Lacosamide

Summary

Lacosamide (CHEMBL58323) is an approved small molecule (ATC N03AX18) targeting SCN2A, SCN3A, and SCN9A; indicated across 21 conditions including epilepsy and focal epilepsy.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N03AX18
• Targets: 4 (SCN2A, SCN3A, SCN9A…)
• Indications: 21 conditions
• Clinical trials: 99
• Chemistry: 250.29 Da · C13H18N2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL58323
Name	Lacosamide
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	219078
ATC	N03AX18
Molecular formula	C13H18N2O3
Molecular weight	250.29
InChIKey	VPPJLAIAVCUEMN-GFCCVEGCSA-N

SMILES: CC(=O)N[C@H](COC)C(=O)NCC1=CC=CC=C1

IUPAC name: (2R)-2-acetamido-N-benzyl-3-methoxypropanamide

Also known as: (r)-lacosamide 1, ADD 243037, ADD-243037, ADD243037, Erlosamide, Lacosamida, Lacosamide, Lacosamide accord, Lacosamide adroiq, Lacosamide cv, Lacosamide ucb, Motpoly

Parent form; salt/anhydrous children: CHEMBL1213900

Patent coverage: 1,549 distinct patent families (5,692 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
SCN2A	Nav1.2	Antagonist	4.52	0.1%	Q99250
SCN3A	Nav1.3	Antagonist	3.4	0.1%	Q9NY46
SCN9A	Nav1.7	Antagonist	3.7	0%	Q15858
SCN10A	Nav1.8	Antagonist	4.8	0.1%	Q9Y5Y9

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Voltage-dependent L-type calcium channel subunit alpha-1C, Carbonic anhydrase 2, Carbonic anhydrase 7, Carbonic anhydrase 1, Carbonic anhydrase 3, Carbonic anhydrase 6, Carbonic anhydrase 12, Carbonic anhydrase 14, Carbonic anhydrase 9, Carbonic anhydrase 4.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 18 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SCN9A	6.74	IC50	182	nM	CHEMBL_ACT_12662679
CA2	6.48	Ki	331	nM	CHEMBL_ACT_2949514
CA5B	6.47	Ki	341	nM	CHEMBL_ACT_2949518
CA9	6.45	Ki	353	nM	CHEMBL_ACT_2949521
CA1	6.44	Ki	362	nM	CHEMBL_ACT_2949513
CA3	6.43	Ki	374	nM	CHEMBL_ACT_2949515
P08104	6.38	IC50	415	nM	CHEMBL_ACT_12662680
P08104	6.38	IC50	415	nM	CHEMBL_ACT_18718771
CA6	6.38	Ki	412	nM	CHEMBL_ACT_2949519
Q99N23	6.34	Ki	461	nM	CHEMBL_ACT_2949525
CA14	6.33	Ki	473	nM	CHEMBL_ACT_2949524
CA4	6.28	Ki	525	nM	CHEMBL_ACT_2949516
CA13	5.92	Ki	1210	nM	CHEMBL_ACT_2949523
CA12	5.43	Ki	3713	nM	CHEMBL_ACT_2949522
CA7	5.35	Ki	4446	nM	CHEMBL_ACT_2949520
CA5A	5.34	Ki	4565	nM	CHEMBL_ACT_2949517

Target pathways

Aggregated over 4 target gene(s): SCN2A, SCN3A, SCN9A, SCN10A.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
Developmental Biology	4	SCN10A, SCN2A, SCN3A, SCN9A
L1CAM interactions	4	SCN10A, SCN2A, SCN3A, SCN9A
Muscle contraction	4	SCN10A, SCN2A, SCN3A, SCN9A
Axon guidance	4	SCN10A, SCN2A, SCN3A, SCN9A
Interaction between L1 and Ankyrins	4	SCN10A, SCN2A, SCN3A, SCN9A
Cardiac conduction	4	SCN10A, SCN2A, SCN3A, SCN9A
Phase 0 - rapid depolarisation	4	SCN10A, SCN2A, SCN3A, SCN9A
Nervous system development	4	SCN10A, SCN2A, SCN3A, SCN9A
Sensory Perception	3	SCN2A, SCN3A, SCN9A
Sensory perception of taste	3	SCN2A, SCN3A, SCN9A
Sensory perception of sweet, bitter, and umami (glutamate) taste	3	SCN2A, SCN3A, SCN9A

