메뉴 건너뛰기




Volumn 43, Issue 11, 2003, Pages 1244-1256

Ragaglitazar: The Pharmacokinetics, Pharmacodynamics, and Tolerability of a Novel Dual PPARα and γ Agonist in Healthy Subjects and Patients with Type 2 Diabetes

Author keywords

Diabetic dyslipidemia; Pharmacodynamics; Pharmacokinetics; Ragaglitazar; Tolerability; Type 2 diabetes

Indexed keywords

C PEPTIDE; CELL RECEPTOR; FATTY ACID; FRUCTOSAMINE; GLUCOSE; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; LOW DENSITY LIPOPROTEIN CHOLESTEROL; OXAZINE DERIVATIVE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR; PHENYLPROPIONIC ACID DERIVATIVE; PLACEBO; RAGAGLITAZAR; TRANSCRIPTION FACTOR; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

EID: 0142135388     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/0091270003257230     Document Type: Article
Times cited : (52)

References (34)
  • 3
    • 0034859567 scopus 로고    scopus 로고
    • Dyslipidaemia and diabetes
    • Betteridge DJ: Dyslipidaemia and diabetes. Pract Diabetes Int 2001;18(6):201-207.
    • (2001) Pract Diabetes Int , vol.18 , Issue.6 , pp. 201-207
    • Betteridge, D.J.1
  • 4
    • 0034978521 scopus 로고    scopus 로고
    • Pathogenesis of dyslipidemia in type 2 diabetes
    • Taskinen M: Pathogenesis of dyslipidemia in type 2 diabetes. Exp Clin Endocrinol Diabetes 2001;109(Suppl. 2):S180-S188.
    • (2001) Exp Clin Endocrinol Diabetes , vol.109 , Issue.SUPPL. 2
    • Taskinen, M.1
  • 5
    • 0035056155 scopus 로고    scopus 로고
    • Peroxisome proliferator-activated receptor (PPAR) gamma agonists for diabetes
    • Moller DE, Greene DA: Peroxisome proliferator-activated receptor (PPAR) gamma agonists for diabetes. Adv Protein Chem 2001;56:181-212.
    • (2001) Adv Protein Chem , vol.56 , pp. 181-212
    • Moller, D.E.1    Greene, D.A.2
  • 6
    • 0032511583 scopus 로고    scopus 로고
    • Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33)
    • UK-Prospective DSG: Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet 1998;352(9131):837-853.
    • (1998) Lancet , vol.352 , Issue.9131 , pp. 837-853
  • 7
    • 1842326783 scopus 로고    scopus 로고
    • Cholesterol-lowering with simvastatin improves prognosis of diabetic-patients with coronary heart-disease: A sub-group analysis of the Scandinavian Simvastatin Survival Study
    • Pyorala K, Pedersen TR, Kjekshus J, Faergeman O, Olsson AG, Thorgeirsson G: Cholesterol-lowering with simvastatin improves prognosis of diabetic-patients with coronary heart-disease: a sub-group analysis of the Scandinavian Simvastatin Survival Study. Diabetes Care 1997;20:1048-1048.
    • (1997) Diabetes Care , vol.20 , pp. 1048-1048
    • Pyorala, K.1    Pedersen, T.R.2    Kjekshus, J.3    Faergeman, O.4    Olsson, A.G.5    Thorgeirsson, G.6
  • 8
    • 0035941990 scopus 로고    scopus 로고
    • Effect of fenofibrate on progression of coronary-artery disease in type 2 diabetes: The Diabetes Atherosclerosis Intervention Study, a randomised study
    • Steiner G, Hamsten A, Hosking J, Stewart D, McLaughlin P, Gladstone P, et al: Effect of fenofibrate on progression of coronary-artery disease in type 2 diabetes: the Diabetes Atherosclerosis Intervention Study, a randomised study. Lancet 2001;357(9260):905-910.
    • (2001) Lancet , vol.357 , Issue.9260 , pp. 905-910
    • Steiner, G.1    Hamsten, A.2    Hosking, J.3    Stewart, D.4    McLaughlin, P.5    Gladstone, P.6
  • 9
    • 0032497945 scopus 로고    scopus 로고
    • Cardiovascular events and their reduction with pravastatin in diabetic and glucose-intolerant myocardial infarction survivors with average cholesterol levels: Subgroup analyses in the Cholesterol and Recurrent Events (CARE) trial
