Lacosamide

Identification

Summary

Lacosamide is an antiepileptic drug used to treat partial-onset seizures and primary generalized tonic-clonic seizures.

Brand Names
Motpoly, Vimpat
Generic Name
Lacosamide
DrugBank Accession Number
DB06218
Background

Lacosamide is an antiepileptic drug used to treat seizures. As a chiral functionalized amino acid, it works by blocking slowly inactivating components of voltage-gated sodium currents. Lacosamide exhibits a stereoselective mode of interaction with sodium channels.3 Lacosamide was first approved by the European Commission in August 2008 and was later approved by the FDA in October 2008.3 It was granted approval by Health Canada in September 2010.9

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 250.2936
Monoisotopic: 250.131742452
Chemical Formula
C13H18N2O3
Synonyms
  • (+)-(2R)-2-(ACETYLAMINO)-N-BENZYL-3-METHOXYPROPANAMIDE
  • (2R)-2-(Acetylamino)-3-methoxy-N-(phenylmethyl)propanamide
  • (R)-2-acetamido-N-benzyl-3- methoxypropionamide
  • (R)-LACOSAMIDE 1
  • Erlosamide
  • Harkoseride
  • Lacosamida
  • Lacosamide
  • Propanamide, 2-(acetylamino)-3-methoxy-N-(phenylmethyl)-, (2R)-
External IDs
  • ADD 243037
  • ADD-243037
  • ADD243037
  • SPM 927
  • SPM-927
  • SPM927

Pharmacology

Indication

In the US and Europe, lacosamide is indicated for the treatment of partial-onset seizures in children and adults.6,7,8 In Canada, it is reserved for use in adults.9

It is also used as an adjunctive therapy in the treatment of primary generalized tonic-clonic seizures in patients four years of age and older.6,8

The extended-release capsules of lacosamide are indicated for the treatment of partial-onset seizures in adults and in pediatric patients weighing at least 50 kg.7

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct therapy in management ofPartial-onset seizures••••••••••••••••••
Management ofPartial-onset seizures••••••••••••••••••
Management ofPartial-onset seizures••••••••••••••••••••••••••• ••••••• •••• ••••••
Adjunct therapy in management ofPartial-onset seizures••••••••••••••••••••••••••• •••••••• •• •••••••••••• ••••••••••••••••• ••••••• •••• ••••••
Management ofPartial-onset seizures•••••••••••••••••••••• ••••••••• ••••••• •••• ••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Lacosamide is an antiepileptic drug with high oral potency, stereoselectivity,4 and anticonvulsant effects.2 By blocking sensory neuronal voltage-gated sodium channels that mediate neuropathic pain responses, lacosamide was shown to possess analgesic activity.1,2 Lacosamide is a chiral functionalized amino acid. The S-stereoisomer does not exhibit antiepileptic activity.2

Mechanism of action

Caused by neuronal hyperexcitability, seizures in epilepsy involve sustained firing of sodium-dependent action potentials. The slow inactivation process, intrinsic to voltage-gated sodium channel functioning, has been implicated in the paroxysmal depolarizing shifts associated with epileptic activity.2 The exact mechanism of action of lacosamide is not fully known; however, in vitro electrophysiological studies have shown that lacosamide selectively enhances the slow inactivation of voltage-gated sodium channels, shifting the slow inactivation curve to more hyperpolarized potentials and augmenting the maximal fraction of channels in the slow inactivated state.4 This results in the stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing.2,6 Lacosamide does not affect the fast component of voltage-gated sodium currents, unlike traditional sodium channel blockers.2

TargetActionsOrganism
USodium channel protein type 9 subunit alpha
blocker
Humans
USodium channel protein type 3 subunit alpha
blocker
Humans
USodium channel protein type 10 subunit alpha
blocker
Humans
Absorption

Lacosamide is completely absorbed after oral administration with negligible first-pass effect. It has a high absolute bioavailability of approximately 100%. Food does not affect the rate and extent of absorption. The Tmax ranges from one to four hours. Steady-state plasma concentrations are achieved after three days of twice-daily repeated administration. The pharmacokinetics of lacosamide are dose-proportional over the dose range between 100 and 800 mg, and time-invariant, with low inter- and intra-subject variability. The major O-desmethyl metabolite of lacosamide has a longer Tmax that ranges from 0.5 to 12 hours.6

