Vixotrigine

Summary

Vixotrigine (CHEMBL3544913) is a phase-3 clinical-stage small molecule targeting SCN9A; indicated across 6 conditions including trigeminal neuralgia and neuralgia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (SCN9A)
• Indications: 6 conditions
• Clinical trials: 18
• Chemistry: 314.4 Da · C18H19FN2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3544913
Name	Vixotrigine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	16046068
Molecular formula	C18H19FN2O2
Molecular weight	314.4
InChIKey	JESCETIFNOFKEU-SJORKVTESA-N

SMILES: C1C[C@H](N[C@H]1C2=CC=C(C=C2)OCC3=CC=CC=C3F)C(=O)N

IUPAC name: (2S,5R)-5-[4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide

Also known as: BIIB-074, BIIB074, CNV-1014802, CNV1014802, GSK-1014802, GSK1014802, Raxatrigine, Vixotrigina, Vixotrigine, VIXOTRIGINE

Parent form; salt/anhydrous children: CHEMBL3544912

Patent coverage: 152 distinct patent families (374 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 368 (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
SCN9A	Nav1.7	Inhibition	5.21	0%	Q15858

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Sodium channel protein type 1 subunit alpha, Sodium channel protein type 5 subunit alpha, Sodium channel protein type 4 subunit alpha, Sodium channel protein type 7 subunit alpha, Sodium channel protein type 2 subunit alpha, Sodium channel protein type 9 subunit alpha, Sodium channel protein type 3 subunit alpha, Sodium channel protein type 8 subunit alpha, Sodium channel protein type 10 subunit alpha.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 11 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SCN5A	5.5	IC50	3200	nM	CHEMBL_ACT_24977328
SCN10A	5.22	IC50	6000	nM	CHEMBL_ACT_18916084
SCN9A	5.21	IC50	6100	nM	CHEMBL_ACT_24977330
SCN4A	5	IC50	10000	nM	CHEMBL_ACT_18916048

Target pathways

Aggregated over 1 target gene(s): SCN9A.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
Developmental Biology	1	SCN9A
L1CAM interactions	1	SCN9A
Muscle contraction	1	SCN9A
Axon guidance	1	SCN9A
Interaction between L1 and Ankyrins	1	SCN9A
Cardiac conduction	1	SCN9A
Phase 0 - rapid depolarisation	1	SCN9A
Nervous system development	1	SCN9A
Sensory Perception	1	SCN9A
Sensory perception of taste	1	SCN9A
Sensory perception of sweet, bitter, and umami (glutamate) taste	1	SCN9A

Dominant GO biological processes

GO term	Targets
inflammatory response	1
circadian rhythm	1
response to toxic substance	1
post-embryonic development	1
neuronal action potential	1
sensory perception of pain	1
sodium ion transmembrane transport	1
behavioral response to pain	1
detection of temperature stimulus involved in sensory perception of pain	1
detection of mechanical stimulus involved in sensory perception	1
cardiac muscle cell action potential involved in contraction	1
action potential propagation	1
action potential	1
regulation of heart rate	1
monoatomic ion transport	1

Indications & clinical

Indications

6 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
trigeminal neuralgia	3	MONDO:0008599	EFO:1001219
neuralgia	2	MONDO:0021667	EFO:0005762
radiculopathy	2	MONDO:0002959	MONDO:0002959
erythromelalgia	2	MONDO:0016028	MONDO:0016028
diabetic neuropathy	1	MONDO:0006626	EFO:1000783
bipolar disorder	1	MONDO:0004985	MONDO:0004985

Clinical trials

Total trials: 18.

