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Details

Stereochemistry ABSOLUTE
Molecular Formula C9H12NO7P
Molecular Weight 277.1678
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FOSLEVODOPA

SMILES

N[C@@H](CC1=CC(O)=C(OP(O)(O)=O)C=C1)C(O)=O

InChI

InChIKey=YNDMEEULGSTYJT-LURJTMIESA-N
InChI=1S/C9H12NO7P/c10-6(9(12)13)3-5-1-2-8(7(11)4-5)17-18(14,15)16/h1-2,4,6,11H,3,10H2,(H,12,13)(H2,14,15,16)/t6-/m0/s1

HIDE SMILES / InChI

Molecular Formula C9H12NO7P
Molecular Weight 277.1678
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23948989 http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021485s20lbl.pdf

Levodopa (L-DOPA) was first isolated from seedlings of Vicia faba by Marcus Guggenheim in 1913. Levodopa, a dopamine precursor, is an effective and well-tolerated dopamine replacement agent used to treat Parkinson's disease. Oral levodopa has been widely used for over 40 years, often in combination with a dopa-decarboxylase inhibitor carbidopa, which reduces many treatment complications, extending its half-life and increasing levodopa availability to the brain. Entacapone, a catechol-O-methyltransferase inhibitor, can also be used to improve the bioavailability of levodopa, especially when used in conjunction with a carbidopa.

Originator

Curator's Comment: # Hoffmann-La Roche

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Stalevo

Approved Use

Stalevo® (carbidopa, levodopa and entacapone) is indicated to treat patients with idiopathic Parkinson’s disease.

