Sufentanil

Summary

Sufentanil (CHEMBL658) is an approved small-molecule opioid analgesic (ATC N01AH03) targeting OPRM1; indicated across 7 conditions including injury and pulpitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N01AH03
• Targets: 1 (OPRM1)
• Indications: 7 conditions
• Clinical trials: 179
• Chemistry: 386.6 Da · C22H30N2O2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL658
Name	Sufentanil
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	41693
ChEBI	CHEBI:9316
ATC	N01AH03
Molecular formula	C22H30N2O2S
Molecular weight	386.6
InChIKey	GGCSSNBKKAUURC-UHFFFAOYSA-N

SMILES: CCC(=O)N(C1=CC=CC=C1)C2(CCN(CC2)CCC3=CC=CS3)COC

IUPAC name: N-[4-(methoxymethyl)-1-(2-thiophen-2-ylethyl)piperidin-4-yl]-N-phenylpropanamide

ChEBI definition: An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid.

Pharmacological roles (ChEBI): opioid analgesic, μ-opioid receptor agonist, anaesthesia adjuvant, intravenous anaesthetic.

Also known as: IDS-NS-001, R 30,730, R-30730, Sufentanil, Sufentanilo, Sufentanyl, sufentanil, Sulfentanil, SUFENTANIL

Parent form; salt/anhydrous children: CHEMBL1201163, CHEMBL4747678

Patent coverage: 5,553 distinct patent families (23,762 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
OPRM1	μ receptor	Full agonist	9.9	0%	P35372

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Opioid receptor, Mu-type opioid receptor, Mu-type opioid receptor, Sigma non-opioid intracellular receptor 1, ATP-dependent translocase ABCB1, Solute carrier family 22 member 1.

Bioactivity

ChEMBL activities: 9 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
P33533	10.7	Ki	0.02	nM	CHEMBL_ACT_340278
P33535	9.66	Ki	0.22	nM	CHEMBL_ACT_101821
P33535	9.4	IC50	0.4	nM	CHEMBL_ACT_19128514
OPRM1	8.89	EC50	1.3	nM	CHEMBL_ACT_19115255
OPRM1	8.82	EC50	1.5	nM	CHEMBL_ACT_19115257
P33533	8.64	IC50	2.3	nM	CHEMBL_ACT_90992
OPRM1	8.11	Ki	7.8	nM	CHEMBL_ACT_29160758
Q60492	5.68	IC50	2077	nM	CHEMBL_ACT_19128527
ABCB1	5.35	IC50	4500	nM	CHEMBL_ACT_11001473

Target pathways

Aggregated over 1 target gene(s): OPRM1.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Opioid Signalling	1	OPRM1
G-protein activation	1	OPRM1
Peptide ligand-binding receptors	1	OPRM1
G alpha (i) signalling events	1	OPRM1
Interleukin-4 and Interleukin-13 signaling	1	OPRM1
MECP2 regulates neuronal receptors and channels	1	OPRM1

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
neuropeptide signaling pathway	1
sensory perception	1
negative regulation of cell population proliferation	1
sensory perception of pain	1
G protein-coupled opioid receptor signaling pathway	1
negative regulation of nitric oxide biosynthetic process	1
behavioral response to ethanol	1
positive regulation of neurogenesis	1
negative regulation of cytosolic calcium ion concentration	1
negative regulation of Wnt protein secretion	1

Indications & clinical

Indications

7 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
injury	3	MONDO:0021178	EFO:0000546
pulpitis	2	MONDO:0006937	EFO:1001139
delirium	0	MONDO:0045057	EFO:0009267

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

Clinical trials

Total trials: 179.

