U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C14H11NO5
Molecular Weight 273.2408
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TOLCAPONE

SMILES

CC1=CC=C(C=C1)C(=O)C2=CC(=C(O)C(O)=C2)[N+]([O-])=O

InChI

InChIKey=MIQPIUSUKVNLNT-UHFFFAOYSA-N
InChI=1S/C14H11NO5/c1-8-2-4-9(5-3-8)13(17)10-6-11(15(19)20)14(18)12(16)7-10/h2-7,16,18H,1H3

HIDE SMILES / InChI

Description
Curator's Comment: Description was created based on several sources, including

Tolcapone is a potent, selective, and reversible inhibitor of catechol-O-methyltransferase (COMT). In humans, COMT is distributed throughout various organs. COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure. Physiological substrates of COMT include dopa, catecholamines (dopamine, norepinephrine, epinephrine) and their hydroxylated metabolites. The function of COMT is the elimination of biologically active catechols and some other hydroxylated metabolites. COMT is responsible for the elimination of biologically active catechols and some other hydroxylated metabolites. In the presence of a decarboxylase inhibitor, COMT becomes the major metabolizing enzyme for levodopa catalyzing it to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD) in the brain and periphery. When tolcapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that these sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to greater effects on the signs and symptoms of Parkinson's disease in patients as well as increased levodopa adverse effects, sometimes requiring a decrease in the dose of levodopa. The precise mechanism of action of tolcapone is unknown, but it is believed to be related to its ability to inhibit COMT and alter the plasma pharmacokinetics of levodopa, resulting in an increase in plasma levodopa concentrations. The inhibition of COMT also causes a reduction in circulating 3-OMD as a result of decreased peripheral metabolism of levodopa. This may lead to an increase distribution of levodopa into the CNS through the reduction of its competitive substrate, 3-OMD, for transport mechanisms. Sustained levodopa concentrations presumably result in more consistent dopaminergic stimulation, resulting in greater reduction in the manifestations of parkinsonian syndrome. Tolcapone is used as an adjunct to levodopa/carbidopa therapy for the symptomatic treatment of Parkinson's Disease. This drug is generally reserved for patients with parkinsonian syndrome receiving levodopa/carbidopa who are experiencing symptom fluctuations and are not responding adequately to or are not candidates for other adjunctive therapies. Tolcapone is sold under the brand name Tasmar.

CNS Activity

Curator's Comment: Tolcapone enters the CNS to a minimal extent, but has been shown to inhibit central COMT activity in animals.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
151.0 nM [IC50]
29.3 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Tasmar

Approved Use

TASMAR is indicated as an adjunct to levodopa and carbidopa for the treatment of the signs and symptoms of idiopathic Parkinson’s disease. Because of the risk of potentially fatal, acute fulminant liver failure, TASMAR (tolcapone) should ordinarily be used in patients with Parkinson’s disease on l-dopa/carbidopa who are experiencing symptom fluctuations and are not responding satisfactorily to or are not appropriate candidates for other adjunctive therapies. Because of the risk of liver injury and because TASMAR, when it is effective, provides an observable symptomatic benefit, the patient who fails to show substantial clinical benefit within 3 weeks of initiation of treatment, should be withdrawn from TASMAR.