After intravenous administration, Cmax is reached at the end of infusion. The 30- and 60-minute intravenous infusions are bioequivalent to the oral tablet. For the 15-minute intravenous infusion, bioequivalence was met for AUC0-tz but not for Cmax. The point estimate of Cmax was 20% higher than Cmax for oral tablet and the 90% CI for Cmax exceeded the upper boundary of the bioequivalence range. In a trial comparing the oral tablet with an oral solution containing 10 mg/mL lacosamide, bioequivalence between both formulations was shown. A single loading dose of 200 mg approximates steady-state concentrations comparable to the 100 mg twice-daily oral administration.6

Volume of distribution

The volume of distribution is approximately 0.6 L/kg and thus close to the volume of total body water.6

Protein binding

Lacosamide is less than 15% bound to plasma proteins.6

Metabolism

Lacosamide is metabolized by CYP3A4, CYP2C9, and CYP2C19 to form O-desmethyl lacosamide, which is a major, pharmacologically inactive metabolite in humans. There is no enantiomeric interconversion of lacosamide.6

Hover over products below to view reaction partners

Route of elimination

Lacosamide is primarily eliminated from the systemic circulation by renal excretion and biotransformation. After oral and intravenous administration of 100 mg radiolabeled lacosamide, approximately 95% of the radioactivity was recovered in the urine and less than 0.5 % in the feces. The major compounds excreted were unchanged lacosamide (approximately 40% of the dose), its O-desmethyl metabolite (approximately 30%), and a structurally unknown polar fraction (~20%).6

Half-life

The elimination half-life of the unchanged drug is approximately 13 hours and is not altered by different doses, multiple dosing or intravenous administration. The major O-desmethyl metabolite of lacosamide has an elimination half-life ranging from 15 to 23 hours).6

Clearance

Not Available

Adverse Effects
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Toxicity

The oral LD50 in rats is 253 mg/kg.5

Dizziness, nausea, and seizures (generalized tonic-clonic seizures, status epilepticus) were observed at doses greater than 800 mg, which is twice the maximum recommended daily dose. Cardiac conduction disorders, confusion, decreased level of consciousness, cardiogenic shock, cardiac arrest, and coma have also been observed.6

Fatal overdoses have occurred with lacosamide. As there is no specific antidote for overdose with lacosamide, standard decontamination procedures should be followed. General supportive care of the patient is indicated including monitoring of vital signs and observation of the clinical status of patient. Standard hemodialysis procedures result in significant clearance of lacosamide (reduction of systemic exposure by 50% in four hours). Hemodialysis may be indicated based on the patient's clinical state or in patients with significant renal impairment.6

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2C19CYP2C19*2ANot Available681G>AEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*2BNot Available681G>AEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*3Not Available636G>AEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*4Not Available1A>GEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*5Not Available1297C>TEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*6Not Available395G>AEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*7Not Available19294T>AEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*22Not Available557G>C / 991A>GEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*24Not Available99C>T / 991A>G  … show all Effect InferredReduced O-desmethyl metabolite concentrations in plasma.Details
Cytochrome P450 2C19CYP2C19*35Not Available12662A>GEffect InferredReduced O-desmethyl metabolite concentrations in plasma.Details

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Lacosamide can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Lacosamide can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Lacosamide.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Lacosamide.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Lacosamide.
Food Interactions
  • Take with or without food. Food does not affect the rate and extent of absorption.

