DGIdb - LAMOTRIGINE Drug Record

LAMOTRIGINE chembl:CHEMBL741 Approved

Alternate Names:

LAMICTAL CD
LAMOTRIGINE
BW-430C
LAMICTAL ODT
LAMICTAL
LAMICTAL XR
LAMOTRIGINUM
QÍN
LAMICTAL®
LAMOTRIGINA
3,5-DIAMINO-6-(2,3-DICHLOROPHENYL)-1,2,4-TRIAZINE
GIZORD
QIN
drugbank:00555
pubchem.compound:3878
chembl:CHEMBL741
rxcui:28439
chemidplus:84057-84-1

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	anticonvulsant

(3 More Sources)

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Milosheska D et al., 2016, Pharmacokinetics of lamotrigine and its metabolite N-2-glucuronide: Influence of polymorphism of UDP-glucuronosyltransferases and drug transporters., Br J Clin Pharmacol
Inoue K et al., 2016, Factors that influence the pharmacokinetics of lamotrigine in Japanese patients with epilepsy., Eur J Clin Pharmacol
Zhou Y et al., 2015, Polymorphisms of ABCG2, ABCB1 and HNF4α are associated with Lamotrigine trough concentrations in epilepsy patients., Drug Metab Pharmacokinet
Singkham N et al., 2013, Influence of the UGT2B7 -161C>T polymorphism on the population pharmacokinetics of lamotrigine in Thai patients., Eur J Clin Pharmacol
Lipkind et al., 2005, Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels., Mol. Pharmacol.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Ma CL et al., 2014, Association of SCN1A, SCN2A and ABCC2 gene polymorphisms with the response to antiepileptic drugs in Chinese Han patients with epilepsy., Pharmacogenomics
Kwan P et al., 2008, Multidrug resistance in epilepsy and polymorphisms in the voltage-gated sodium channel genes SCN1A, SCN2A, and SCN3A: correlation among phenotype, genotype, and mRNA expression., Pharmacogenet Genomics
Shen CH et al., 2016, Specific OCT1 and ABCG2 polymorphisms are associated with Lamotrigine concentrations in Chinese patients with epilepsy., Epilepsy Res
Aberg et al., 1997, Lamotrigine therapy in infantile neuronal ceroid lipofuscinosis (INCL)., Neuropediatrics
Kazeem GR et al., 2009, High-resolution HLA genotyping and severe cutaneous adverse reactions in lamotrigine-treated patients., Pharmacogenet Genomics
Klarica Domjanović I et al., 2018, Interaction between ABCG2 421C>A polymorphism and valproate in their effects on steady-state disposition of lamotrigine in adults with epilepsy., Br J Clin Pharmacol
Chang Y et al., 2014, Correlation of the UGT1A4 gene polymorphism with serum concentration and therapeutic efficacy of lamotrigine in Han Chinese of Northern China., Eur J Clin Pharmacol
Zhou J et al., 2011, Functional analysis of UGT1A4(P24T) and UGT1A4(L48V) variant enzymes., Pharmacogenomics
Bertok S et al., 2017, The association of SCN1A p.Thr1067Ala polymorphism with epilepsy risk and the response to antiepileptic drugs in Slovenian children and adolescents with epilepsy., Seizure
Haerian BS et al., 2013, SCN1A, SCN2A and SCN3A gene polymorphisms and responsiveness to antiepileptic drugs: a multicenter cohort study and meta-analysis., Pharmacogenomics
Kumari R et al., 2011, Pharmacogenomic association study on the role of drug metabolizing, drug transporters and drug target gene polymorphisms in drug-resistant epilepsy in a north Indian population., Indian J Hum Genet
Yang B et al., 2008, Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides., Bioorg Med Chem

LAMOTRIGINE PPT1

Interaction Score: 2.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9151331

Sources:
NCI
LAMOTRIGINE UGT1A4

Interaction Score: 1.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29791014 26790665 24820767 23263737 22047493

Sources:
PharmGKB
LAMOTRIGINE AQP4

Interaction Score: 0.59

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18572411

Sources:
DTC
LAMOTRIGINE UGT2B7

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27096250 26790665 26213157 23263737

Sources:
PharmGKB
LAMOTRIGINE HNF4A

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27610747 26213157

Sources:
PharmGKB
LAMOTRIGINE HLA-C

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19668019

Sources:
PharmGKB
LAMOTRIGINE HLA-DQB1

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19668019

Sources:
PharmGKB
LAMOTRIGINE SLC22A1

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27610747

Sources:
PharmGKB
LAMOTRIGINE SCN2A

Interaction Score: 0.32

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name Lamictal

Novel drug target Established target

Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs:
16174788 17016423 17139284 25155934 18784617

