Suzetrigine

Summary

Suzetrigine (CHEMBL5314487) is a phase-3 clinical-stage small-molecule non-narcotic analgesic targeting SCN10A; indicated across 3 conditions including diabetic neuropathy and neuralgia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (SCN10A)
• Indications: 3 conditions
• Clinical trials: 41
• Chemistry: 473.4 Da · C21H20F5N3O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5314487
Name	Suzetrigine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	156445116
ChEBI	CHEBI:233446
Molecular formula	C21H20F5N3O4
Molecular weight	473.4
InChIKey	XSQUJFKRXZMOKA-PAFIKIDNSA-N

SMILES: C[C@H]1[C@H]([C@@H](O[C@@]1(C)C(F)(F)F)C(=O)NC2=CC(=NC=C2)C(=O)N)C3=C(C(=C(C=C3)F)F)OC

IUPAC name: 4-[[(2R,3S,4S,5R)-3-(3,4-difluoro-2-methoxyphenyl)-4,5-dimethyl-5-(trifluoromethyl)oxolane-2-carbonyl]amino]pyridine-2-carboxamide

ChEBI definition: A member of the class of oxolanes that is oxolane substituted by 4-aminoacyl-pyridine-2-carboxamide, 3,4-difluoro-2-methoxyphenyl, methyl, and trifluoromethyl groups at positions 2, 3, 4, 5, and 5, respectively (the 2R,3S,4S,5R-stereoisomer). It is a selective blocker of the NaV 1.8 voltage-gated sodium channel and has been approved for the treatment of moderate to severe acute pain in adults.

Pharmacological roles (ChEBI): non-narcotic analgesic, voltage-gated sodium channel blocker.

Also known as: Suzetrigina, Suzetrigine, VRT-1737548, Vx-548, VX-548, VXc-548, SUZETRIGINE, VXC-548, SUZETRIGINA, VX548

Patent coverage: 13 distinct patent families (41 SureChEMBL compound mentions), from 2 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
SCN10A	Nav1.8	Binding	7.19	0.1%	Q9Y5Y9

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): SCN10A.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Developmental Biology	1	SCN10A
L1CAM interactions	1	SCN10A
Muscle contraction	1	SCN10A
Axon guidance	1	SCN10A
Interaction between L1 and Ankyrins	1	SCN10A
Cardiac conduction	1	SCN10A
Phase 0 - rapid depolarisation	1	SCN10A
Nervous system development	1	SCN10A

Dominant GO biological processes

GO term	Targets
regulation of heart rate	1
sensory perception	1
regulation of monoatomic ion transmembrane transport	1
sodium ion transmembrane transport	1
odontogenesis of dentin-containing tooth	1
regulation of cardiac muscle contraction	1
regulation of atrial cardiac muscle cell membrane depolarization	1
cardiac muscle cell action potential involved in contraction	1
membrane depolarization during action potential	1
AV node cell action potential	1
bundle of His cell action potential	1
monoatomic ion transport	1
sodium ion transport	1
monoatomic ion transmembrane transport	1
transmembrane transport	1

Indications & clinical

Indications

3 indications (0 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
diabetic neuropathy	2	MONDO:0006626	EFO:1000783
neuralgia	1	MONDO:0021667	EFO:0009430

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

Clinical trials

Total trials: 41.

