Artigo Acesso aberto

Cerivastatin (BAY w 6228): A Novel HMG‐CoA Reductase Inhibitor

1998; Wiley; Volume: 16; Issue: 3 Linguagem: Inglês

10.1111/j.1527-3466.1998.tb00357.x

ISSN

1527-3466

Autores

J. Kuhlmann, Wolfgang Mück, Hilmar Bischoff, Eckhard von Keutz, Michael Llewellyn,

Tópico(s)

Microbial Metabolism and Applications

Resumo

Cardiovascular Drug ReviewsVolume 16, Issue 3 p. 236-263 Free Access Cerivastatin (BAY w 6228): A Novel HMG-CoA Reductase Inhibitor J. Kuhlmann, Corresponding Author J. Kuhlmann Bayer AG, Pharma-Research-Center, Wuppertal, GermanyAddress correspondence and reprint requests to Dr. J. Kuhlmann, Bayer AG, Pharma-Research-Center, Institute of Clinical Pharmacology, Building 429, D-42096 Wuppertal, Germany. Fax: 49-202-36-4115.Search for more papers by this authorW. Mück, W. Mück Bayer AG, Pharma-Research-Center, Wuppertal, GermanySearch for more papers by this authorH. Bischoff, H. Bischoff Bayer AG, Pharma-Research-Center, Wuppertal, GermanySearch for more papers by this authorE. von Keutz, E. von Keutz Bayer AG, Pharma-Research-Center, Wuppertal, GermanySearch for more papers by this authorM. Llewellyn, M. Llewellyn Bayer Plc, European Medical Affairs, Stoke Court, UK.Search for more papers by this author J. Kuhlmann, Corresponding Author J. Kuhlmann Bayer AG, Pharma-Research-Center, Wuppertal, GermanyAddress correspondence and reprint requests to Dr. J. Kuhlmann, Bayer AG, Pharma-Research-Center, Institute of Clinical Pharmacology, Building 429, D-42096 Wuppertal, Germany. Fax: 49-202-36-4115.Search for more papers by this authorW. Mück, W. Mück Bayer AG, Pharma-Research-Center, Wuppertal, GermanySearch for more papers by this authorH. Bischoff, H. Bischoff Bayer AG, Pharma-Research-Center, Wuppertal, GermanySearch for more papers by this authorE. von Keutz, E. von Keutz Bayer AG, Pharma-Research-Center, Wuppertal, GermanySearch for more papers by this authorM. Llewellyn, M. Llewellyn Bayer Plc, European Medical Affairs, Stoke Court, UK.Search for more papers by this author First published: 02 April 2007 https://doi.org/10.1111/j.1527-3466.1998.tb00357.xCitations: 13AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat REFERENCES 1 Alberts AW, Chen J, Kuron G, et al. Mevinolin: A highly potent competitive inhibitor of hydroxymethyl-glutaryl-coenzyme A reductase and a cholesterol-lowering agent. Proc Natl Acad Sci USA 1980: 77: 3957– 3961. 2 Anderson KM, Castelli WP, Levy D. Cholesterol and mortality: 30 years follow-up from the Framingham study. JAMA 1987; 257: 2176– 2180. 3 Angerbauer R, Bischoff H, Steinke W, Ritter W. BAY w 6228. Drugs Future 1994; 19: 537– 541. 4 Azuma J. A clinical trial of pharmacokinetics of BAY w 6228 in elderly volunteers. Jpn Pharmacol Ther 1996; 24(Suppl. 9): 55– 66. 5 Azuma J. Phase I study of an antihyperlipidaemic BAY w 6228 (cerivastatin sodium.) 1. Results of single administration studies in healthy adult male volunteers. Jpn Pharmacol Ther 1996; 24(Suppl. 9): 29– 36. 6 Azuma J. Phase I study of an antihyperlipidaemic BAY w 6228 (cerivastatin sodium.) 2. Results of multiple administration studies in healthy adult male volunteers. Jpn Pharmacol Ther 1996; 24(Suppl. 9): 37– 53. 