Aleglitazar

"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

相关产品

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.

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