Dominant GO biological processes

GO term	Targets
sodium ion transport	4
sodium ion transmembrane transport	4
cardiac muscle cell action potential involved in contraction	4
regulation of heart rate	4
monoatomic ion transport	4
monoatomic ion transmembrane transport	4
transmembrane transport	4
monoatomic cation transmembrane transport	4
action potential	3
cardiac muscle cell action potential	3
regulation of muscle system process	3
neuronal action potential	2
regulation of membrane potential	2
behavioral response to pain	2
membrane depolarization during action potential	2

Indications & clinical

Indications

21 indications (3 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
visual epilepsy	4	MONDO:0001386	HP:0001250
diabetic neuropathy	3	MONDO:0006626	EFO:1000783
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050
migraine disorder	3	MONDO:0005277	MONDO:0005277
erythromelalgia	3	MONDO:0016028	MONDO:0007571
sciatica	3	MONDO:0024333	HP:0011868
neuralgia	2	MONDO:0021667	EFO:0005762
fibromyalgia	2	MONDO:0005546	EFO:0005687
brain neoplasm	2	MONDO:0021211	EFO:0003833
osteoarthritis	2	MONDO:0005178	MONDO:0005178
alcohol abuse	2	MONDO:0002046	MONDO:0007079
paraganglioma	2	MONDO:0000448	EFO:1000453
kidney disorder	1	MONDO:0005240	EFO:0003086
amyotrophic lateral sclerosis	1	MONDO:0004976	MONDO:0004976

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

Clinical trials

Total trials: 99.