7 Bayer AG/Corp., Data on file. 8 Bischoff H, Angerbauer R, Bender J, et al. Cerivastatin. Pharmacology of a novel synthetic and highly active HMG-CoA-reductase inhibitor. Atherosclerosis 1997: 135: 119– 130. 9 Bischoff H, Angerbauer R, Boberg M, Schmidt D. Cerivastatin: High enzyme affinity and active metabolites contribute to its high pharmacological activity. Atherosclerosis 1997; 130(suppl.): S25. 10 Blankenhorn DH, Azen SP, Kramsch DM, et al. Coronary angiographic changes with lovastatin therapy. The monitored atherosclerosis regression study (MARS). Am Coll Phys 1993: 119: 969– 976. 11 Boberg M, Angerbauer R, Kanhai W, Karl W, Kern A, Radtke M. [14C]BAY w 6228: Biotransformation in human liver microsomes in vitro. Characterization of primary metabolite pathways and of cytochrome P450 isozymes involved. Drug Metab Dispos 1997: 25: 321– 331. 12 Boberg M, Angerbauer R, Kanhai WK, et al. Biotransformation of cerivastatin in mouse, rat, and dog, in vivo. Drug Metab Dispos 1998; 26: 640– 652. 13 Brown G, Albers JJ, Fisher LD, et al. Regression of coronary artery disease as a result of intensive lipid-lowering therapy in men with high levels of apolipoprotein B. N Engl J Med 1990; 232: 1289– 1298. 14 Brown MS, Goldstein JL. A receptor-mediated pathway for cholesterol homeostasis. Science 1986; 232: 34– 47. 15 Chao Y, Chen JS, Hunt VM, et al. Lowering of plasma cholesterol levels in animals by lovastatin and simvastatin. Eur J Clin Pharmacol 1991; 40: S11– 14. 16 Corsini A, Arnalboldi L, Raiteri M, et al. Effect of the new HMG-CoA-reductase inhibitor cerivastatin (BAY w 6228) on migration, proliferation, and cholesterol synthesis in arterial myocytes. Pharmacol Res 1996; 33: 55– 61. 17 Desager JP, Horsmans. Clinical pharmacokinetics of 3-hydroxy-3-methylglutaryl-coenzyme A-reductase inhibitors. Clin Pharmacokin 1996; 31: 348– 371. 18 Dobs AS, Sarma PS, Schteingart D. Long-term endocrine function in hypercholesterolemic patients treated with pravastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A-reductase inhibitor. Metabolism 1993; 42: 1146– 1152. 19 Eisenberg D. The importance of lowering cholesterol in patients with coronary heart disease. Clin Cardiol 1998; 21: 81– 84. 20 Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults. Summary of the second report of the National Cholesterol Education Program (NCEP) expert panel on detection, evaluation, and treatment of high blood cholesterol in adults (Adult Treatment Panel II). JAMA 1993; 269: 3015– 3023. 21 Food and Drug Administration. Summary basis for approval of NDA 20–261 (fluvastatin). Pharmacol Rev 1993. 22 Frey R, Mazzu A, Ritter W, Heller AH, Kuhlmann J. Safety and tolerability of rivastatin, a novel HMG-CoA reductase inhibitor, in phase-I single dose studies. Naunyn Schmiedeberg's Arch Pharmacol 1993; 347(suppl.): R30. 23 Garnett WR. Interactions with hydroxymethylglutaryl-coenzyme A-reductase inhibitors. Am J Health Syst Pharm 1995; 52: 1639– 1645. 24 Gerson RJ, MacDonald JS, Alberts AW, et al. Animal safety and toxicology of simvastatin and related hydroxy-methylglutaryl-coenzyme A–reductase inhibitors. Am J Med 1989; 87(Suppl. 