt, E.P., Schwartz, S.M. Cell proliferation in human coronary arteries. Proc Natl Acad Sci USA 1990, 87: 4600-4.
72. Steinberg, D., Parthasarathy, S., Carew, T., Khoo, J., Witztum, J. Beyond cholesterol. Modifications of low-density lipoprotein that increase its atherogenicity. New Engl J Med 1989, 320: 915-24.
73. Heinecke, J.W. Cellular mechanisms for the oxidative modification of lipoprotein implications for atherogenesis. Coronary Artery Dis 1994, 5: 205-10.
74. Witzum, J.L., Steinberg, D. Role of oxidized low-density lipoprotein in atherogenesis. J Clin Invest 1991. 88: 1785-92.
75. Brown, M.S., Goldstein, J.L. Lipoprotein metabolism in the macrophage: Implications for cholesterol deposition in atherosclerosis. Annu Rev Biochem 1983, 52: 223-61.
76. Kurihara, Y., Matsumoto, A., Itakura, H., Kodama, T. Macrophage scavenger receptors. Curr Opin Lipidol 1991, 2: 295-300.
77. Kodama, T., Reddy, P., Kishimoto, C., Krieger, M. Purification and characterization of a bovine acetyl low density lipoprotein receptor. Proc Natl Acad Sci USA 1988, 85: 9238-42.
78. Corsini, A., Raiteri, M., Soma, M.R., Fumagalli, R., Paoletti, R. Simvastatin but not pravastatin inhibits the proliferation of rat aorta myocytes. Pharm Res 1991, 23: 173-80.
79. MacDonald, J.S., Gerson, R.J., Kornburst, D.J. et al. Preclinical evaluation of lovastatin. Amer J Cardiol 1988, 62: 16J-27J.
80. Hrab, R.V., Hartman, H.A., Cox, R.H. Prevention of fluvastatin-induced toxicity, mortality and cardiac myopathy in pregnant rats by mevalonic acid supplementation. Teratology 1994, 50: 19-26.
81. Robinson, R.L., Suter, W., Cox, R.H. Carcinogenicity and mutagenicity studies with fluvastatin, a new. entirely synthetic HMG-CoA reductase inhibitor. Fundam Appl Toxicol 1994, 23: 9-20.
82. Tse, F.L.S., Smith, H.T., Ballard, F.H., Nicoletti, J. Disposition of fluvastatin, an inhibitor of HMG-CoA reductase, in mouse, rat, dog, and monkey. Biopharm Drug Disp 1990, 11: 519-31.
83. Tse, F.L.S., Labbadia, D. Absorption and disposition of fluvastatin, an inhibitor of HMG-CoA reductase, in the rabbit. Biopharm Drug Disp 1992, 13: 285-94.
84. Duggan, D.E., Vickers, S. Physiological disposition of HMG-CoA reductase inhibitors. Drug Metab Rev 1990, 22(4): 333-62.
85. Bocan, T.M.A., Ferguson, E., McNally, W. et al. Hepatic and nonhepatic sterol synthesis and tissue distribution following administration of a liver selective HMG-CoA reductase inhibitor, Cl-981: Comparison with selected HMG-CoA reductase inhibitors. Biochim Biophys Acta 1992, 1123: 133-44.
86. Koga, T., Fukuda, K., Shimada, Y., Fukami, M., Koike, H., Tsujita, Y. Tissue selectivity of pravastatin sodium, lovastatin and simvastatin. The relationship between inhibition of de novo sterol synthesis and active drug concentrations in the liver, spleen and testis in rat. Eur J Biochem 1992, 209: 315-9.
87. Sirtori, C.R. Tissue selectivity of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors. Pharmacol Ther 1993, 60: 431-59.
88. Germershausen, J.I., Hunt, V.M., Bostedor, R.G., Bailey, P.J., Karkas, J.D., Alberts, A.W. Tissue selectivity of the cholesterol-lowering agents lovastatin, simvastatin and pravastatin in rats in vivo. Biochem Biophys Res Commun 1989, 158: 667-75. [Published erratum appears in Biochem Biophys Res Commun 1991, 174(2): 1053].
89. Koga, T., Shimada, Y., Kuroda, M., Hasegawa, K., Yamazaki, M. Tissue-selective inhibition of cholesterol synthesis in vivo by pravastatin sodium, a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Biochim Biophys Acta 1990, 1045: 115-20.
90. Guillot, F., Misslin, P., Lemaire, M. Comparison of fluvastatin and lovastatin blood-brain barrier transfer using in vitro and in vivo methods. J Cardiovasc Pharmacol 1993, 21: 339-46.
91. Tse, F.L.S., Nickerson, D.F., Yardley, W.S. Binding fluvastatin to blood cells and plasma proteins. J Pharm Sci 1993, 82: 942-7.
92. Dain, J.G., Fu, E., Gorski, J., Nicoletti, J., Scallen, T.J. Biotransformation of fluvastatin sodium in humans. Drug Metab Dispos 1993, 21: 567-72.
93. Duggan, D.E., Chen, I.W., Bayne, W.F. et al. The physiological disposition of lovastatin. Drug Metab Dispos 1989, 17: 166-73.
94. Vickers, S., Duncan, C.A., Chen, I.W., Rosegay, A., Duggan, D.E. Metabolic disposition studies on simvastatin, a cholesterol-lowering prodrug. Drug Metab Dispos 1990, 18: 138-45.