"目录号: HY-14728 ee.: 99.75%
Cell Cycle/DNA DamageNF-κB-
Aleglitazar(R1439; RO-0728804)是PPAR-α/γ激动剂，IC50分别为2.8 nM/4.6 nM。
PPAR
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GW9662-Rosiglitazone-Retinoic acid-Troglitazone-Pioglitazone hydrochloride-Elafibranor-GW 501516-CDDO-Im-Fenofibrate-T0070907-Wy-14643-GW0742-Daidzein-FH535-BMS-687453-
生物活性
Description
Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)Target: PPARα/γAleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARα and PPARγ. Aleglitazar is being developed for the treatment of type II diabetes; It is currently in phase III clinical trials. In preliminary clinical studies, Aleglitazar has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. Aleglitazar has beneficial effects on both lipid and glucose parameters and may have a therapeutic role in modifying cardiovascular risk factors and improving glycemic control in patients with T2DM. Aleglitazar combines the lipid benefits of fibrates and the insulin-sensitizing benefits of thiazolidinediones.
Clinical Trial
NCT01197911
Hoffmann-La Roche
Healthy Volunteer
September 2010
Phase 1
NCT01701739
Hoffmann-La Roche
Healthy Volunteer
October 2012
Phase 1
NCT01679639
Hoffmann-La Roche
Healthy Volunteer
August 2012
Phase 1
NCT01711775
Hoffmann-La Roche
Healthy Volunteer
November 2012
Phase 1
NCT01043029
Hoffmann-La Roche
Diabetes Mellitus Type 2
May 2010
Phase 2
NCT01042769
Hoffmann-La Roche
Diabetes Mellitus Type 2
February 2010
Phase 3
NCT01871428
Hoffmann-La Roche
Diabetes Mellitus Type 2
June 2013
Phase 3
NCT01715818
Hoffmann-La Roche
Cardiovascular Disease, Diabetes Mellitus Type 2
December 2012
Phase 3
NCT01691846
Hoffmann-La Roche
Diabetes Mellitus Type 2
October 2012
Phase 3
NCT01188317
Hoffmann-La Roche
Healthy Volunteer
June 2010
Phase 1
NCT01188304
Hoffmann-La Roche
Healthy Volunteer
July 2010
Phase 1
NCT00461006
Hoffmann-La Roche
Diabetes Mellitus Type 2
June 2007
Phase 2
NCT01691755
Hoffmann-La Roche
Diabetes Mellitus Type 2
November 2012
Phase 3
NCT00461058
Hoffmann-La Roche
Diabetes Mellitus Type 2
May 2007
Phase 2
NCT01691989
Hoffmann-La Roche
Diabetes Mellitus Type 2
December 2012
Phase 3
NCT01871415
Hoffmann-La Roche
Diabetes Mellitus Type 2
May 2013
Phase 3
NCT01680978
Hoffmann-La Roche
Diabetes Mellitus Type 2
October 2012
Phase 2
NCT01729403
Hoffmann-La Roche
Diabetes Mellitus Type 2
December 2012
Phase 2
NCT01398267
Hoffmann-La Roche
Diabetes Mellitus Type 2
August 2011
Phase 1
NCT00388518
Hoffmann-La Roche
Diabetes Mellitus Type 2
November 2006
Phase 2
NCT01893242
Hoffmann-La Roche
Diabetes Mellitus Type 2, Kidney Disease, Chronic
December 2013
Phase 3
NCT01615354
Hoffmann-La Roche
Healthy Volunteer
July 2012
Phase 1
NCT01197911
Hoffmann-La Roche
Healthy Volunteer
September 2010
Phase 1
NCT01701739
Hoffmann-La Roche
Healthy Volunteer
October 2012
Phase 1
NCT01679639
Hoffmann-La Roche
Healthy Volunteer
August 2012
Phase 1
NCT01711775
Hoffmann-La Roche
Healthy Volunteer
November 2012
Phase 1
NCT01043029
Hoffmann-La Roche
Diabetes Mellitus Type 2
May 2010
Phase 2
NCT01042769
Hoffmann-La Roche
Diabetes Mellitus Type 2
February 2010
Phase 3
NCT01871428
Hoffmann-La Roche
Diabetes Mellitus Type 2
June 2013
Phase 3
NCT01715818
Hoffmann-La Roche
Cardiovascular Disease, Diabetes Mellitus Type 2
December 2012
Phase 3
NCT01691846
Hoffmann-La Roche
Diabetes Mellitus Type 2
October 2012
Phase 3
NCT01188317
Hoffmann-La Roche
Healthy Volunteer
June 2010
Phase 1
NCT01188304
Hoffmann-La Roche
Healthy Volunteer
July 2010
Phase 1
NCT00461006
Hoffmann-La Roche
Diabetes Mellitus Type 2
June 2007
Phase 2
NCT01691755
Hoffmann-La Roche
Diabetes Mellitus Type 2
November 2012
Phase 3
NCT00461058
Hoffmann-La Roche
Diabetes Mellitus Type 2
May 2007
Phase 2
NCT01691989
Hoffmann-La Roche
Diabetes Mellitus Type 2
December 2012
Phase 3
NCT01871415
Hoffmann-La Roche
Diabetes Mellitus Type 2
May 2013
Phase 3
NCT01680978
Hoffmann-La Roche
Diabetes Mellitus Type 2
October 2012
Phase 2
NCT01729403
Hoffmann-La Roche
Diabetes Mellitus Type 2
December 2012
Phase 2
NCT01398267
Hoffmann-La Roche
Diabetes Mellitus Type 2
August 2011
Phase 1
NCT00388518
Hoffmann-La Roche
Diabetes Mellitus Type 2
November 2006
Phase 2
NCT01893242
Hoffmann-La Roche
Diabetes Mellitus Type 2, Kidney Disease, Chronic
December 2013
Phase 3
NCT01615354
Hoffmann-La Roche
Healthy Volunteer
July 2012
Phase 1
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References
[1].Bénardeau A, Verry P, Atzpodien EA, et al. Effects of the dual PPAR-α/γ agonist aleglitazar on glycaemic control and organ protection in the Zucker diabetic fatty rat. Diabetes Obes Metab. 2013 Feb;15(2):164-74.
[2].Younk LM, Uhl L, Davis SN. Pharmacokinetics, efficacy and safety of aleglitazar for the treatment of type 2 diabetes with high cardiovascular risk. Expert Opin Drug Metab Toxicol. 2011 Jun;7(6):753-63.
[3].Foley-Comer AJ, Young AM, Russell-Yarde F, et al. Aleglitazar, a balanced PPARα/γ agonist, has no clinically relevant pharmacokinetic interaction with high-dose atorvastatin or rosuvastatin. Expert Opin Investig Drugs. 2011 Jan;20(1):3-12.
[4].Cavender MA, Lincoff AM. Therapeutic potential of aleglitazar, a new dual PPAR-α/γ agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16.
[5].Bénardeau A, Benz J, Binggeli A, et al. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes. Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73.