Sources:
TdgClinicalTrial ChemblInteractions PharmGKB
LAMOTRIGINE SCN1A

Interaction Score: 0.28

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
28753467 25155934 23859570 21747585 16174788

Sources:
ChemblInteractions PharmGKB
LAMOTRIGINE ABCG2

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29791014 27610747 26213157

Sources:
PharmGKB
LAMOTRIGINE HLA-DRB1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19668019

Sources:
PharmGKB
LAMOTRIGINE SCN11A

Interaction Score: 0.08

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
LAMOTRIGINE SCN7A

Interaction Score: 0.04

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LAMOTRIGINE SCN8A

Interaction Score: 0.04

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LAMOTRIGINE SCN3A

Interaction Score: 0.04

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs:
None found

Sources:
ChemblInteractions
LAMOTRIGINE SCN4A

Interaction Score: 0.04

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LAMOTRIGINE SCN9A

Interaction Score: 0.04

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LAMOTRIGINE SCN10A

Interaction Score: 0.03

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs:
None found

Sources:
ChemblInteractions
LAMOTRIGINE SCN5A

Interaction Score: 0.03

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LAMOTRIGINE CYP2C9

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
LAMOTRIGINE CYP2C19

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
LAMOTRIGINE ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
LAMOTRIGINE CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
LAMOTRIGINE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
LAMOTRIGINE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC

TdgClinicalTrial: LAMOTRIGINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications anticonvulsant

Drug Class Small Molecule

FDA Approval approved

Publications:
NCI: LAMOTRIGINE
- Version: 14-September-2017
Alternate Names:

C38703 NCI drug code

Drug Info:

Publications:

Aberg et al., 1997, Lamotrigine therapy in infantile neuronal ceroid lipofuscinosis (INCL)., Neuropediatrics

DTC: LAMOTRIGINE

Version: 02-September-2020

Alternate Names:

CHEMBL741 ChEMBL Drug ID

Drug Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Yang B et al., 2008, Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides., Bioorg Med Chem

PharmGKB: lamotrigine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Shen CH et al., 2016, Specific OCT1 and ABCG2 polymorphisms are associated with Lamotrigine concentrations in Chinese patients with epilepsy., Epilepsy Res

Haerian BS et al., 2013, SCN1A, SCN2A and SCN3A gene polymorphisms and responsiveness to antiepileptic drugs: a multicenter cohort study and meta-analysis., Pharmacogenomics

Kumari R et al., 2011, Pharmacogenomic association study on the role of drug metabolizing, drug transporters and drug target gene polymorphisms in drug-resistant epilepsy in a north Indian population., Indian J Hum Genet

TTD: Lamotrigine
- Version: 2020.06.01
Alternate Names:

D03FLC TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL741
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL741
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Trial Name	Lamictal
Novel drug target	Established target
Mechanism of Interaction	Sodium channel alpha subunit blocker

Mechanism of Interaction	Sodium channel alpha subunit blocker
Direct Interaction	yes

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

LAMOTRIGINE Drug Record

LAMOTRIGINE chembl:CHEMBL741 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9151331

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29791014 26790665 24820767 23263737 22047493

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18572411

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27096250 26790665 26213157 23263737

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27610747 26213157

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19668019

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19668019

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27610747

Sources: PharmGKB

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name Lamictal Novel drug target Established target Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs: 16174788 17016423 17139284 25155934 18784617

Sources: TdgClinicalTrial ChemblInteractions PharmGKB

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

PMIDs: 28753467 25155934 23859570 21747585 16174788

Sources: ChemblInteractions PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29791014 27610747 26213157

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19668019

Sources: PharmGKB

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs: None found

Interaction Types & Directionality:

n/a

PMIDs:
9151331

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
29791014 26790665 24820767 23263737 22047493

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18572411

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
27096250 26790665 26213157 23263737

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27610747 26213157

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
19668019

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
19668019

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27610747

Sources:
PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name Lamictal

Novel drug target Established target

Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs:
16174788 17016423 17139284 25155934 18784617

Sources:
TdgClinicalTrial ChemblInteractions PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
28753467 25155934 23859570 21747585 16174788

Sources:
ChemblInteractions PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
29791014 27610747 26213157

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
19668019

Sources:
PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a