Launch Date

2003
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.946 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered: CARBIDOPA, DL-
LEVODOPA plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
84.8 μg × min/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered: CARBIDOPA, DL-
LEVODOPA plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
78.7 min
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered: CARBIDOPA, DL-
LEVODOPA plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
80%
LEVODOPA plasma
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
3 g 1 times / day multiple, oral
Dose: 3 g, 1 times / day
Route: oral
Route: multiple
Dose: 3 g, 1 times / day
Sources:
unhealthy, 54 years
Health Status: unhealthy
Age Group: 54 years
Sex: F
Sources:
Disc. AE: Alopecia...
AEs leading to
discontinuation/dose reduction:
Alopecia (1 patient)
Sources:
420 mg 1 times / day multiple, respiratory
Recommended
Dose: 420 mg, 1 times / day
Route: respiratory
Route: multiple
Dose: 420 mg, 1 times / day
Sources:
unhealthy, adult
84 mg 2 times / day multiple, respiratory
Recommended
Dose: 84 mg, 2 times / day
Route: respiratory
Route: multiple
Dose: 84 mg, 2 times / day
Sources:
unhealthy, adult
Disc. AE: Cough...
AEs leading to
discontinuation/dose reduction:
Cough (2%)
Sources:
0.51 mg/kg 3 times / day steady, oral
Dose: 0.51 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.51 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Other AEs: Headache, Nausea...
Other AEs:
Headache (below serious, 2 patients)
Nausea (below serious, 2 patients)
Sources:
0.76 mg/kg 3 times / day steady, oral
Dose: 0.76 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.76 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Other AEs: Headache, Dry mouth...
Other AEs:
Headache (below serious, 1 patient)
Dry mouth (below serious, 2 patients)
Nausea (below serious, 1 patient)
Fatigue (below serious, 2 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Alopecia 1 patient
Disc. AE
3 g 1 times / day multiple, oral
Dose: 3 g, 1 times / day
Route: oral
Route: multiple
Dose: 3 g, 1 times / day
Sources:
unhealthy, 54 years
Health Status: unhealthy
Age Group: 54 years
Sex: F
Sources:
Cough 2%
Disc. AE
84 mg 2 times / day multiple, respiratory
Recommended
Dose: 84 mg, 2 times / day
Route: respiratory
Route: multiple
Dose: 84 mg, 2 times / day
Sources:
unhealthy, adult
Headache below serious, 2 patients
0.51 mg/kg 3 times / day steady, oral
Dose: 0.51 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.51 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Nausea below serious, 2 patients
0.51 mg/kg 3 times / day steady, oral
Dose: 0.51 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.51 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Headache below serious, 1 patient
0.76 mg/kg 3 times / day steady, oral
Dose: 0.76 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.76 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Nausea below serious, 1 patient
0.76 mg/kg 3 times / day steady, oral
Dose: 0.76 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.76 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Dry mouth below serious, 2 patients
0.76 mg/kg 3 times / day steady, oral
Dose: 0.76 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.76 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Fatigue below serious, 2 patients
0.76 mg/kg 3 times / day steady, oral
Dose: 0.76 mg/kg, 3 times / day
Route: oral
Route: steady
Dose: 0.76 mg/kg, 3 times / day
Sources:
unhealthy, child|adult
Health Status: unhealthy
Age Group: child|adult
Sources:
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Metoclopramide and pimozide in Parkinson's disease and levodopa-induced dyskinesias.
1975 Apr
Reduction of dyskinesia and induction of akinesia induced by morphine in two parkinsonian patients with severe sciatica.
1999
The anticataleptic effect of 7-OH-DPAT: are dopamine D3 receptors involved?
1999
A unified dyskinesias rating scale for L-dopa-induced dyskinesias?
1999
Levodopa-induced dyskinesias treated by pallidotomy.
1999 Aug 1
Comparative effects of unilateral and bilateral subthalamic nucleus deep brain stimulation.
1999 Aug 11
Comparison of pallidal and subthalamic nucleus deep brain stimulation for advanced Parkinson's disease: results of a randomized, blinded pilot study.
1999 Dec
[Levodopa-induced psychosis in patients with idiopathic Parkinson disease].
1999 Feb 27
Drug-induced motor complications in dopa-responsive dystonia: implications for the pathogenesis of dyskinesias and motor fluctuations.
1999 Jul-Aug
Modulation of gastrin processing by vesicular monoamine transporter type 1 (VMAT1) in rat gastrin cells.
1999 Jun 1
Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP.
1999 Nov
Amantadine for levodopa-induced dyskinesias: a 1-year follow-up study.
1999 Nov
Internal globus pallidus discharge is nearly suppressed during levodopa-induced dyskinesias.
1999 Nov
Dopamine D2 receptor gene polymorphism and the risk of levodopa-induced dyskinesias in PD.
1999 Oct 22
The alpha2-adrenergic receptor antagonist idazoxan reduces dyskinesia and enhances anti-parkinsonian actions of L-dopa in the MPTP-lesioned primate model of Parkinson's disease.
1999 Sep
[Amantadine for the treatment of levodopa dyskinesias in Parkinson's disease].
2000
Bilateral subthalamic stimulation for Parkinson's disease by using three-dimensional stereotactic magnetic resonance imaging and electrophysiological guidance.
2000 Apr
L-Dopa uptake and dopamine production in proximal tubular cells are regulated by beta(2)-adrenergic receptors.
2000 Jul
Embryonic ventral mesencephalic grafts improve levodopa-induced dyskinesia in a rat model of Parkinson's disease.
2000 Jul
Population pharmacokinetics of levodopa in patients with Parkinson's disease treated with tolcapone.
2000 Jun
[Worsened orthostatic hypotension due to levodopa administration in a case of Parkinson's disease].
2000 Mar
Levodopa-induced dyskinesias in Parkinson's disease: is sensitization reversible?
2000 May
Centrally initiated postural adjustments in parkinsonian patients on and off levodopa.
2000 Nov
Apomorphine: an underutilized therapy for Parkinson's disease.
2000 Sep
High dose naltrexone for dyskinesias induced by levodopa.
2001 Apr
Localization of a novel locus for autosomal recessive early-onset parkinsonism, PARK6, on human chromosome 1p35-p36.
2001 Apr
Does stimulation of the GPi control dyskinesia by activating inhibitory axons?
2001 Mar
Effects of N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP4) on alpha2-adrenoceptors which regulate the synthesis and release of noradrenaline in the rat brain.
2001 Mar
Coadministration of (-)-OSU6162 with l-DOPA normalizes preproenkephalin mRNA expression in the sensorimotor striatum of primates with unilateral 6-OHDA lesions.
2001 May
Patents