4A): 28S– 38S. 25 Holme I. An analysis of randomized trials evaluating the effect of cholesterol reduction on total mortality and coronary heart disease incidence. Circulation 1990; 82: 1916– 1924. 26 Igarashi M, Takeda Y, Mori S, et al. Suppression of neointimal thickening by a newly developed HMG-CoA-reductase inhibitor, BAY w 6228, and its inhibitory effect on vascular smooth muscle cell growth. Br J Pharmacol 1997; 120: 1172– 1178. 27 Igarashi M, Takeda Y, Mori S, et al. BAY w 6228 suppresses accumulation of macrophages in balloon-induced intimai thickening of rabbit carotid artery. Atherosclerosis 1997; 128: 251– 4. 28 Ikeda T, Ishigami M, Yamazoe Y. Inhibition of hepatic cytochrome P450 isoform, CYP3A, by 3-hydroxy-3-methylglutaryl-CoA-reductase inhibitors. Atherosclerosis 1997; 134: 135. 29 Kane JP, Malloy MJ, Ports TA, Phillips NR, Diehl JC, Havel RJ. Regression of coronary atherosclerosis during treatment of familial hypercholesterolemia with combined drug regimens. JAMA 1990; 264: 3007– 3012. 30 Kannel WB. Range of serum cholesterol values in the population developing coronary artery disease. Am J Cardiol 1995; 76: 69c– 77c. 31 Katsuda S, Boyd HC, Fligner C, Ross R, Gown AM. Human Atherosclerosis. III. Immunocytochemical analysis of the cell composition of lesions of young adults. Am J Pathol 1992; 140: 907– 914. 32 Kovanen PT, Bilheimer DW, Goldstein JL, Jaramillo JJ, Brown MS. Regulatory role of hepatic low-density lipoprotein receptors in vivo in the dog. Proc Natl Acad Sci USA 1981; 78: 1194– 1198. 33 Krol GJ, Beck GW, Ritter W, Lettieri JT. LC separation and induced fluorometric detection of rivastatin in blood plasma. J Pharm Biomed Anal 1993; 11: 1269– 1275. 34 Lettieri J, Krol G, Mazzu A, Shah A, Falk R, Beck C. Effect of age and gender on steady-state pharmacokinetics of rivastatin. Pharm Res 1993; 10(suppl.): S338. 35 Lettieri J, Krol G, Mazzu A, Fiebach MZ, Heller AH. Lack of pharmacokinetic interaction between cerivastatin, a new HMG-CoA reductase inhibitor, and digoxin. Atherosclerosis 1997; 130(suppl.): S29. 36 Levy RI. Cholesterol and cardiovascular disease: No longer whether, but rather when, in whom, and how Circulation 1985; 72: 686– 691. 37 Levy RI, Troendle AJ, Fattu JM. 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. 38 MacDonald JS, Gerson RJ, Kornbrust DJ, et al. Preclinical evaluation of lovastatin. Am J Cardiol 1998; 62: 16J– 27J. 39 Mai I, Bauer S, Fritsche J, et al. Clinical pharmacokinetics of a new HMG-CoA reductase inhibitor in renal transplant patients treated with cyclosporine A (CSA). Eur J Clin Pharmacol 1997; 52(suppl.): A137. 40 Mazzu A, Lettieri J, Kaiser L, Frey R, Heller AH. Ascending multiple dose safety, tolerability, and pharmacokinetics of rivastatin in humans. Clin Pharmacol Ther 1993; 53: 230. 41 Mazzu A, Lettieri J, Heller AH. Pharmacokinetics of cerivastatin administration with and without food in the morning and evening. Atherosclerosis 1997; 130(suppl.): S29. 42 Mazzu A, Lettieri J, Kaiser L, Heller AH. A multiple-dose study on the safety and pharmacokinetics of cerivastatin in young and elderly male volunters. Atherosclerosis 1997; 130(suppl.): S29. 