Products

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Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Alembic-lacosamideTablet100 mgOralAlembic Pharmaceuticals LimitedNot applicableNot applicableCanada flag
Alembic-lacosamideTablet200 mgOralAlembic Pharmaceuticals LimitedNot applicableNot applicableCanada flag
Alembic-lacosamideTablet50 mgOralAlembic Pharmaceuticals LimitedNot applicableNot applicableCanada flag
Alembic-lacosamideTablet150 mgOralAlembic Pharmaceuticals LimitedNot applicableNot applicableCanada flag
LacosamideTablet50 mgOralSanis Health Inc2021-09-27Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ach-lacosamideTablet150 mgOralAccord Healthcare Inc2021-04-27Not applicableCanada flag
Ach-lacosamideTablet100 mgOralAccord Healthcare Inc2021-04-27Not applicableCanada flag
Ach-lacosamideTablet200 mgOralAccord Healthcare Inc2021-04-27Not applicableCanada flag
Ach-lacosamideTablet50 mgOralAccord Healthcare Inc2021-04-27Not applicableCanada flag
Ag-lacosamideTablet200 mgOralAngita Pharma Inc.2022-04-29Not applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
ELEPSİ 50 MG+100 MG TEDAVİYE BAŞLAMA PAKETİ, 42 ADETLacosamide (50 mg) + Lacosamide (100 mg)Tablet, film coatedOralSANTA FARMA İLAÇ SAN. A.Ş.2018-11-28Not applicableTurkey flag
ELEPSİ 50 MG+100 MG TEDAVİYE BAŞLAMA PAKETİ, 42 ADETLacosamide (50 mg) + Lacosamide (100 mg)Tablet, film coatedOralSANTA FARMA İLAÇ SAN. A.Ş.2018-11-28Not applicableTurkey flag
Lacopat-Filmtabletten Packung zur BehandlungseinleitungLacosamide (50 mg) + Lacosamide (100 mg) + Lacosamide (150 mg) + Lacosamide (200 mg)Kit; Tablet, film coatedOralG.L. Pharma Gmb H2018-04-17Not applicableAustria flag
Lacopat-Filmtabletten Packung zur BehandlungseinleitungLacosamide (50 mg) + Lacosamide (100 mg) + Lacosamide (150 mg) + Lacosamide (200 mg)Kit; Tablet, film coatedOralG.L. Pharma Gmb H2018-04-17Not applicableAustria flag
Lacopat-Filmtabletten Packung zur BehandlungseinleitungLacosamide (50 mg) + Lacosamide (100 mg) + Lacosamide (150 mg) + Lacosamide (200 mg)Kit; Tablet, film coatedOralG.L. Pharma Gmb H2018-04-17Not applicableAustria flag

Categories

ATC Codes
N03AX18 — Lacosamide
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as n-acyl-alpha amino acids and derivatives. These are compounds containing an alpha amino acid (or a derivative thereof) which bears an acyl group at its terminal nitrogen atom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
N-acyl-alpha amino acids and derivatives
Alternative Parents
Alpha amino acid amides / Benzene and substituted derivatives / Acetamides / Secondary carboxylic acid amides / Dialkyl ethers / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Acetamide / Alpha-amino acid amide / Aromatic homomonocyclic compound / Benzenoid / Carbonyl group / Carboxamide group / Dialkyl ether / Ether / Hydrocarbon derivative / Monocyclic benzene moiety
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
563KS2PQY5
CAS number
175481-36-4
InChI Key
VPPJLAIAVCUEMN-GFCCVEGCSA-N
InChI
InChI=1S/C13H18N2O3/c1-10(16)15-12(9-18-2)13(17)14-8-11-6-4-3-5-7-11/h3-7,12H,8-9H2,1-2H3,(H,14,17)(H,15,16)/t12-/m1/s1
IUPAC Name
(2R)-N-benzyl-2-acetamido-3-methoxypropanamide
SMILES
COC[C@@H](NC(C)=O)C(=O)NCC1=CC=CC=C1

References

Synthesis Reference

http://www.google.com/patents?id=IIanAAAAEBAJ&pg=PA2&source=gbsselectedpages&cad=3#v=onepage&q&f=false

