Carbamazepine

Summary

Carbamazepine (CHEMBL108) is an approved small-molecule anticonvulsant (ATC N03AF01) targeting FZD8; indicated across 19 conditions including epilepsy and focal epilepsy.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N03AF01
• Targets: 1 (FZD8)
• Indications: 19 conditions
• Clinical trials: 101
• Chemistry: 236.27 Da · C15H12N2O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL108
Name	Carbamazepine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	2554
ChEBI	CHEBI:3387
ATC	N03AF01
Molecular formula	C15H12N2O
Molecular weight	236.27
InChIKey	FFGPTBGBLSHEPO-UHFFFAOYSA-N

SMILES: C1=CC=C2C(=C1)C=CC3=CC=CC=C3N2C(=O)N

IUPAC name: benzo[b][1]benzazepine-11-carboxamide

ChEBI definition: A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.

Pharmacological roles (ChEBI): anticonvulsant, EC 3.5.1.98 (histone deacetylase) inhibitor, mitogen, glutamate transporter activator, antimanic drug, analgesic, non-narcotic analgesic, drug allergen, sodium channel blocker.

Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.

Also known as: Arbil mr, Biston, Carbagen sr, Carbamazepina, Carbamazepine, Carbamazepine anhydrous, Carbamazepine extended release, Carbamazepinum, Carbatrol, Carnexiv, Epimaz, Epimaz ret

Patent coverage: 16,531 distinct patent families (53,528 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 52,591 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
FZD8	FZD8	Negative	4.77	0%	Q9H461

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Prelamin-A/C, Thyrotropin receptor, Sodium channel protein type 5 subunit alpha, Sodium channel protein type 4 subunit alpha, Mitogen-activated protein kinase 1, Sodium channel protein type 9 subunit alpha, Frizzled-8.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	8.4	Potency	4	nM	CHEMBL_ACT_3665498
MAPK1	7	Potency	100	nM	CHEMBL_ACT_4521462
TSHR	5.2	Potency	6310	nM	CHEMBL_ACT_3911228
TSHR	5.2	Potency	6310	nM	CHEMBL_ACT_4617637

Target pathways

Aggregated over 1 target gene(s): FZD8.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
Class B/2 (Secretin family receptors)	1	FZD8
Asymmetric localization of PCP proteins	1	FZD8
Regulation of FZD by ubiquitination	1	FZD8
Signaling by RNF43 mutants	1	FZD8

Dominant GO biological processes

GO term	Targets
angiogenesis	1
neuron differentiation	1
T cell differentiation in thymus	1
non-canonical Wnt signaling pathway	1
canonical Wnt signaling pathway	1
signal transduction	1
cell surface receptor signaling pathway	1
G protein-coupled receptor signaling pathway	1
Wnt signaling pathway	1

Indications & clinical

Indications

19 indications (7 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
epilepsy	4	MONDO:0005027	EFO:0000474
focal epilepsy	4	MONDO:0005384	EFO:0004263
trigeminal neuralgia	4	MONDO:0008599	EFO:1001219
visual epilepsy	4	MONDO:0001386	HP:0001250
bipolar disorder	4	MONDO:0004985	EFO:0009963
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050
HIV infectious disease	2	MONDO:0005109	EFO:0000764
cocaine dependence	2	MONDO:0005186	EFO:0002610
reflex epilepsy	2	MONDO:0017768	MONDO:0015643
drug dependence	2	MONDO:0005303	EFO:0003890
hepatitis B virus infection	1	MONDO:0005344	EFO:0004197
Parkinson disease	1	MONDO:0005180	MONDO:0005180
severe acute respiratory syndrome	1	MONDO:0005091	MONDO:0100096

4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 101.