Phase distribution

Phase	Trials
PHASE3	35
PHASE2	20
Not specified	18
PHASE4	11
PHASE1	10
PHASE2/PHASE3	4
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06866691	PHASE4	RECRUITING	Seizure Prevention in Traumatic Brain Injury With Levetiracetam and Lacosamide
NCT00832884	PHASE4	COMPLETED	The Safety of Intravenous Lacosamide
NCT00955357	PHASE4	COMPLETED	Trial to Assess Lacosamide as the First add-on Anti-epileptic Drug Treatment in Patients With Partial-onset Seizures
NCT01175954	PHASE4	COMPLETED	Cognitive and Behavioral Effects of Lacosamide
NCT01190098	PHASE4	COMPLETED	Randomized Controlled Trial to Assess Effects of Lacosamide on Sleep and Wake in Adults With Focal Epilepsy
NCT01235403	PHASE4	COMPLETED	Trial to Assess Optimized Dosage of Lacosamide as add-on Therapy in Patients With Partial Onset Seizure
NCT02409433	PHASE4	TERMINATED	Comparative Trial of IV Lacosamide Versus Phenytoin for Seizure Management
NCT04144218	PHASE4	UNKNOWN	Evaluation of the Efficacy and Safety of Lacosamide in Pediatric Patients With Epilepsy
NCT05510856	PHASE4	COMPLETED	Comparative Clinical Study Evaluating the Possible Efficacy of Duloxetine, Gabapentin and Lacosamide on Oxaliplatin-Induced Peripheral Neuropathy in Cancer Patients
NCT05598905	PHASE4	COMPLETED	Combined Effect of Pregabalin and Oxycodone, and Lacosamide and Oxycodone, on Breathing
NCT05969054	PHASE4	UNKNOWN	Improvement Effect of Lacosamide and Levetiracetam on Cognitive in Alzheimer’s Disease Patients With Epilepsy
NCT07412132	PHASE3	RECRUITING	Evaluation of the Efficacy, Safety, and Tolerability of Lacosamide in Major Depressive Episodes of Bipolar Disorder Types I and II.
NCT00135109	PHASE3	COMPLETED	Trial to Assess the Efficacy and Safety of SPM 927 (200, 400, and 600mg/Day) in Subjects With Painful Distal Diabetic Neuropathy
NCT00136019	PHASE3	COMPLETED	SPM 927 (400mg/Day and 600mg/Day) as Adjunctive Therapy in Subjects With Partial Seizures With or Without Secondary Generalization
NCT00151879	PHASE2/PHASE3	COMPLETED	Safety and Tolerability of Intravenous SPM 927 as Replacement for Oral SPM 927 in Subjects With Partial Seizures
NCT00220337	PHASE3	COMPLETED	A Trial to Assess the Long-term Safety and Efficacy of Lacosamide in Subjects With Painful Diabetic Neuropathy
NCT00220415	PHASE3	COMPLETED	A Multicenter, Double-blind, Randomized, Placebo-controlled, Parallel Group Trial to Investigate the Efficacy and Safety of SPM 927 (200mg/Day and 400mg/Day) as Adjunctive Therapy in Subjects With Partial Seizures With or Without Secondary Generalization
NCT00235443	PHASE2/PHASE3	COMPLETED	A Follow-On Trial to Assess the Long Term Safety and Efficacy of SPM 927 in Painful Distal Diabetic Neuropathy
NCT00235469	PHASE2/PHASE3	COMPLETED	A Trial to Assess the Efficacy and Safety of SPM 927 in Subjects With Painful Distal Diabetic Neuropathy
NCT00238524	PHASE3	COMPLETED	A Trial to Assess the Efficacy and Safety of SPM 927 (Lacosamide) in Subjects With Painful Distal Diabetic Neuropathy
NCT00515619	PHASE3	COMPLETED	Assess Safety and Efficacy of Lacosamide in Patients With Partial Seizures
NCT00520741	PHASE3	COMPLETED	Trial to Demonstrate the Efficacy and Safety of Conversion to Lacosamide Monotherapy for Partial-onset Seizures
NCT00522275	PHASE3	COMPLETED	Determine Safety and Efficacy of Long-term Oral Lacosamide in Patients With Partial Seizures
NCT00530855	PHASE3	COMPLETED	Trial to Assess Long-term Lacosamide (LCM) Monotherapy Use and Safety of LCM Monotherapy and Adjunctive Therapy for Partial-onset Seizures
NCT00546351	PHASE3	COMPLETED	Study Evaluating Long-term Safety and Efficacy of Lacosamide in Subjects With Painful Distal Diabetic Neuropathy.
NCT00655486	PHASE3	COMPLETED	Study to Assess the Long-term Safety of Oral Lacosamide in Subjects With Partial-onset Seizures
NCT00655551	PHASE3	COMPLETED	Safety of Intravenous Lacosamide Dose Followed by Twice Daily Oral Lacosamide in Subjects With Partial-onset Seizures
NCT01243177	PHASE3	COMPLETED	Trial Comparing the Efficacy and Safety of Lacosamide (LCM) to Carbamazepine Controlled-Release (CBZ-CR); Initial Monotherapy in Epilepsy; Subjects Aged 16 and Older
NCT01345058	PHASE3	COMPLETED	Add on Lacosamide Versus High Dose Monotherapy
NCT01375374	PHASE3	TERMINATED	Hormonal and Lipid Levels in Male Subjects After a Switch From Carbamazepine to Lacosamide
NCT01465997	PHASE3	COMPLETED	Evaluating Long Term Safety of Lacosamide (LCM) to Carbamazepine Controlled-release (CBZ-CR); Initial Monotherapy in Epilepsy Subjects 16 Years and Older
NCT01484977	PHASE3	COMPLETED	eValuation of the Efficacy and toleRability of Vimpat When Added to lEvetiracetam
NCT01710657	PHASE3	COMPLETED	A Trial to Evaluate the Efficacy and Safety of Adjunctive Therapy With Lacosamide in Adults With Partial-Onset Seizures
NCT01832038	PHASE3	COMPLETED	Study to Evaluate the Safety, Tolerability, and Efficacy of Long-term Adjunctive Therapy With Lacosamide in Adults With Partial-onset Seizures
NCT01911975	PHASE3	COMPLETED	Safety and Tolerability of Lacosamide in Patients With Gain-of-function Nav1.7 Mutations Related Small Fiber Neuropathy
NCT01921205	PHASE3	COMPLETED	Study to Investigate Lacosamide as Add-on Therapy in Subjects ≥4 Years to <17 Years of Age With Partial Onset Seizures
NCT01964560	PHASE3	COMPLETED	A Clinical Study to Investigate the Efficacy and Safety of Lacosamide as an Add on Therapy in Children With Epilepsy With Partial-onset Seizures
NCT02124564	PHASE3	COMPLETED	A Trial to Evaluate the Long Term Safety and Tolerability of Lacosamide Taken as Monotherapy in Adults With Partial-onset Seizures
NCT02192814	PHASE3	COMPLETED	Open-label Study to Evaluate the Safety and Tolerability of iv Lacosamide in Japanese Adults With Partial-onset Seizures
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 11 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