General References
  1. Sheets PL, Heers C, Stoehr T, Cummins TR: Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine. J Pharmacol Exp Ther. 2008 Jul;326(1):89-99. doi: 10.1124/jpet.107.133413. Epub 2008 Mar 31. [Article]
  2. Curia G, Biagini G, Perucca E, Avoli M: Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68. doi: 10.2165/00023210-200923070-00002. [Article]
  3. Perucca E, Yasothan U, Clincke G, Kirkpatrick P: Lacosamide. Nat Rev Drug Discov. 2008 Dec;7(12):973-4. doi: 10.1038/nrd2764. [Article]
  4. Rogawski MA, Tofighy A, White HS, Matagne A, Wolff C: Current understanding of the mechanism of action of the antiepileptic drug lacosamide. Epilepsy Res. 2015 Feb;110:189-205. doi: 10.1016/j.eplepsyres.2014.11.021. Epub 2014 Dec 3. [Article]
  5. European Directorate for the Quality of Medicines & HealthCare: Lacosamide MSDS [Link]
  6. FDA Approved Drug Products: VIMPAT (lacosamide) intravenous injection or oral solution or tablets (October 2023) [Link]
  7. FDA Approved Drug Products: MOTPOLY XR (lacosamide) extended-release capsules, for oral use, CV (May 2023) [Link]
  8. EMA Approved Drug Products: Vimpat (lacosamide) Oral Tablets [Link]
  9. Health Canada Approved Drug Products: VIMPAT (lacosamide) Oral Tablets or Intavenous Injection [Link]
KEGG Drug
D07299
PubChem Compound
219078
PubChem Substance
175427063
ChemSpider
189902
BindingDB
50300204
RxNav
623400
ChEBI
135939
ChEMBL
CHEMBL58323
ZINC
ZINC000000007673
PharmGKB
PA166160048
PDBe Ligand
LQO
Wikipedia
Lacosamide
PDB Entries
8s9b