Launch Date

8.859456E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.3 mg/L
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.7 mg/L
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4.6 mg/L
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6.3 mg/L
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.3 mg/L
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
13.4 mg/L
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
2.4 mg/L
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
20.3 mg/L
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
0.5 mg × h/L
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.1 mg × h/L
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
12.2 mg × h/L
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
18.5 mg × h/L
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2.8 mg × h/L
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
43.8 mg × h/L
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
5.7 mg × h/L
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
67.7 mg × h/L
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.7 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.7 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2.1 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.6 h
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2.2 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
1.7 h
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3.4 h
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TOLCAPONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.1%
unknown, unknown
TOLCAPONE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
800 mg 3 times / day multiple, oral
Overdose
Dose: 800 mg, 3 times / day
Route: oral
Route: multiple
Dose: 800 mg, 3 times / day
Co-administed with::
L-dopa, po(100 mg, tid)
carbidopa, po(25 mg, tid)
Sources:
healthy, 55 - 75
n = 6
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (severe, 33%)
Vomiting (severe, 33%)
Sources:
800 mg 3 times / day multiple, oral
Overdose
Dose: 800 mg, 3 times / day
Route: oral
Route: multiple
Dose: 800 mg, 3 times / day
Sources: Page: p.25
healthy
Disc. AE: Dizziness...
AEs leading to
discontinuation/dose reduction:
Dizziness
Sources: Page: p.25
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.21, p.12
unhealthy
n = 592
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 592
Sources: Page: p.21, p.12
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (6%)
Sources: Page: p.21, p.12
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.1, p.21
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.1, p.21
Disc. AE: Acute liver failure, Hepatocellular injury...
AEs leading to
discontinuation/dose reduction:
Acute liver failure (grade 3-5)
Hepatocellular injury (grade 3-5)
Sources: Page: p.1, p.21
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.10
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.10
Disc. AE: ALT increased, Aspartate aminotransferase increased...
AEs leading to
discontinuation/dose reduction:
ALT increased (1.7%)
Aspartate aminotransferase increased (1.7%)
Sources: Page: p.10
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.11
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.11
Disc. AE: Somnolence...
AEs leading to
discontinuation/dose reduction:
Somnolence (1%)
Sources: Page: p.11
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.21
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.21
Disc. AE: Hallucinations...
AEs leading to
discontinuation/dose reduction:
Hallucinations (1%)
Sources: Page: p.21
AEs

AEs

AESignificanceDosePopulation
Nausea severe, 33%
Disc. AE
800 mg 3 times / day multiple, oral
Overdose
Dose: 800 mg, 3 times / day
Route: oral
Route: multiple
Dose: 800 mg, 3 times / day
Co-administed with::
L-dopa, po(100 mg, tid)
carbidopa, po(25 mg, tid)
Sources:
healthy, 55 - 75
n = 6
Vomiting severe, 33%
Disc. AE
800 mg 3 times / day multiple, oral
Overdose
Dose: 800 mg, 3 times / day
Route: oral
Route: multiple
Dose: 800 mg, 3 times / day
Co-administed with::
L-dopa, po(100 mg, tid)
carbidopa, po(25 mg, tid)
Sources:
healthy, 55 - 75
n = 6
Dizziness Disc. AE
800 mg 3 times / day multiple, oral
Overdose
Dose: 800 mg, 3 times / day
Route: oral
Route: multiple
Dose: 800 mg, 3 times / day
Sources: Page: p.25
healthy
Diarrhea 6%
Disc. AE
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.21, p.12
unhealthy
n = 592
Health Status: unhealthy
Condition: Parkinson’s disease
Population Size: 592
Sources: Page: p.21, p.12
Acute liver failure grade 3-5
Disc. AE
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.1, p.21
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.1, p.21
Hepatocellular injury grade 3-5
Disc. AE
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.1, p.21
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.1, p.21
ALT increased 1.7%
Disc. AE
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.10
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.10
Aspartate aminotransferase increased 1.7%
Disc. AE
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.10
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.10
Somnolence 1%
Disc. AE
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.11
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.11
Hallucinations 1%
Disc. AE
200 mg 3 times / day multiple, oral
Recommended
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Co-administed with::
L-dopa, po
carbidopa, po
Sources: Page: p.21
unhealthy
Health Status: unhealthy
Condition: Parkinson’s disease
Sources: Page: p.21
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