43 Minsker DH, MacDonald JS, Robertson RT, Bokelman DL. Mevalonate supplementation in pregnant rats suppresses the teratogenicity of mevinolinic acid, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Teratology 1983, 28: 449– 456. 44 Mück W, Ritter W, Frey R, Wetzelsberger N, Lücker PW, Kuhlmann J. Influence of cholestyramine on the pharmacokinetics of cerivastatin. Int J Clin Pharmacol Ther 1997; 35: 250– 254. 45 Mück W, Ritter W, Ochmann K, Kuhlmann J. Absolute and relative bioavailability of the HMG-CoA reductase inhibitor cerivastatin. Int J Clin Pharmacol Ther 1997; 35: 255– 260. 46 Mück W, Ritter W, Dietrich H, Frey R, Kuhlmann J. Influence of the antacid Maalox and the H2 antagonist cimetidine on the pharmacokinetics of cerivastatin. Int J Clin Pharmacol Ther 1997; 35: 261– 264. 47 Mück W, Ochmann K, Kuhlmann J. Rationale for pharmacokinetic drug-drug interaction programme within clinical development—Case history cerivastatin, a new HMG-CoA reductase inhibitor. Eur J Clin Pharmacol 1997; 52(suppl.): A138. 48 Mück W, Ochmann K, Mazzu A, Lettieri J. Biopharmaceutical profile of cerivastatin, a novel HMG-CoA reductase inhibitor. Atherosclerosis 1997: 134: 130. 49 Mück W, Ochmann K, Rohde G, Unger S, Kuhlmann J. Influence of erythromycin pre-and co-treatment on single-dose pharmacokinetics of the HMG-CoA-reductase inhibitor cerivastatin. Eur J Clin Pharmacol 1998: 53: 469– 473. 50 Mück W, Ochmann K, Rohde G, Unger S, Kuhlmann J. No drug-drug interaction between cerivastatin and omeprazole. Naunyn-Schmiedeberg's Arch Pharmacol 1998; 357(suppl.): R175. 51 Mück W, Kawano K, Unger S, Ahr G. Interethnic comparisons of the pharmacokinetics of the HMG-CoA reductase inhibitor cerivastatin. Br J Clin Pharmacol 1998: 45: 583– 590. 52 Nègre-Aminou P, van Vliet AK, van Erck M, van Thiel GCF, van Leeuwen REW, Cohen LH. Inhibition of proliferation of human smooth muscle cells by various HMG-CoA-reductase inhibitors; comparison with other human cell types. Biochim Biophys Acta 1997: 1345: 259– 268. 53 Newman TB, Hulley SB. Carcinogenicity of lipid-lowering drugs. JAMA 1996: 275: 55– 60. 54 Radtke M, Boberg M, Kanhai W, Kern A, Leega A, Nowak K. Cerivastatin: Identification of human cytochrome P-450 isozymes involved in the biotransformation of the drug and two active metabolites. Proceedings of the 8th North American ISSX Meeting, Hilton Head, SC/USA, October 2630, 1997: 109. 55 Radtke M, Kanhai W. Characterization of the cytochrome P450 isozymes involved in the metabolism of cerivastatin in humans. Drug Metab Dispos 1998; (in press). 56 Raines EW, Ross R. Smooth muscle cells and the pathogenesis of atherosclerosis. Br Heart J 1993; 69: S30– 37. 57 Ritter W, Frey R, Krol G, Kuhlmann J. Rivastatin single dose pharmacokinetics. Clin Pharmacol Ther 1993: 53: 210. 58 Ritter W, Frey R, Krol G, Kuhlmann J. Single-dose pharmacokinetics of rivastatin, a novel HMG-CoA reductase inhibitor. Naunyn Schmiedeberg's Arch Pharmacol 1993; 347(suppl.): R39. 59 Ross R. The pathogenesis of atherosclerosis: A perspective for the 1990s. Nature 1993; 362: 801– 809. 60 Sachse R, Brendel E, Mück W, et al. Lack of drug-drug interactions between cerivastatin and nifedipine. Int J Clin Pharmacol Ther 1998: 36: 409– 413. 