    • Goldberg RB, Mellies MJ, Sacks FM, Moye LA, Howard BV, Howard WJ, et al: Cardiovascular events and their reduction with pravastatin in diabetic and glucose-intolerant myocardial infarction survivors with average cholesterol levels: subgroup analyses in the Cholesterol and Recurrent Events (CARE) trial. Circulation 1998;98(23):2513-2519.
    • (1998) Circulation , vol.98 , Issue.23 , pp. 2513-2519
    • Goldberg, R.B.1    Mellies, M.J.2    Sacks, F.M.3    Moye, L.A.4    Howard, B.V.5    Howard, W.J.6
  • 10
    • 10544229794 scopus 로고    scopus 로고
    • Effect of diuretic-based antihypertensive treatment on cardiovascular disease risk in older diabetic patients with isolated systolic hypertension
    • Curb JD, Pressel SL, Cutler JA, Savage PJ, Applegate WB, Black H, et al: Effect of diuretic-based antihypertensive treatment on cardiovascular disease risk in older diabetic patients with isolated systolic hypertension. JAMA 1996;276(23):1886-1892.
    • (1996) JAMA , vol.276 , Issue.23 , pp. 1886-1892
    • Curb, J.D.1    Pressel, S.L.2    Cutler, J.A.3    Savage, P.J.4    Applegate, W.B.5    Black, H.6
  • 11
    • 0035797363 scopus 로고    scopus 로고
    • (-)3-[4-[2-(Phenoxazin-10-yl)ethoxylphenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: A dual PPAR agonist with potent antihyperglycemic and lipid modulating activity
    • Lohray BB, Lohray VB, Bajji AC, Kalchar S, Poondra RR, Padakanti S, et al: (-)3-[4-[2-(Phenoxazin-10-yl)ethoxylphenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity. J Med Chem 2001;44(16):2675-2678.
    • (2001) J Med Chem , vol.44 , Issue.16 , pp. 2675-2678
    • Lohray, B.B.1    Lohray, V.B.2    Bajji, A.C.3    Kalchar, S.4    Poondra, R.R.5    Padakanti, S.6
  • 12
    • 0037075146 scopus 로고    scopus 로고
    • Novel tricyclic-alpha-alkyloxyphenylpropionic acids: Dual PPARα/γ agonists with hypolipidemic and antidiabetic activity
    • Sauerberg P, Pettersson I, Jeppesen L, Bury PS, Mogensen JP, Wassermann K, et al: Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARα/γ agonists with hypolipidemic and antidiabetic activity. J Med Chem 2002;45:789-804.
    • (2002) J Med Chem , vol.45 , pp. 789-804
    • Sauerberg, P.1    Pettersson, I.2    Jeppesen, L.3    Bury, P.S.4    Mogensen, J.P.5    Wassermann, K.6
  • 13
    • 0033542873 scopus 로고    scopus 로고
    • Medical significance of peroxisome proliferator-activated receptors
    • Vamecq J, Latruffe N: Medical significance of peroxisome proliferator-activated receptors. Lancet 1999;354(9173):141-148.
    • (1999) Lancet , vol.354 , Issue.9173 , pp. 141-148
    • Vamecq, J.1    Latruffe, N.2
  • 14
    • 0034235964 scopus 로고    scopus 로고
    • Potential new treatments for type 2 diabetes
    • Bailey CJ: Potential new treatments for type 2 diabetes. Trends Pharmacol Sci 2000;21(7):259-265.
    • (2000) Trends Pharmacol Sci , vol.21 , Issue.7 , pp. 259-265
    • Bailey, C.J.1
  • 15
    • 0034713444 scopus 로고    scopus 로고
    • Roles of PPARs in health and disease
    • Kersten S, Desvergne B, Wahli W: Roles of PPARs in health and disease. Nature 2000;405(6785):421-424.
    • (2000) Nature , vol.405 , Issue.6785 , pp. 421-424
    • Kersten, S.1    Desvergne, B.2    Wahli, W.3
  • 16
    • 0034735992 scopus 로고    scopus 로고
    • Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone
    • Sakamoto J, Kimura H, Moriyama S, Odaka H, Momose Y, Sugiyama Y, et al: Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochem Biophys Res Commun 2000;278(3):704-711.
    • (2000) Biochem Biophys Res Commun , vol.278 , Issue.3 , pp. 704-711
    • Sakamoto, J.1    Kimura, H.2    Moriyama, S.3    Odaka, H.4    Momose, Y.5    Sugiyama, Y.6
  • 17
    • 0031578033 scopus 로고    scopus 로고
    • Declaration of Helsinki: Recommendations guiding physicians in biomedical research involving human subjects