Phase distribution

Phase	Trials
Not specified	79
PHASE4	62
PHASE3	17
PHASE2	11
PHASE2/PHASE3	4
PHASE1/PHASE2	2
EARLY_PHASE1	2
PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00577200	PHASE4	ACTIVE_NOT_RECRUITING	Safety of Driving After Minor Surgery With Monitored Anesthesia Care
NCT05826327	PHASE4	RECRUITING	Effects of Epidural Labor Analgesia With Esketamine on the Incidence of Postpartum Depression in Parturients
NCT06037330	PHASE4	RECRUITING	Nalbuphine in ARDS Patients After Surgery
NCT06784999	PHASE4	RECRUITING	Sufentanil Infusion vs Intravenous Methadone for Postoperative Analgesia Following Head and Neck Dissection With Free Flap or Rotational Reconstruction
NCT06958393	PHASE4	NOT_YET_RECRUITING	Effect of Opioid-free Anaesthesia on Postoperative Delirium in Elderly Patients Undergoing Gastrointestinal Surgery
NCT07018375	PHASE4	NOT_YET_RECRUITING	The Effect of Oliceridine Patient-Controlled Intravenous Analgesia on Postoperative Chronic Pain After Video-Assisted Thoracoscopic Lobectomy
NCT07019818	PHASE4	RECRUITING	Esmolol Versus Sufentanil on the Quality of Post-cholecystectomy Recovery Laparoscopic Anaesthesia With Orotracheal Intubation on an Outpatient Basis
NCT07026162	PHASE4	RECRUITING	Oliceridine on Postoperative Nausea and Vomiting in Gynecological Laparoscopic Surgery
NCT07235995	PHASE4	NOT_YET_RECRUITING	Paracetamol and Mannitol Injection and Postoperative Delirium
NCT07597564	PHASE4	NOT_YET_RECRUITING	Dose-Response Interaction of Metoprolol and Sufentanil for Attenuating Hemodynamic Responses in Tracheal Intubation
NCT00421720	PHASE4	TERMINATED	A Study Comparing Two Analgesia/Sedation Regimens, Remifentanil/Propofol Versus Sufentanil/Propofol In Mechanically Ventilated Intensive Care Patients Requiring Analgesia And Sedation.
NCT00772616	PHASE4	COMPLETED	Influence of Intraoperative Analgesia on the Postoperative Morphine Consumption
NCT01320475	PHASE4	TERMINATED	Epidural Levobupivacaine-sufentanil Versus Epidural Levobupivacaine and Intravenous Ketamine
NCT01356732	PHASE4	COMPLETED	Determination of the 90% Effective Dose of a Sufentanil Bolus in Analgesia During Lateral Decubitus of Mechanically Ventilated Patients
NCT01490268	PHASE4	COMPLETED	Pain Therapy After Elective Cardiac Surgery
NCT01516268	PHASE4	COMPLETED	The Effect of Adding Sufentanyl to Bupivacaine in Transversus Abdominis Plane Block to Reduce the Narcotic Dosage and Pain After Cesarean Delivery
NCT01777100	PHASE4	COMPLETED	Sufentanil for Anesthesia Induction in Continuous Remifentanil Anesthesia
NCT01954368	PHASE4	COMPLETED	Intranasal Sufentanil Pain-management at Entrance of Emergency Department : Influence on Pain-relief Delay
NCT02053818	PHASE4	COMPLETED	Remifentanil/Sufentanil for CABG+/-AVR Evaluated by Recovery, Cognitive Function, Haemodynamics and Biochemical Markers.
NCT02085577	PHASE4	COMPLETED	The Effect of Intraoperative Ketamine on Opioid Consumption and Pain After Spine Surgery in Opioid-dependent Patients
NCT02095366	PHASE4	COMPLETED	Intra Nasal Sufentanil Versus Intravenous Morphine for Acute Severe Traumatic Pain Analgesia in Emergency Setting
NCT02111265	PHASE4	UNKNOWN	THe Comparison of Target Controlled Infusion of Propofol or Etomidate at General Anesthesia in Geriatric Patients
NCT02152514	PHASE4	TERMINATED	RCT Comparing Analgesia Post-VATS With Epimorph VS Placebo
NCT02213718	PHASE4	UNKNOWN	The Effect of Desflurane on Myocardial Function in Patients Undergoing Coronary Artery Bypass Grafting
NCT02503826	PHASE4	UNKNOWN	The Efficacy and Optimal Dose of Sufentanil in Patient Controlled Analgesia After Moderate Surgery
NCT02544282	PHASE4	COMPLETED	Large-scale Prospective Double-blind Randomized Controlled Trial of Pecs II Block for Breast Surgery
NCT02552459	PHASE4	UNKNOWN	Effect of Dexmedetomidine Combined With Sufentanil for Postoperative Intravenous Analgesia in Neurosurgery
NCT02573597	PHASE4	TERMINATED	PIEB vs CEI for Labor Analgesia: An MLAC Study
NCT02741219	PHASE4	COMPLETED	A Multicenter Study: Dexmedetomidine Combined With Sufentanil for Patient Controlled Intravenous Analgesia After Caesarean Section
NCT02816567	PHASE4	UNKNOWN	Laparoscopic Surgery and Abdominal Compliance
NCT02923128	PHASE4	COMPLETED	Whether Dexmedetomidine Can Improve the Prognosis of Elderly Patients With Postoperative Cognitive Dysfunction
NCT02989597	PHASE4	TERMINATED	Intraoperative Methadone Administration for Improved Pain Control in Spinal Fusion Patients
NCT03018171	PHASE4	UNKNOWN	Intrathecal Clonidine Addiction for Combined Spinal Epidural Analgesia During Labor
NCT03135795	PHASE4	UNKNOWN	The Epigenetic Modification in OPRM1 on Postoperative Analgesia and Side Effect Induced by Sufentanil
NCT03152955	PHASE4	UNKNOWN	Postoperative Analgesia in Patients With Microvascular Decompression
NCT03224039	PHASE4	UNKNOWN	Intranasal Sufentanil Versus Intravenous Morphine for the Management of Acute Pain
NCT03344042	PHASE4	UNKNOWN	Effect of Epidural Opioid Administered in the First A Period on the Progress of Labour
NCT03386630	PHASE4	COMPLETED	Effects of Analgesics in Cesarean Section Elective
NCT03726268	PHASE4	COMPLETED	Optimizing Outpatient Anesthesia (OSPREy-Outpatient Surgery Pain Relief Enhancement)
NCT03901716	PHASE4	COMPLETED	Comparison of Sufentanil, Fentanyl and Remifentanil in Combination With Midazolam During Bronchoscopy Under Conscious Sedation