Phase distribution

Phase	Trials
PHASE1	10
PHASE2	6
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03070132	PHASE3	WITHDRAWN	802NP301 Efficacy and Safety Study of BIIB074 in Participants With Trigeminal Neuralgia
NCT03637387	PHASE3	WITHDRAWN	802NP302 Efficacy and Safety Study of BIIB074 in Participants With Trigeminal Neuralgia
NCT01540630	PHASE2	COMPLETED	A Phase IIa Withdrawal Study of CNV1014802 in Patients With Trigeminal Neuralgia
NCT01561027	PHASE2	COMPLETED	Crossover Study of CNV1014802 in Subjects With Neuropathic Pain From Lumbosacral Radiculopathy
NCT02917187	PHASE2	COMPLETED	A Phase 2a Study of BIIB074 in the Treatment of Erythromelalgia
NCT02935608	PHASE2	COMPLETED	Study to Evaluate the Efficacy and Safety of BIIB074 in Neuropathic Pain From Lumbosacral Radiculopathy
NCT02957617	PHASE2	TERMINATED	Extension Study to Evaluate the Long-Term Safety, Tolerability, and Maintenance of Effect of BIIB074
NCT03339336	PHASE2	TERMINATED	Efficacy and Safety Study of BIIB074 in Participants With Small Fiber Neuropathy
NCT00908154	PHASE1	COMPLETED	Safety, Tolerability and Pharmacokinetics of Repeat Doses of GSK1014802.
NCT00955396	PHASE1	COMPLETED	Study to Investigate the Effect of GSK1014802 on Ambulatory Blood Pressure
NCT02359344	PHASE1	COMPLETED	PK & Tolerability of CNV1014802 in Young and Elderly Healthy Volunteers
NCT02551497	PHASE1	COMPLETED	Study to Evaluate the Interaction Between a Drug and CNV1014802 in Healthy Subjects
NCT02698267	PHASE1	COMPLETED	Effect of Itraconazole on the Pharmacokinetics of BIIB074
NCT02751905	PHASE1	COMPLETED	Absorption, Metabolism, and Excretion Study of BIIB074
NCT02831517	PHASE1	COMPLETED	PK and Safety Study of BIIB074 in Healthy Japanese and Caucasian Participants
NCT03324685	PHASE1	COMPLETED	A Drug Interaction Study of BIIB074 and an Oral Contraceptive Regimen
NCT03385525	PHASE1	COMPLETED	Study to Evaluate the Effect of UGT Inhibition by Valproic Acid on the Pharmacokinetics of BIIB074
NCT04106050	PHASE1	WITHDRAWN	Pharmacodynamic Study of BIIB095 and BIIB074 in Healthy Participants and Participants With Painful Diabetic Polyneuropathy

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

30 molecules share ≥1 primary target. Top 30 by shared-target count:

Molecule	Source	Status	Shared targets
SAFINAMIDE	ChEMBL + PubChem	Phase 4 (approved)	SCN9A
AMIODARONE	ChEMBL	Phase 4 (approved)	SCN9A
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	SCN9A
CANNABIDIOL	ChEMBL	Phase 4 (approved)	SCN9A
CARBAMAZEPINE	ChEMBL	Phase 4 (approved)	SCN9A
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	SCN9A
DILTIAZEM	ChEMBL	Phase 4 (approved)	SCN9A
HALOPERIDOL	ChEMBL	Phase 4 (approved)	SCN9A
IMIPRAMINE	ChEMBL	Phase 4 (approved)	SCN9A
LACOSAMIDE	ChEMBL	Phase 4 (approved)	SCN9A
LAMOTRIGINE	ChEMBL	Phase 4 (approved)	SCN9A
LIDOCAINE	ChEMBL	Phase 4 (approved)	SCN9A
MEXILETINE	ChEMBL	Phase 4 (approved)	SCN9A
MIBEFRADIL	ChEMBL	Phase 4 (approved)	SCN9A
NIFEDIPINE	ChEMBL	Phase 4 (approved)	SCN9A
PIMOZIDE	ChEMBL	Phase 4 (approved)	SCN9A
RILUZOLE	ChEMBL	Phase 4 (approved)	SCN9A
SERTINDOLE	ChEMBL	Phase 4 (approved)	SCN9A
TETRACAINE	ChEMBL	Phase 4 (approved)	SCN9A
AJMALINE	ChEMBL	Phase 3	SCN9A
ELECLAZINE	ChEMBL	Phase 3	SCN9A
NITRENDIPINE	ChEMBL	Phase 3	SCN9A
RALFINAMIDE	ChEMBL	Phase 3	SCN9A
TEDISAMIL	ChEMBL	Phase 3	SCN9A
TETRODOTOXIN	ChEMBL	Phase 3	SCN9A
CIFENLINE	ChEMBL	Phase 2	SCN9A
DS-1971	ChEMBL	Phase 2	SCN9A
FUNAPIDE	ChEMBL	Phase 2	SCN9A
PF-04531083	ChEMBL	Phase 2	SCN9A
PF-05089771	ChEMBL	Phase 2	SCN9A