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Anti-Parkinson's disease drugs Pharmacokinetics Chemical property Uses Production method
Entacapone structure
Chemical Name:
Comtan;Comtes; OR-611;Comtess;ENTACAPONE;E Entacapone;Entacapone CRS;ENTACAPONE F·S;Entacapone (150 mg);Entacapone USP/EP/BP
Molecular Formula:
Formula Weight:
MOL File:

Entacapone Properties

Melting point:
Boiling point:
526.6±50.0 °C(Predicted)
1.392±0.06 g/cm3(Predicted)
storage temp. 
DMSO: soluble20mg/mL, clear
pKa ~4.5(at 25℃)
white to light brown
CAS DataBase Reference
130929-57-6(CAS DataBase Reference)
NCI Drug Dictionary
ATC code
  • Risk and Safety Statements
WGK Germany  3
HS Code  2926900005

Entacapone price More Price(10)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0654 Entacapone ≥98% (HPLC) 130929-57-6 10mg $64.8 2021-03-22 Buy
Sigma-Aldrich Y0001249 Entacapone European Pharmacopoeia (EP) Reference Standard 130929-57-6 $190 2021-03-22 Buy
Sigma-Aldrich 1235933 Entacapone United States Pharmacopeia (USP) Reference Standard 130929-57-6 150mg $666 2018-11-13 Buy
Cayman Chemical 14153 Entacapone ≥98% 130929-57-6 10mg $35 2021-03-22 Buy
Cayman Chemical 14153 Entacapone ≥98% 130929-57-6 25mg $61 2021-03-22 Buy

Entacapone Chemical Properties,Uses,Production

Anti-Parkinson's disease drugs

Entacapone is an anti-Parkinson's disease drug which is successfully developed by Orion Pharma company in Swedish. It is a highly selective potent catechol-O-methyltransferase (COMT) inhibitor, rarely penetrating the blood-brain barrier, and primarily acting in the intestinal tract. It is dose-dependent to decrease levels of 3-OMD in serum and the brain, increasing levodopa, dopamine and DOPAC levels in the brain and significantly reducing the dose which is required to increase dopamine concentration in striatal. Levodopa and carbidopa combining with COMTI can significantly increase the bioavailability of levodopa (3-4 times). Activity of COMTI in red blood cell is reversible. When in 800mg dose, the maximum inhibitory activity is up to 82%, so Entacapone combines with levodopa and carbidopa, which can be used for adjuvant therapy of idiopathic Parkinson's disease.


This product is rapid oral absorption, the bioavailability is a dose-dependent with the range of 30% to 45%. In the range of 5~800 mg, pharmacokinetics of Entacapone (abbreviation: Ent) is linear, peak plasma concentration is related to AUC and dose. Food does not affect the absorption of this product, 98% Ent combines with plasma albumin, rarely distributing in tissues. In patients with Parkinson disease (abbreviated: PD), and is required to take levodopa/carbidopa, the peak concentration of Ent arrives within 1~2h. The rate of Ent through the blood-brain barrier is low, the plasma elimination half-life is 1.5~3.5h. After oral administration, Ent (E-configuration) is metabolized to Z-isomer in the blood and is present in plasma and red blood cells. Z-isomer has little impact on the clinical efficacy. Its drug-time curve is similar to Ent. Z-Ent accounts for about 5% of the total AUC. Ent and Z-Ent are acidified by glucose in the liver. After metabolism of Ent: 10% excreted in the urine, 90% of Ent excreted in the feces, only 0.2% excreted in the urine in phony drugs. While taking levodopa in PD patients, and oral Ent 200 mg after elimination half-life of about 1 h, the body has no savings.
Pharmacokinetic study shows that in healthy persons and patients with PD, Ent can increase the bioavailability of levodopa. In the short-term PD patients taking Ent, AUC of levodopa increase 25%, while the long-term taking Ent can increase 50%. AUC of 3-OMD relatively reduces 60%. In these studies, they found that plasma peak time of levodopa will be extended. Single dose of Entacapone (while not taking levodopa/carbidopa), in patients with liver disease, the patient's AUC and Cmax is 2 times of the patients with normal liver function. We should adjust the dosage of the patient. In patients with mild to moderate kidney disease, it is not necessary to adjust the dosage. Kidney patients receiving dialysis can extend dosing interval.
The above information is edited by the Chemicalbook of Liu Yujie.

Chemical property

Crystals, melting point 162--163 ℃.


As COMT inhibitors, it is used to treat Parkinson's disease.

