"目录号: HY-14280A
Metabolic Enzyme/ProteaseNeuronal Signaling-
Entacapone是特异的儿茶酚-o-甲基转移酶（COMT）抑制剂，IC50为151 nM。
COMT
相关产品
Tolcapone-Opicapone-Entacapone-
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].Di Giovanni, S., et al., 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. 285(20): p. 14941-54.
[2].Jenner, P., Avoidance of dyskinesia: preclinical evidence for continuous dopaminergic stimulation. Neurology, 2004. 62(1 Suppl 1): p. S47-55.
[3].Hamaue, N., et al., Entacapone, a catechol-O-methyltransferase inhibitor, improves the motor activity and dopamine content of basal ganglia in a rat model of Parkinson's disease induced by Japanese encephalitis virus. Brain Res, 2010. 1309: p. 110-5.