OverviewOther

Other InhibitorOther SubstrateOther Inducer





Drug as perpetrator​Drug as victim
PubMed

PubMed

TitleDatePubMed
Inhibition of catechol-O-methyltransferase (COMT) in the brain does not affect the action of dopamine and levodopa: an in vitro electrophysiological evidence from rat mesencephalic dopamine neurons.
1999
Vitiligo associated with tolcapone and levodopa in a patient with Parkinson's disease.
1999 Nov
Tolcapone increases maximum concentration of levodopa.
2000
Neuroleptic malignant-like syndrome in an elderly patient caused by abrupt withdrawal of tolcapone, a-catechol-o-methyl transferase inhibitor.
2000 Apr 15
Population pharmacokinetics of levodopa in patients with Parkinson's disease treated with tolcapone.
2000 Jun
Neuroleptic malignant-like syndrome and acute hepatitis during tolcapone and clozapine medication.
2001
Catechol-O-methyltransferase inhibitors in the management of Parkinson's disease.
2001
Comparative toxicological study on the hepatic safety of entacapone and tolcapone in the rat.
2001
Comparison of two dosages of tolcapone added to levodopa in nonfluctuating patients with PD.
2001 Jul-Aug
D1-like dopamine receptor activation and natriuresis by nitrocatechol COMT inhibitors.
2001 May
Approaching disturbed sleep in late Parkinson's Disease: first step toward a proposal for a revised UPDRS.
2001 Oct
Randomized trial of tolcapone versus pergolide as add-on to levodopa therapy in Parkinson's disease patients with motor fluctuations.
2001 Sep
Pharmacogenetic analysis of adverse drug effect reveals genetic variant for susceptibility to liver toxicity.
2002
DA agonists -- ergot derivatives: bromocriptine: management of Parkinson's disease.
2002
Catechol-O-methyltransferase and Parkinson's disease.
2002 Feb
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
2002 Jan 31
Dopaminergic transmission in the rat striatum in vivo in conditions of pharmacological modulation.
2002 Mar-Apr
Different modes of action of catecholamine-O-methyltransferase inhibitors entacapone and tolcapone on adenylyl cyclase activity in vitro.
2002 May
Different toxicological profile of two COMT inhibitors in vivo: the role of uncoupling effects.
2002 Nov
Mechanisms of idiosyncratic drug reactions: the case of felbamate.
2002 Nov 10
Effects of entacapone and tolcapone on mitochondrial membrane potential.
2002 Oct 18
Modifications of plasma and platelet levels of L-DOPA and its direct metabolites during treatment with tolcapone or entacapone in patients with Parkinson's disease.
2003 Aug
Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat.
2003 Feb
Effects of peripheral and central catechol-O-methyltransferase inhibition on striatal extracellular levels of dopamine: a microdialysis study in freely moving rats.
2003 Jan
Tissue histopathology, clinical chemistry and behaviour of adult Comt-gene-disrupted mice.
2003 Jul-Aug
Assessment of catechol induction and glucuronidation in rat liver microsomes.
2004 Dec
Safety and tolerability of COMT inhibitors.
2004 Jan 13
Differences in toxicity of the catechol-O-methyl transferase inhibitors, tolcapone and entacapone to cultured human neuroblastoma cells.
2004 Mar
Clinical advantages of COMT inhibition with entacapone - a review.
2004 Oct
Catechol-O-methyltransferase inhibitors for levodopa-induced complications in Parkinson's disease.
2004 Oct 18
SL25.1131 [3(S),3a(S)-3-methoxymethyl-7-[4,4,4-trifluorobutoxy]-3,3a,4,5-tetrahydro-1,3-oxazolo[3,4-a]quinolin-1-one], a new, reversible, and mixed inhibitor of monoamine oxidase-A and monoamine oxidase-B: biochemical and behavioral profile.
2004 Sep
[Tolcapone treatment of late stages of Parkinson's disease].
2005
Oxidative stress mediated idiosyncratic drug toxicity.
2005
Tolcapone: a review of its use in the management of Parkinson's disease.
2005
The combination of liquid chromatography/tandem mass spectrometry and chip-based infusion for improved screening and characterization of drug metabolites.
2005
The effect of nicotine in combination with various dopaminergic drugs on nigrostriatal dopamine in rats.
2005 Jun
Prediction of genotoxicity of chemical compounds by statistical learning methods.
2005 Jun
Rapid simultaneous determination of metabolic clearance of multiple compounds catalyzed in vitro by recombinant human UDP-glucuronosyltransferases.
2005 Jun 1
Transcriptional and behavioral interaction between 22q11.2 orthologs modulates schizophrenia-related phenotypes in mice.
2005 Nov
Pharmacokinetic optimisation in the treatment of Parkinson's disease : an update.
2006
Tolcapone: new drug. In Parkinson's disease: unacceptable risk of severe hepatitis.
2006 Apr
Optimal design for multivariate response pharmacokinetic models.
2006 Apr
Practice Parameter: treatment of Parkinson disease with motor fluctuations and dyskinesia (an evidence-based review): report of the Quality Standards Subcommittee of the American Academy of Neurology.
2006 Apr 11
Tolcapone decreases plasma levels of S-adenosyl-L-homocysteine and homocysteine in treated Parkinson's disease patients.
2006 Jun
Treatment of cognitive deficits associated with schizophrenia: potential role of catechol-O-methyltransferase inhibitors.
2007
The endophenotype concept in psychiatric genetics.
2007 Feb
Entacapone to tolcapone switch: Multicenter double-blind, randomized, active-controlled trial in advanced Parkinson's disease.
2007 Jan
Tolcapone improves cognition and cortical information processing in normal human subjects.
2007 May
Increased catechol-O-methyltransferase activity and protein expression in OX-42-positive cells in the substantia nigra after lipopolysaccharide microinfusion.
2007 Nov-Dec
Safety and tolerability of adjunctive tolcapone treatment in patients with early Parkinson's disease.
2007 Sep
Patents