Production method

1.83 g 3,4-dihydroxy-5-nitrobenzaldehyde and 1.5g N, N-diethyl-cyanoacetamide and a catalytic amount of piperidine acetate are dissolved in 40ml of dry ethanol , followed by stirring overnight , 2.23 g crude product is obtained, yield 73%, melting point 153~156 ℃.
Heated at 90 ℃, the 3.0 kg crude product is dissolved in 8.0kg acetic acid (or formic acid) containing 80 g HBr (or 40gHCl).It is slowly cooled to 20 ℃, and stirred at this temperature for 20h, then at 15 ℃ stirred for 6h. The precipitated crystals were collected by filtration, carefully washed with cool (4 ℃) 1L toluene-acetic acid (1: l v/v) mixed solution, and washed with 1L cold toluene. It is dried at 45 ℃under vacuum and 2.4kg crystalline pure Entacapone is obtained, yield 80%, melting point 162-163 ℃.


Entacapone was introduced in Finland, Germany and Sweden as an adjunctive treatment with L-dopa in Parkinson’s disease. Entacapone is the second drug in its class to reach the market; it can be obtained by basecatalyzed condensation of the corresponding benzaldehyde with a cyanoacetamide. Entacapone is a highly selective and orally-active catechol-0- methyltransferase (COMT) inhibitor ; by inhibiting metabolism of L-dopa when given as an adjuvant in patients with Parkinson’s disease, Entacapone markedly prolongs the effects of L-dopa and improves its bioavailability. Results from clinical studies showed that 200mglday Entacapone coadministered with L-dopa lowered the dose of the latter required to reduce fluctuations in motor performance.

Chemical Properties

Yellow Crystalline Solid


Orion Pharma (Finland)


(E)-Isomer of Entacapone polymorphic form A. Peripherally acting inhibitor of catechol-O-methyl transferase (COMT), an enzyme involved in the metabolism of catecholamine neurotransmitters and related drugs. Antiparkinsonian


antiparkinsinian;catechol-O-methyl transferase inhibitor


This compound belongs to the cinnamic acid amides. These are amides of cinnamic acids. Used as an adjunct to levodopa / carbidopa in the symptomatic treatment of patients with idiopathic Parkinson's Disease who experience the signs and symptoms of end-of-


ChEBI: A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5 nitrophenyl group.

Manufacturing Process

N,N-Diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide (2- Propenamide, 2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl).
A solution containing 1.83 g of 3,4-dihydroxy-5-nitrobenzaldehyde, 1.5 g of N,N-diethylcyanoacetamide and catalytic amount of piperidine acetate in 40 ml of dry ethanol was refluxed over night. After cooling the solvent was evaporated in vacuo and the residue was recrystallized from waterdimethylformamide. Yield of desired product was 2.23 g (73%), melting point 153°-156°C.

brand name


Therapeutic Function


General Description

Entacapone, (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide (Comtan),is a nitrocatechol that is practically insoluble in water (pKa=4.50). Entacapone is rapidly absorbed after oral administrationand does not cross the BBB. Entacapone does not distributewidely into tissues because of its high plasma proteinbinding and it is completely metabolized before excretion.The main metabolic pathway is by isomerization to the cisisomerfollowed by direct glucuronidation of the parent andthe cis-isomer. The glucuronide conjugates are inactive.Entacapone is eliminated in the feces (90%) and urine (10%).Entacapone is indicated as an adjunct to levodopa/carbidopato treat patients with idiopathic PD who experience the signsand symptoms of end-of-dose wearing off.

Entacapone Preparation Products And Raw materials

Raw materials

Preparation Products

Entacapone Suppliers

Global( 286)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 China 20012 60
Henan DaKen Chemical CO.,LTD.
+86-371-66670886 China 20914 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693 CHINA 22607 55
Guangzhou PI PI Biotech Inc
020-81716319; China 3245 55
career henan chemical co
+86-371-86658258 CHINA 29954 58
08657186217390 CHINA 310 58
Hubei Jusheng Technology Co.,Ltd.
027-59599243 CHINA 28229 58
Shandong chuangyingchemical Co., Ltd.
18853181302 CHINA 5917 58
BOC Sciences
1-631-614-7828 United States 19752 58
Chongqing Chemdad Co., Ltd
+86-13650506873 CHINA 37282 58

View Lastest Price from Entacapone manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-11-30 Entacapone
US $543.00 / KG 100g 99% 1000kg/month Shanxi Lianxu New Material Co., LTD
2021-07-28 Entacapone USP/EP/BP
US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited
2019-07-06 Entacapone
US $2.00 / kg 1kg 99% 100kg career henan chemical co

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