    • World Medical Association: Declaration of Helsinki: recommendations guiding physicians in biomedical research involving human subjects. JAMA 1997;277(11):925-926.
    • (1997) JAMA , vol.277 , Issue.11 , pp. 925-926
  • 18
    • 0037420702 scopus 로고    scopus 로고
    • Determination of ragaglitazar, a novel dual acting peroxisome proliferator-activated receptor (PPAR) α and γ agonist, in human plasma by high-performance liquid chromatography coupled with tandem mass spectrometry
    • Andersen MP, Nielsen KK: Determination of ragaglitazar, a novel dual acting peroxisome proliferator-activated receptor (PPAR) α and γ agonist, in human plasma by high-performance liquid chromatography coupled with tandem mass spectrometry. J Chromatogr B 2003;788(1):45-55.
    • (2003) J Chromatogr B , vol.788 , Issue.1 , pp. 45-55
    • Andersen, M.P.1    Nielsen, K.K.2
  • 21
    • 0037362638 scopus 로고    scopus 로고
    • PPARα/γ ragaglitazar eliminates fatty liver and enhances insulin action in fat-fed rats in the absence of hepatomegaly
    • Ye J, Iglesias MA, Watson DG, Ellis B, Wood L, Jensen PB, et al: PPARα/γ ragaglitazar eliminates fatty liver and enhances insulin action in fat-fed rats in the absence of hepatomegaly. Am J Physiol Endocrinol Metab 2003;284:E531-E540.
    • (2003) Am J Physiol Endocrinol Metab , vol.284
    • Ye, J.1    Iglesias, M.A.2    Watson, D.G.3    Ellis, B.4    Wood, L.5    Jensen, P.B.6
  • 22
    • 24444432518 scopus 로고    scopus 로고
    • Ragaglitazar: No pharmacokinetic differences between young and elderly, male and female subjects, fasted and non-fasted state including impact of hepatic recycling on the plasma elimination half-life
    • Skrumsager BK, Pedersen PC, Nielsen KK, Mueller M: Ragaglitazar: no pharmacokinetic differences between young and elderly, male and female subjects, fasted and non-fasted state including impact of hepatic recycling on the plasma elimination half-life. Diabetologia 2002;45(Suppl. 2):A232.
    • (2002) Diabetologia , vol.45 , Issue.SUPPL. 2
    • Skrumsager, B.K.1    Pedersen, P.C.2    Nielsen, K.K.3    Mueller, M.4
  • 23
    • 4243687462 scopus 로고    scopus 로고
    • NNC 61-0029 ((-)DRF2725): The single dose pharmacokinetics of a novel dual acting PPARα and PPARγ agonist in Caucasian and Japanese healthy subjects
    • Skrumsager BK, Nielsen KK, Reinhardt R, Pedersen PC: NNC 61-0029 ((-)DRF2725): the single dose pharmacokinetics of a novel dual acting PPARα and PPARγ agonist in Caucasian and Japanese healthy subjects. Diabetes 2001;50(Suppl. 2):A445.
    • (2001) Diabetes , vol.50 , Issue.SUPPL. 2
    • Skrumsager, B.K.1    Nielsen, K.K.2    Reinhardt, R.3    Pedersen, P.C.4
  • 24
    • 0028173754 scopus 로고
    • Comparison of tests for glycated haemoglobin and fasting and two hour plasma glucose concentrations as diagnostic methods for diabetes
    • McCance DR, Hanson RL, Charles MA, Jacobsson LT, Pettitt DJ, Bennett PH, et al: Comparison of tests for glycated haemoglobin and fasting and two hour plasma glucose concentrations as diagnostic methods for diabetes. Br Med J 1994;308(6940):1323-1328.
    • (1994) Br Med J , vol.308 , Issue.6940 , pp. 1323-1328
    • McCance, D.R.1    Hanson, R.L.2    Charles, M.A.3    Jacobsson, L.T.4    Pettitt, D.J.5    Bennett, P.H.6
  • 25
    • 0033754530 scopus 로고    scopus 로고
    • Pioglitazone hydrochloride monotherapy improves glycemic control in the treatment of patients with type 2 diabetes: A 6-month randomized placebo-controlled dose-response study
    • The Pioglitazone 001 Study Group
    • Aronoff S, Rosenblatt S, Braithwaite S, Egan JW, Mathisen AL, Schneider RL: Pioglitazone hydrochloride monotherapy improves glycemic control in the treatment of patients with type 2 diabetes: a 6-month randomized placebo-controlled dose-response study. The Pioglitazone 001 Study Group. Diabetes Care 2000;23(11):1605-1611.