Phase distribution

Phase	Trials
PHASE1	50
PHASE4	21
Not specified	13
PHASE3	9
PHASE2	7
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06849219	PHASE4	ACTIVE_NOT_RECRUITING	Comparison of Oxcarbazepine Versus Carbamazepine in the Management of Trigeminal Neuralgia
NCT00000218	PHASE4	COMPLETED	Pharmacotherapy and Intensive Treatment - 2
NCT00000441	PHASE4	COMPLETED	Drug Therapy for Alcohol Detoxification
NCT00153296	PHASE4	COMPLETED	Study of Efficacy of Carbamazepine in Therapy of Patients With Moderate Persistent and Severe Bronchial Asthma
NCT00190892	PHASE4	COMPLETED	Olanzapine Plus Carbamazepine in the Treatment of Bipolar I Mania
NCT00207428	PHASE4	COMPLETED	Antiepileptic Drug Carbamazepine in Treatment of Bronchial Asthma
NCT00260247	PHASE4	COMPLETED	Induction of Drug Metabolism: In Vivo Comparison of Carbamazepine and Oxcarbazepine.
NCT00350857	PHASE4	COMPLETED	The Young Adult and Pediatric Bipolar Study
NCT00438451	PHASE4	COMPLETED	Study on the Treatment of Elderly Patients With Older and Newer Antiepileptic Drugs
NCT00807989	PHASE4	COMPLETED	The Efficacy and Safety of Low Dose Combination of LTG and VPA Compared to CBZ Monotherapy
NCT00896987	PHASE4	COMPLETED	Lamotrigine Cognitive Function Study in Adult Untreated Epilepsies
NCT01089855	PHASE4	COMPLETED	Efficacy and Tolerability of Carbamazepine CR in Diabetic Neuropathy Pain
NCT01127256	PHASE4	COMPLETED	Comparative Study of Zonisamide and Carbamazepine as an Initial Monotherapy: Efficacy and Safety Evaluation
NCT02214615	PHASE4	COMPLETED	Carbamazapine for Inherited Erythromelalgia Patients With NaV1.7 Mutations
NCT02623504	PHASE4	TERMINATED	DB/Maintenance of Equetro (Carbamazepine) in Children With Acute Manic or Mixed Bipolar 1 Disorder
NCT02705768	PHASE4	COMPLETED	Effect of Carbamazepine and Oxcarbazepine on Serum Neuron-specific Enolase and S100B in Focal Seizures
NCT02870283	PHASE4	COMPLETED	Cost- Effectiveness and Quality of Life Assessment in Mood Disorder
NCT02912364	PHASE4	COMPLETED	Comparison of the Cognitive and Behavioral Effects of Eslicarbazepine Acetate and Carbamazepine in Healthy Adults
NCT04610879	PHASE4	TERMINATED	Changing Agendas on Sleep, Treatment and Learning in Epilepsy
NCT04996199	PHASE4	UNKNOWN	Comparision Efficacy of Carbamazepine & Oxcarbazepine in the Treatment of Trigeminal Neuralgia- a Randomised Clinical Trial
NCT05697614	PHASE4	UNKNOWN	The Benefit and Safety of Older Generation Anti-Epileptic Drugs (AEDs) in Drug-Resistant Epilepsy Children
NCT00007670	PHASE3	COMPLETED	Does Gabapentin and Lamotriginel Have Significantly Fewer Side-effects While Providing Equal or Better Seizure Control Than the Current Drug Choice, Carbamazepine, for the Treatment of Seizures in the Elderly.
NCT00150553	PHASE3	COMPLETED	Efficacy and Safety of SPD417 in Treatment of Manic Symptoms in Adults With Bipolar I Disorder
NCT00150605	PHASE3	COMPLETED	Safety of SPD417 Combined With Other Psychotropic Medications in the Treatment of Bipolar I Disorder
NCT00266630	PHASE3	COMPLETED	Efficacy and Safety of Olanzapine in the Extended Treatment for Manic or Mixed Episode of Bipolar I Disorder
NCT00477295	PHASE3	COMPLETED	A Double-blind Study to Compare the Efficacy and Safety of Zonisamide and Carbamazepine as Monotherapy, in Newly Diagnosed Partial Epilepsy
NCT00542802	PHASE3	UNKNOWN	Levetiracetam Versus Carbamazepine in Post-Stroke Late Onset Crisis
NCT00848549	PHASE3	COMPLETED	Assessing The Long-Term Safety And To Explore The Long-Term Efficacy Of Zonisamide As Monotherapy In Newly Diagnosed Partial Seizures
NCT01954121	PHASE3	COMPLETED	Open-label, Randomized, Active-controlled Study of LEV Used as Monotherapy in Patients With Partial-Onset Seizures
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT00000191	PHASE2	COMPLETED	Carbamazepine Treatment for Cocaine Dependence - 5
NCT00000217	PHASE2	COMPLETED	Pharmacotherapy and Intensive Treatment of Drug Abuse - 1
NCT00000242	PHASE2	COMPLETED	Carbamazepine Treatment of Cocaine Dependence - 1
NCT00004758	PHASE2	COMPLETED	Phase II Randomized Study of Early Surgery Vs Multiple Sequential Antiepileptic Drug Therapy for Infantile Spasms Refractory to Standard Treatment
NCT00294892	PHASE2	COMPLETED	Pharmacokinetics Study on Nevirapine Resistance in Tanzania
NCT00894010	PHASE2	COMPLETED	Photosensitivity Proof of Concept Trial
NCT01581918	PHASE2	UNKNOWN	Efficacy and Safety Evaluation of Carbamazepine for Prevention of Chemotherapy-induced Nausea and Vomiting
NCT06672900	PHASE1	ACTIVE_NOT_RECRUITING	A Multi-part Study of ALG-000184 to Evaluate Safety, Tolerability, Pharmacokinetics and Drug-drug Interaction Potential After Single and Multiple Doses in Healthy Volunteers
NCT06909162	PHASE1	RECRUITING	A Study to Evaluate the Effect of Food on the Single-Dose Pharmacokinetics and a Drug-Drug Interaction Evaluation of Itraconazole and Carbamazepine on INCB123667 When Administered Orally to Healthy Adult Participants
NCT07395024	PHASE1	RECRUITING	A Study to Learn How Fluconazole, Carbamazepine and Itraconazole Affect How the Body Processes ASP3082 in Healthy Adults

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (5) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for carbamazepine and HLA-A, HLA-B	CPIC	HLA-A;HLA-B		yes
Annotation of CPNDS Guideline for carbamazepine and HLA-A, HLA-B	CPNDS	HLA-A;HLA-B		yes
Annotation of DPWG Guideline for carbamazepine and HLA-A	DPWG	HLA-A		yes
Annotation of DPWG Guideline for carbamazepine and HLA-B	DPWG	HLA-B		yes
Annotation of RNPGx Guideline for carbamazepine, oxcarbazepine and HLA	RNPGx	HLA-A;HLA-B		yes

PharmGKB also curates 52 clinical and 405 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).