Phase distribution

Phase	Trials
PHASE4	12
PHASE1	12
PHASE3	10
PHASE2	5
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07145346	PHASE4	ENROLLING_BY_INVITATION	Suzetrigine for Acute Pain Control in Patients With Multiple Rib Fractures
NCT07195669	PHASE4	NOT_YET_RECRUITING	RCT: Suzetrigine vs Norco for Post-op Pain
NCT07219888	PHASE4	ENROLLING_BY_INVITATION	Comparison of Suzetrigine and Oxycodone for Postoperative Pain After Primary Total Knee Arthroplasty
NCT07355166	PHASE4	NOT_YET_RECRUITING	Suzetrigine Versus Usual-care Opioids for Postop Pain in Sports
NCT07463430	PHASE4	ENROLLING_BY_INVITATION	Suzetrigine for Non-Mastectomy Breast Surgery
NCT07534709	PHASE4	NOT_YET_RECRUITING	Suzetrigine for Opioid-Free Recovery After Cesarean Delivery
NCT07538570	PHASE4	RECRUITING	Evaluation of Pain Treatment After Total Knee Arthroplasty
NCT07575230	PHASE4	ENROLLING_BY_INVITATION	Suzetrigine vs Norco-postoperative Mohs Pain
NCT07600697	PHASE4	NOT_YET_RECRUITING	Suzetrigine for Opioid-Sparing Postoperative Analgesia Following Transvaginal Pelvic Reconstructive Surgery
NCT06887959	PHASE4	COMPLETED	A Single-arm Study Evaluating the Effectiveness and Safety of Suzetrigine (SUZ) for Acute Pain After Selected Surgeries
NCT06887972	PHASE4	COMPLETED	A Single-Arm Study Evaluating the Effectiveness and Safety of Suzetrigine (SUZ) for Acute Pain After Aesthetic or Reconstructive Surgeries
NCT07257133	PHASE4	COMPLETED	A Study Of Opioid Avoidance In Surgery Through Integrating Suzetrigine
NCT06628908	PHASE3	RECRUITING	Evaluation of Efficacy and Safety of Suzetrigine for Pain Associated With Diabetic Peripheral Neuropathy
NCT06696443	PHASE3	ACTIVE_NOT_RECRUITING	Evaluation of the Long-term Safety and Effectiveness of Suzetrigine (SUZ) in Participants With Painful Diabetic Peripheral Neuropathy (DPN)
NCT07226700	PHASE3	RECRUITING	Suzetrigine in Total Hip Arthroplasty
NCT07231419	PHASE3	RECRUITING	Evaluation of Efficacy and Safety of Suzetrigine (SUZ) for Pain Associated With Diabetic Peripheral Neuropathy
NCT07357376	PHASE3	NOT_YET_RECRUITING	Evaluating Suzetrigine for Pain Control Following TKA
NCT07525219	PHASE3	NOT_YET_RECRUITING	Suzetrigine Frame Trial Comparing Suzetrigine and Acetaminophen
NCT07539623	PHASE3	RECRUITING	Suzetrigine-enhanced MultimOdal Opioid-sparing THerapy in Cardiac and Bariatric SURGery
NCT07548385	PHASE3	RECRUITING	Suzetrigine for Treatment and Reduction of Intense Discomfort After knEe Replacement PAIN
NCT05558410	PHASE3	COMPLETED	Evaluation of Efficacy and Safety of Suzetrigine for Acute Pain After an Abdominoplasty
NCT05661734	PHASE3	COMPLETED	A Single-arm Study to Evaluate Safety and Effectiveness of VX-548 for Acute Pain
NCT04977336	PHASE2	COMPLETED	A Study Evaluating Efficacy and Safety of VX-548 for Acute Pain After a Bunionectomy
NCT05034952	PHASE2	COMPLETED	A Study Evaluating Efficacy and Safety of VX-548 for Acute Pain After an Abdominoplasty
NCT05660538	PHASE2	COMPLETED	Evaluation of Efficacy and Safety of VX-548 for Painful Diabetic Peripheral Neuropathy (DPN)
NCT06176196	PHASE2	COMPLETED	Evaluation of Efficacy and Safety of VX-548 for Painful Lumbosacral Radiculopathy (PLSR)
NCT06774625	PHASE2	COMPLETED	This is a Study Evaluating the Efficacy and Safety of LTG-001 for Acute Pain After Surgical Removal of Impacted Third Molars
NCT07378865	PHASE1	RECRUITING	Evaluation of the Excretion of Suzetrigine Into Breast Milk in Healthy Lactating Female Participants
NCT07570069	PHASE1	NOT_YET_RECRUITING	Effects of Efavirenz on the Pharmacokinetics of Suzetrigine in Healthy Participants
NCT05455502	PHASE1	COMPLETED	A Study to Evaluate the Relative Bioavailability and Food Effect of a New Tablet Formulation of VX-548
NCT05541471	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetic Drug-drug Interactions Between VX-548, Midazolam, and Digoxin
NCT05560464	PHASE1	COMPLETED	Evaluation of the Pharmacokinetics and Safety of VX-548 in Participants With Mild or Moderate Hepatic Impairment
NCT05635110	PHASE1	COMPLETED	Evaluation of the Effects of Omeprazole and Rifampin on the Pharmacokinetics of VX-548 in Healthy Participants
NCT05704556	PHASE1	COMPLETED	Evaluation of the Pharmacokinetics and Safety of VX-548 in Participants With Renal Impairment
NCT05818852	PHASE1	COMPLETED	A Study to Evaluate the Effect of VX-548 on the QT/QTc Interval in Healthy Participants
NCT05851157	PHASE1	COMPLETED	A Study to Evaluate the Effect of Food on the Pharmacokinetics of VX-548
NCT06336096	PHASE1	COMPLETED	A Study to Evaluate the Relative Bioavailability and Food Effect of a New Tablet Formulation and Strength of Suzetrigine
NCT06420765	PHASE1	COMPLETED	A Microneurography Study of NaV1.8 Inhibition in Healthy Adults
NCT06820307	PHASE1	COMPLETED	Evaluation of the Effect of Suzetrigine (SUZ) on the Pharmacokinetics of Oral Contraceptives in Healthy Female Participants
NCT07511400	EARLY_PHASE1	RECRUITING	The Role of NaV1.8 in Human Pain Models

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

21 molecules share ≥1 primary target. Top 21 by shared-target count:

Molecule	Source	Status	Shared targets
AMIODARONE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
AMITRIPTYLINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
CHLORPROMAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
DILTIAZEM	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
LAMOTRIGINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
MEXILETINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
NIFEDIPINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A
MIBEFRADIL	ChEMBL	Phase 4 (approved)	SCN10A
SERTINDOLE	ChEMBL	Phase 4 (approved)	SCN10A
AJMALINE	ChEMBL	Phase 3	SCN10A
ELECLAZINE	ChEMBL	Phase 3	SCN10A
NITRENDIPINE	ChEMBL	Phase 3	SCN10A
TEDISAMIL	ChEMBL	Phase 3	SCN10A
VIXOTRIGINE	ChEMBL	Phase 3	SCN10A
CIFENLINE	ChEMBL	Phase 2	SCN10A
FUNAPIDE	ChEMBL	Phase 2	SCN10A
PF-04531083	ChEMBL	Phase 2	SCN10A
Dofetilide	PubChem	Approved	SCN10A