Clinical Trials

Clinical Trials

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionIntravenous10 mg/ml
SyrupOral1 g
TabletOral50.000 mg
Tablet, coatedOral200 mg
Tablet, coatedOral5000000 mg
Tablet, coatedOral20000000 mg
SyrupOral
TabletOral100.000 mg
SolutionIntravenous10 mg
SolutionParenteral10 mg/ml
Tablet, film coatedOral
Injection, solutionIntravenous10 mg/1mL
SolutionOral10 mg/1mL
SolutionOral100 mg/10mL
SolutionOral150 mg/15mL
SolutionOral200 mg/20mL
SolutionOral50 mg/5mL
TabletOral100 mg/1
TabletOral150 mg/1
TabletOral200 mg/1
TabletOral50 mg/1
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral150 mg/1
Tablet, film coatedOral200 mg/1
Tablet, film coatedOral100 MG
Tablet, film coatedOral150 MG
Tablet, film coatedOral50 MG
SyrupOral10 mg/ml
Tablet, film coatedOral
Capsule, extended releaseOral100 mg/1
Capsule, extended releaseOral150 mg/1
Capsule, extended releaseOral200 mg/1
InjectionIntravenous10 mg/1mL
Kit; tablet, film coatedOral
SolutionIntravenous10 mg / mL
SolutionParenteral10.000 mg
SyrupOral1.000 g
SyrupOral15 MG/ML
TabletOral100 mg
TabletOral150 mg
TabletOral200 mg
TabletOral200.000 mg
TabletOral50 mg
Tablet, coatedOral
Tablet, film coatedOral50 mg/1
SolutionOral1000 mg
Tablet, coatedOral100 mg
Tablet, coatedOral50 mg
SyrupOral15 mg
SyrupOral10 mg/1ml
Tablet, film coatedOral200 mg
Tablet, coatedOral150 mg
SolutionIntravenous200 mg
Injection, solutionIntravenous10 mg/ml
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5654301No1997-08-052014-08-05US flag
USRE38551No2004-07-062022-03-17US flag
US11337943No2020-06-052040-06-05US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)140-146˚Chttp://www.ema.europa.eu/docs/en_GB/document_library/Application_withdrawal_assessment_report/2010/01/WC500064326.pdf
boiling point (°C)536.447 °C at 760 mmHgACD/Labs
water solubility10-33.3 g/Lhttps://sds.edqm.eu/pdf/SDS/EDQM_201700391_1.0_SDS_EN.pdf
logP0.728ACD/Labs
Predicted Properties
PropertyValueSource
Water Solubility0.465 mg/mLALOGPS
logP0.18ALOGPS
logP-0.022Chemaxon
logS-2.7ALOGPS
pKa (Strongest Acidic)12.46Chemaxon
pKa (Strongest Basic)-2Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count3Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area67.43 Å2Chemaxon
Rotatable Bond Count6Chemaxon
Refractivity67.57 m3·mol-1Chemaxon
Polarizability26.68 Å3Chemaxon
Number of Rings1Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9771
Blood Brain Barrier+0.7181
Caco-2 permeable-0.6886
P-glycoprotein substrateSubstrate0.7158
P-glycoprotein inhibitor INon-inhibitor0.6904
P-glycoprotein inhibitor IINon-inhibitor0.8878
Renal organic cation transporterNon-inhibitor0.8757
CYP450 2C9 substrateNon-substrate0.8732
CYP450 2D6 substrateNon-substrate0.7634
CYP450 3A4 substrateNon-substrate0.6572
CYP450 1A2 substrateNon-inhibitor0.8084
CYP450 2C9 inhibitorNon-inhibitor0.8704
CYP450 2D6 inhibitorNon-inhibitor0.8775
CYP450 2C19 inhibitorNon-inhibitor0.8201
CYP450 3A4 inhibitorNon-inhibitor0.837
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9732
Ames testNon AMES toxic0.7694
CarcinogenicityNon-carcinogens0.8388
BiodegradationNot ready biodegradable0.8499
Rat acute toxicity2.1629 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9678
hERG inhibition (predictor II)Non-inhibitor0.8489
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (18.4 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03dl-5920000000-9d5b2fbeb8e1c5f16b9a
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0znc-9400000000-d294c9319650e545b274
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-9700000000-dca3475de3ab528d0c9b
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0pbc-9600000000-576d9d53a856121b38e6
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0kc6-9300000000-665c83929139ac8d2366
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0f6x-8900000000-73acddbff6c5d745953a
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-164.945654
predicted
DarkChem Lite v0.1.0
[M-H]-159.19606
predicted
DeepCCS 1.0 (2019)
[M+H]+166.126654
predicted
DarkChem Lite v0.1.0
[M+H]+161.55406
predicted
DeepCCS 1.0 (2019)
[M+Na]+165.523054
predicted
DarkChem Lite v0.1.0
[M+Na]+167.6472
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Blocker
General Function
Voltage-gated sodium channel activity
Specific Function
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a...
Gene Name
SCN9A
Uniprot ID
Q15858
Uniprot Name
Sodium channel protein type 9 subunit alpha
Molecular Weight
226370.175 Da
References
  1. Sheets PL, Heers C, Stoehr T, Cummins TR: Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine. J Pharmacol Exp Ther. 2008 Jul;326(1):89-99. doi: 10.1124/jpet.107.133413. Epub 2008 Mar 31. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Blocker
General Function
Voltage-gated sodium channel activity
Specific Function
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a...
Gene Name
SCN3A
Uniprot ID
Q9NY46
Uniprot Name
Sodium channel protein type 3 subunit alpha
Molecular Weight
226291.905 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
  2. Sheets PL, Heers C, Stoehr T, Cummins TR: Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine. J Pharmacol Exp Ther. 2008 Jul;326(1):89-99. doi: 10.1124/jpet.107.133413. Epub 2008 Mar 31. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Blocker
General Function
Voltage-gated sodium channel activity
Specific Function
Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference acro...
Gene Name
SCN10A
Uniprot ID
Q9Y5Y9
Uniprot Name
Sodium channel protein type 10 subunit alpha
Molecular Weight
220623.605 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
  2. Sheets PL, Heers C, Stoehr T, Cummins TR: Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine. J Pharmacol Exp Ther. 2008 Jul;326(1):89-99. doi: 10.1124/jpet.107.133413. Epub 2008 Mar 31. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: VIMPAT (lacosamide) for oral or intravenous use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. FDA Approved Drug Products: VIMPAT (lacosamide) for oral or intravenous use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Contin M, Albani F, Riva R, Candela C, Mohamed S, Baruzzi A: Lacosamide therapeutic monitoring in patients with epilepsy: effect of concomitant antiepileptic drugs. Ther Drug Monit. 2013 Dec;35(6):849-52. doi: 10.1097/FTD.0b013e318290eacc. [Article]
  2. Bentue-Ferrer D, Tribut O, Verdier MC: [Therapeutic drug monitoring of lacosamide]. Therapie. 2012 Mar-Apr;67(2):151-5. doi: 10.2515/therapie/2012012. Epub 2012 Aug 2. [Article]
  3. Chung SS: New treatment option for partial-onset seizures: efficacy and safety of lacosamide. Ther Adv Neurol Disord. 2010 Mar;3(2):77-83. doi: 10.1177/1756285609355850. [Article]
  4. FDA Approved Drug Products: VIMPAT (lacosamide) for oral or intravenous use [Link]

Drug created at March 19, 2008 16:17 / Updated at May 29, 2024 19:09