"目录号: HY-14280

Metabolic Enzyme/ProteaseNeuronal Signaling-

Entacapone是特异的外周活性的邻苯二酚-O-甲基转移酶（COMT）抑制剂，IC50为151 nM。

COMT

相关产品

Tolcapone-Opicapone-Entacapone sodium salt-

生物活性

Description

Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.IC50 Value: 151 nMTarget: COMTin vitro: Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.in vivo:  Levodopa/carbidopa/entacapone has been shown to improve the pharmacokinetic profile of levodopa and provide superior symptomatic control compared with conventional levodopa/dopa decarboxylase inhibitor therapy. We report four case histories describing clinical experience of using levodopa/carbidopa/entacapone 200/50/200 mg, one of the latest doses of this formulation, in a range of patients with Parkinson's disease. These cases illustrate that levodopa/carbidopa/entacapone 200/50/200 mg provides improvements in symptomatic control.Clinical trial: The combination product carbidopa/levodopa/entacapone (CLE) was approved in 2003 for the treatment of PD patients.

Clinical Trial

NCT02349243

Kaichun Wu-National Institute of Biological Sciences, Beijing-Fourth Military Medical University

Obesity

January 2015

Phase 1-Phase 2

NCT00373087

Assistance Publique - Hôpitaux de Paris

Parkinson's Disease

October 2006

Phase 4

NCT00192855

Rambam Health Care Campus

Schizophrenia

June 2003

NCT00547911

National Institute of Neurological Disorders and Stroke (NINDS)-National Institutes of Health Clinical Center (CC)

Parkinson Disease-Multiple System Atrophy-Autonomic Nervous System Diseases

October 2007

Phase 1-Phase 2

NCT00391898

Novartis

Parkinson's Disease

October 2006

Phase 4

NCT02058966

Oregon Health and Science University-Portland VA Medical Center

Methamphetamine Dependence

June 2014

Early Phase 1

NCT00237263

Novartis

Parkinson's Disease

February 2003

Phase 2

NCT00219284

Novartis Pharmaceuticals-Novartis

Parkinson's Disease With End of Dose Wearing Off

January 2005

Phase 4

NCT00099268

Novartis Pharmaceuticals-Orion Corporation, Orion Pharma-Novartis

Parkinson's Disease

September 2004

Phase 3

NCT00642356

Novartis

Parkinson's Disease

March 2008

Phase 4

NCT00415740

Novartis

Healthy

May 2006

Phase 1

NCT00415831

Novartis

Healthy

June 2006

Phase 1

NCT00415922

Novartis

Healthy

July 2006

Phase 1

NCT00415844

Novartis

Healthy

June 2006

Phase 1

NCT01130493

IMPAX Laboratories, Inc.

Parkinson's Disease

May 2010

Phase 3

NCT01437293

New York State Psychiatric Institute-National Institute on Drug Abuse (NIDA)-Columbia University

Cocaine Abuse

August 2010

Phase 1

NCT00143026

Novartis

Parkinson's Disease

July 2005

Phase 4

NCT00134966

Novartis

Parkinson's Disease

August 2005

Phase 3

NCT00601978

Novartis Pharmaceuticals-Novartis

Parkinson's Disease

August 2008

Phase 4

NCT01158950

University of California, San Francisco-University of California, Berkeley-United States Department of Defense

Impulsive Behavior

March 2010

NCT01568073

Bial - Portela C S.A.

Parkinson's Disease

March 2011

Phase 3

NCT01468012

New York State Psychiatric Institute

Cocaine Dependence

July 2014

Phase 2-Phase 3

NCT01840423

Orion Corporation, Orion Pharma

Healthy

May 2013

Phase 1

NCT00200447

Molecular NeuroImaging

Parkinson's Disease

March 2004

Phase 2

NCT01688089

Orion Corporation, Orion Pharma

Healthy

September 2012

Phase 1

NCT00906828

Uppsala University-Swedish Parkinson's Disease Foundation-Swedish Society for Medical Research

Parkinson Disease

October 2008

Phase 4

NCT02170376

Bial - Portela C S.A.

Parkinson's Disease (PD)

September 2011

Phase 1

NCT00491998

Vernalis (R&D) Ltd-Cita NeuroPharmaceuticals-INC Research

Parkinson's Disease

November 2006

Phase 1-Phase 2

NCT00562198

Orion Corporation, Orion Pharma

Parkinson´s Disease

January 2008

Phase 2

NCT00125567

Orion Corporation, Orion Pharma

Idiopathic Parkinson's Disease

August 2005

Phase 4

NCT01070628

Orion Corporation, Orion Pharma

Parkinson's Disease

December 2009

Phase 1

NCT01519284

Bial - Portela C S.A.

Parkinson Disease

November 2009

Phase 1

NCT02554734

Orion Corporation, Orion Pharma

Parkinson's Disease

August 2015

Phase 1

NCT00693862

Orion Corporation, Orion Pharma

Pharmacokinetics

December 2006

Phase 1

NCT00262470

Satish R. Raj-National Institutes of Health (NIH)-Vanderbilt University

Tachycardia-Chronic Orthostatic Intolerance

April 1997

Phase 1-Phase 2

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References

[1].Piccini P, Brooks DJ, Korpela K, The catechol-O-methyltransferase(COMT) inhibitor entacapone enhances the pharmacokinetic and clinical response to Sinemet CR in Parkinson's disease. J Neurol Neurosurg Psychiatry. 2000 May;68(5):589-94.

[2].Di Giovanni S, Eleuteri S, Paleologou KE, Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J Biol Chem. 2010 May 14;285(20):1494

[3].Sethi KD, Hauser RA, Isaacson SH, Levodopa/carbidopa/entacapone 200/50/200 mg (Stalevo 200) in the treatment of Parkinson's disease: a case series. Cases J. 2009 Jul 30;2:7134.

[4].Poulopoulos M, Waters C. Carbidopa/levodopa/entacapone: the evidence for its place in the treatment of Parkinson's disease. Core Evid. 2010 Jul 27;5:1-10.