Sample Use Guides

The initial dose of TASMAR is always 100 mg three times per day. The recommended daily dose of TASMAR is also 100 mg tid.
Route of Administration: Oral
When using a fixed amount of total protein (2 ug/ml), but variable concentrations of COMT, the inhibitory potency of tolcapone upon S- and MB-COMT activity in the rat brain was in the low nM range (IC50's of 2 and 3 nM, respectively), whereas in rat liver the IC50 values for tolcapone against liver MB- and S-COMT (IC50's of 123 and 795 nM, respectively) were markedly higher than those observed in the brain. By contrast, when inhibition studies were performed with a fixed concentration of COMT (15 nM), tolcapone was found to be endowed with the same potency (in the low nM range) in inhibiting S- and MB-COMT from both brain and liver.
Name Type Language
TOLCAPONE
EMA EPAR   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN   INN  
Official Name English
Tolcapone [WHO-DD]
Common Name English
RO-407592
Code English
TOLCAPONE [USP MONOGRAPH]
Common Name English
TOLCAPONE [MI]
Common Name English
TOLCAPONE [MART.]
Common Name English
TOLCAPONE [ORANGE BOOK]
Common Name English
TOLCAPONE [USAN]
Common Name English
RO-40-7592
Code English
TOLCAPONE [JAN]
Common Name English
TOLCAPONE [EMA EPAR]
Common Name English
RO 40-7592
Code English
3,4-DIHYDROXY-4'-METHYL-5-NITROBENZOPHENONE
Systematic Name English
tolcapone [INN]
Common Name English
TOLCAPONE [VANDF]
Common Name English
TOLCAPONE [USP-RS]
Common Name English
TASMAR
Brand Name English
METHANONE, (3,4-DIHYDROXY-5-NITROPHENYL)(4-METHYLPHENYL)-
Systematic Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS TASMAR (AUTHORIZED: PARKINSON DISEASE)
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
NDF-RT N0000175756
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
WHO-ATC N04BX01
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
WHO-VATC QN04BX01
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
LIVERTOX NBK548573
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
FDA ORPHAN DRUG 413913
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
NDF-RT N0000175757
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
NCI_THESAURUS C38149
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
Code System Code Type Description
EVMPD
SUB11151MIG
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
SMS_ID
100000089195
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
RXCUI
72937
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY RxNorm
USAN
FF-11
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
PUBCHEM
4659569
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
MERCK INDEX
M10938
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY Merck Index
RS_ITEM_NUM
1670207
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
DRUG BANK
DB00323
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
EPA CompTox
DTXSID3023685
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
WIKIPEDIA
TOLCAPONE
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
INN
6873
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
ChEMBL
CHEMBL1324
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
CHEBI
63630
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
CAS
134308-13-7
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
IUPHAR
6646
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
LACTMED
Tolcapone
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
DRUG CENTRAL
2697
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
DAILYMED
CIF6334OLY
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
FDA UNII
CIF6334OLY
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
MESH
C066340
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY
NCI_THESAURUS
C47762
Created by admin on Thu Jul 06 23:08:05 UTC 2023 , Edited by admin on Thu Jul 06 23:08:05 UTC 2023
PRIMARY