61 Sacks FM. The effect of pravastatin on coronary events after myocardial infarction in patients with average cholesterol levels. N Engl J Med 1996: 335: 1001– 1009. 62 Scandinavian simvastatin survival study group. Randomised trial of cholesterol lowering in 4,444 patients with coronary heart disease: The Scandivavian Simvastatin Survival Study (4S). Lancet 1994; 344: 1383– 1389. 63 Schall R, Mueller FO, Hundt HK, et al. No pharmacokinetic or pharmacodynamic interaction between rivastatin and warfarin. J Clin Pharmacol 1995; 35: 306– 313. 64 Shepherd J, Cobbe SM, Ford I, et al. Prevention of coronary heart disease with pravastatin in men with hypercholesterolemia. N Engl J Med 1995; 333: 1301– 1307. 65 Stary HC, Chandler AB, Glagov S, et al. A definition of initial, fatty streak, and intermediate lesions of atherosclerosis. Artehoscl Thromb 1994; 14: 840– 856. 66 Stein E, Sprecher D, Allenby KS, Tosiello RL, Whalen E, Ripa SR. Cerivastatin, a new potent synthetic HMG-CoA-reductase inhibitor; effect of 0.2 mg daily in subjects with primary hypercholesterolemia. J Curdiovasc Pharmacol Ther 1997; 2: 7– 16. 67 Stein EA. Extending therapy options in treating lipid disorders. A clinical review of cerivastatin, a novel HMG-CoA-reductase inhibitor. Drugs 1998; 56(Suppl. 1): 25– 31. 68 Stein EA, Isaacsohn J, Zinny M, Mazzu A, Lettieri J, Heller AH. Pharmacokinetics, safety and tolerability of multiple-dose cerivastatin in males and females: A double-blind study. Atherosclerosis 1997; 130(suppl.): S33. 69 Stein E, Isaacsohn J, Stoltz R, et al. Efficacy and Safety of 0.8-mg dosage of cerivastatin, a novel HMG-CoA-reductase inhibitor. J Am Coll Cardiol 1998; 31;2(Suppl. A):abstract 1116-5. 70 Steinke W, Yamashita S, Tabei M, et al. Cerivastatin, a new inhibitor of HMG-CoA reductase. Pharmacokinetics in rats and dogs. Jpn Pharmacol Ther 1996; 24(Suppl. 9): 1217– 1223. 71 The Expert Panel: Report of the National Cholesterol Education Program expert panel on detection, evaluation, and treatment of high blood cholesterol in adults. Arch Intern Med 1988; 148: 36– 692. 72 Thyberg J, Hedin U, Sjolund M, Palmberg L, Bottger BA. Regulation of differentiated properties and proliferation of arterial smooth muscle cells. Arteriosclerosis 1990; 10: 966– 990. 73 von Keutz E, Schlüter G. Preclinical safety evaluation of cerivastatin, a novel HMG-CoA-reductase inhibitor. Am J Cardiol 1998; 82(in press). 74 Vormfelde SV, Freudenthaler S, Mück W, et al. Cerivastatin, an inhibitor of the HMG-CoA reductase, has no need for dose adjustment in renal dysfunction. Eur J Clin Pharmacol 1997; 52(suppl.): A163. 75 Vormfelde SV, Gleiter CH, Freudenthaler S, Mück W, Schmage N, Kuhlmann J. Pharmacokinetics of single dose cerivastatin in subjects with normal and impaired renal function. Atherosclerosis 1997; 130(suppl.): S33. 76 Yasunobu Y, Hayahsi K, Shingu T, et al. Reduction of plasma cholesterol levels and induction of hepatic LDL receptor by cerivastatin sodium (CAS 143201-11-0, BAY w 6228), a new inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, in dogs. Cardiovasc Drugs Ther 1997; 11: 567– 574. Citing Literature Volume16, Issue3September 1998Pages 236-263 ReferencesRelatedInformation

Referência(s)
Altmetric
PlumX