139 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
AMIODARONE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
AMITRIPTYLINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
CHLORPROMAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
DILTIAZEM	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
LAMOTRIGINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
MEXILETINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
NIFEDIPINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
MIBEFRADIL	ChEMBL	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
SERTINDOLE	ChEMBL	Phase 4 (approved)	SCN10A, SCN2A, SCN3A, SCN9A
AJMALINE	ChEMBL	Phase 3	SCN10A, SCN2A, SCN3A, SCN9A
ELECLAZINE	ChEMBL	Phase 3	SCN10A, SCN2A, SCN3A, SCN9A
NITRENDIPINE	ChEMBL	Phase 3	SCN10A, SCN2A, SCN3A, SCN9A
TEDISAMIL	ChEMBL	Phase 3	SCN10A, SCN2A, SCN3A, SCN9A
VIXOTRIGINE	ChEMBL	Phase 3	SCN10A, SCN2A, SCN3A, SCN9A
CIFENLINE	ChEMBL	Phase 2	SCN10A, SCN2A, SCN3A, SCN9A
Carbamazepine	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A, SCN9A
Lidocaine	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A, SCN9A
TETRACAINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A, SCN9A
TETRODOTOXIN	ChEMBL	Phase 3	SCN2A, SCN3A, SCN9A
FUNAPIDE	ChEMBL	Phase 2	SCN10A, SCN2A, SCN9A
PF-05089771	ChEMBL	Phase 2	SCN2A, SCN3A, SCN9A
Dofetilide	PubChem	Approved	SCN10A, SCN2A, SCN3A
BROMPHENIRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
CHLORPHENIRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
COCAINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
CYPROHEPTADINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
DESIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
DIBUCAINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
DICYCLOMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
DIPHENHYDRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
DROPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
FELODIPINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
FLUPHENAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
LEVORPHANOL	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
LOPERAMIDE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
NISOLDIPINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PHENOXYBENZAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PHENTOLAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PHENYTOIN	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PRAMOXINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PRAZOSIN	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PRILOCAINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PROMETHAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
PROPARACAINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
QUINIDINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
QUININE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
RESERPINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
TETRABENAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
THIORIDAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
TRIFLUOPERAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
VERAPAMIL	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN3A
ARTICAINE	ChEMBL	Phase 4 (approved)	SCN2A, SCN3A
BENOXINATE	ChEMBL	Phase 4 (approved)	SCN2A, SCN3A
BEPRIDIL	ChEMBL	Phase 4 (approved)	SCN2A, SCN3A
BUPIVACAINE	ChEMBL	Phase 4 (approved)	SCN2A, SCN3A
CINNARIZINE	ChEMBL	Phase 4 (approved)	SCN2A, SCN3A
DIPHENIDOL	ChEMBL	Phase 4 (approved)	SCN2A, SCN3A