Sample Use Guides

Maximum dosage in a 24-hour period is eight tablets (Stalevo 50, containing 12.5 mg of carbidopa, 50 mg of levodopa and 200 mg of entacapone; Stalevo 75, containing 18.75 mg of carbidopa, 75 mg of levodopa and 200 mg of entacapone; Stalevo 100, containing 25 mg of carbidopa, 100 mg of levodopa and 200 mg of entacapone; Stalevo 125, containing 31.25 mg of carbidopa, 125 mg of levodopa and 200 mg of entacapone; Stalevo 150, containing 37.5 mg of carbidopa, 150 mg of levodopa and 200 mg of entacapone; Stalevo 200, containing 50 mg of carbidopa, 200 mg of levodopa and 200 mg of entacapone). The optimum daily dosage must be determined by careful titration in each patient.
Route of Administration: Oral
Low dose (<30 uM) Levodopa protects PC12 cells against oxidative stress which might be related to the up-regulation of CD39 and pCREB expression.
Substance Class Chemical
Created
by admin
on Tue Apr 01 19:30:58 GMT 2025
Edited
by admin
on Tue Apr 01 19:30:58 GMT 2025
Record UNII
37NQZ0J76I
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
FOSLEVODOPA
INN   USAN  
Official Name English
ABBV-951 COMPONENT FOSLEVODOPA
Preferred Name English
FOSLEVODOPA [USAN]
Common Name English
3-HYDROXY-O-PHOSPHONO-L-TYROSINE
Common Name English
L-TYROSINE, 3-HYDROXY-O-PHOSPHONO-
Common Name English
VYALEV COMPONENT FOSLEVODOPA
Brand Name English
FOSLEVODOPA [JAN]
Common Name English
L-TYROSINE, 3-HYDROXY-, 4-(DIHYDROGEN PHOSPHATE)
Systematic Name English
foslevodopa [INN]
Common Name English
Foslevodopa [WHO-DD]
Common Name English
LEVODOPA-4'-MONOPHOSPHATE
Common Name English
Code System Code Type Description
USAN
HI-136
Created by admin on Tue Apr 01 19:30:58 GMT 2025 , Edited by admin on Tue Apr 01 19:30:58 GMT 2025
PRIMARY
CAS
97321-87-4
Created by admin on Tue Apr 01 19:30:58 GMT 2025 , Edited by admin on Tue Apr 01 19:30:58 GMT 2025
PRIMARY
FDA UNII
37NQZ0J76I
Created by admin on Tue Apr 01 19:30:58 GMT 2025 , Edited by admin on Tue Apr 01 19:30:58 GMT 2025
PRIMARY
INN
11006
Created by admin on Tue Apr 01 19:30:58 GMT 2025 , Edited by admin on Tue Apr 01 19:30:58 GMT 2025
PRIMARY
SMS_ID
300000005928
Created by admin on Tue Apr 01 19:30:58 GMT 2025 , Edited by admin on Tue Apr 01 19:30:58 GMT 2025
PRIMARY
PUBCHEM
127766
Created by admin on Tue Apr 01 19:30:58 GMT 2025 , Edited by admin on Tue Apr 01 19:30:58 GMT 2025
PRIMARY
NCI_THESAURUS
C166651
Created by admin on Tue Apr 01 19:30:58 GMT 2025 , Edited by admin on Tue Apr 01 19:30:58 GMT 2025
PRIMARY
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