    • (2000) Diabetes Care , vol.23 , Issue.11 , pp. 1605-1611
    • Aronoff, S.1    Rosenblatt, S.2    Braithwaite, S.3    Egan, J.W.4    Mathisen, A.L.5    Schneider, R.L.6
  • 27
    • 0035941990 scopus 로고    scopus 로고
    • Effect of fenofibrate on progression of coronary-artery disease in type 2 diabetes: The Diabetes Atherosclerosis Intervention Study, a randomised study
    • Steiner G, Hamsten A, Hosking J, Steward D, McLaughlin P, Gladstone P, et al: Effect of fenofibrate on progression of coronary-artery disease in type 2 diabetes: the Diabetes Atherosclerosis Intervention Study, a randomised study. Lancet 2001;357(9260):905-910.
    • (2001) Lancet , vol.357 , Issue.9260 , pp. 905-910
    • Steiner, G.1    Hamsten, A.2    Hosking, J.3    Steward, D.4    McLaughlin, P.5    Gladstone, P.6
  • 28
    • 0035962077 scopus 로고    scopus 로고
    • Relation of gemfibrozil treatment and lipid levels with major coronary events: VA-HIT: A randomized controlled trial
    • Robins SJ, Collins D, Wittes JT, Papademetriou V, Deedwania PC, Schaefer EJ, et al: Relation of gemfibrozil treatment and lipid levels with major coronary events: VA-HIT: a randomized controlled trial. JAMA 2001;285(12):1585-1591.
    • (2001) JAMA , vol.285 , Issue.12 , pp. 1585-1591
    • Robins, S.J.1    Collins, D.2    Wittes, J.T.3    Papademetriou, V.4    Deedwania, P.C.5    Schaefer, E.J.6
  • 29
    • 0000771591 scopus 로고    scopus 로고
    • Pioglitazone in the treatment of type 2 diabetes mellitus: U.S. clinical experience
    • Buse JB: Pioglitazone in the treatment of type 2 diabetes mellitus: U.S. clinical experience. Exp Clin Endocrinol Diabetes 2000;108(Suppl. 2):S250-S255.
    • (2000) Exp Clin Endocrinol Diabetes , vol.108 , Issue.SUPPL. 2
    • Buse, J.B.1
  • 30
    • 0034816025 scopus 로고    scopus 로고
    • Safety profile of pioglitazone
    • Hanefeld M, Belcher G: Safety profile of pioglitazone. Int J Clin Pract 2001;55(Suppl. 121):27-31.
    • (2001) Int J Clin Pract , vol.55 , Issue.SUPPL. 121 , pp. 27-31
    • Hanefeld, M.1    Belcher, G.2
  • 31
    • 0035786908 scopus 로고    scopus 로고
    • Insulin resistance and its treatment by thiazolidinediones
    • Lebovitz HE, Banerji MA: Insulin resistance and its treatment by thiazolidinediones. Recent Prog Horm Res 2001;56:265-294.
    • (2001) Recent Prog Horm Res , vol.56 , pp. 265-294
    • Lebovitz, H.E.1    Banerji, M.A.2
  • 32
    • 0000292785 scopus 로고    scopus 로고
    • Poor correlation between 24 hr urinary 6βhydroxycortisol: Cortisol molar ratios (CMR) and plasma midazolam clearance (MDZ CL) as measures of hepatic CYP3A activity
    • Gotzkowsky SK, Kashuba ADM, Hall W, Kulaway RW, Beck DJ, Rocci ML, et al: Poor correlation between 24 hr urinary 6βhydroxycortisol: cortisol molar ratios (CMR) and plasma midazolam clearance (MDZ CL) as measures of hepatic CYP3A activity. Clin Pharm Ther 1999;65(2):167.
    • (1999) Clin Pharm Ther , vol.65 , Issue.2 , pp. 167
    • Gotzkowsky, S.K.1    Kashuba, A.D.M.2    Hall, W.3    Kulaway, R.W.4    Beck, D.J.5    Rocci, M.L.6
  • 33
    • 0028071759 scopus 로고
    • Noninvasive tests of CYP3A enzymes
    • Watkins PB: Noninvasive tests of CYP3A enzymes. Pharmacogenetics 1994;4(4):171-184.
    • (1994) Pharmacogenetics , vol.4 , Issue.4 , pp. 171-184
    • Watkins, P.B.1
  • 34
    • 0031655412 scopus 로고    scopus 로고
    • Effect of troglitazone on urinary excretion of 6β-hydroxycortisol
    • Koup JR, Anderson GD, Loi CM: Effect of troglitazone on urinary excretion of 6β-hydroxycortisol. J Clin Pharmacol 1998;38(9):815-818.
    • (1998) J Clin Pharmacol , vol.38 , Issue.9 , pp. 815-818
    • Koup, J.R.1    Anderson, G.D.2    Loi, C.M.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.