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for alfentanil, buprenorphine, codeine, f	CPIC	COMT;OPRM1

PharmGKB also curates 12 clinical and 68 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.

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

Molecule	Source	Status	Shared targets
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
ELUXADOLINE	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
MAVORIXAFOR	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
PIMAVANSERIN	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
VORAPAXAR	ChEMBL + PubChem	Phase 4 (approved)	OPRM1
ALFENTANIL	ChEMBL	Phase 4 (approved)	OPRM1
ALOGLIPTIN	ChEMBL	Phase 4 (approved)	OPRM1
ALPIDEM	ChEMBL	Phase 4 (approved)	OPRM1
ALVIMOPAN	ChEMBL	Phase 4 (approved)	OPRM1
AMBENONIUM	ChEMBL	Phase 4 (approved)	OPRM1
AMILORIDE	ChEMBL	Phase 4 (approved)	OPRM1
AMIODARONE	ChEMBL	Phase 4 (approved)	OPRM1
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	OPRM1
AMLODIPINE	ChEMBL	Phase 4 (approved)	OPRM1
AMODIAQUINE	ChEMBL	Phase 4 (approved)	OPRM1
AMOXAPINE	ChEMBL	Phase 4 (approved)	OPRM1
ANTAZOLINE	ChEMBL	Phase 4 (approved)	OPRM1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	OPRM1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	OPRM1
ATOMOXETINE	ChEMBL	Phase 4 (approved)	OPRM1
AZELASTINE	ChEMBL	Phase 4 (approved)	OPRM1
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	OPRM1
BENFLUOREX	ChEMBL	Phase 4 (approved)	OPRM1
BENZBROMARONE	ChEMBL	Phase 4 (approved)	OPRM1
BENZIODARONE	ChEMBL	Phase 4 (approved)	OPRM1
BENZTROPINE	ChEMBL	Phase 4 (approved)	OPRM1
BENZYDAMINE	ChEMBL	Phase 4 (approved)	OPRM1
BEPRIDIL	ChEMBL	Phase 4 (approved)	OPRM1
BEXAROTENE	ChEMBL	Phase 4 (approved)	OPRM1
BITHIONOL	ChEMBL	Phase 4 (approved)	OPRM1
BOSUTINIB	ChEMBL	Phase 4 (approved)	OPRM1
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	OPRM1
BROMODIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	OPRM1
BROMPERIDOL	ChEMBL	Phase 4 (approved)	OPRM1
BUPRENORPHINE	ChEMBL	Phase 4 (approved)	OPRM1
BUTORPHANOL	ChEMBL	Phase 4 (approved)	OPRM1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	OPRM1
CANNABIDIOL	ChEMBL	Phase 4 (approved)	OPRM1
CARVEDILOL	ChEMBL	Phase 4 (approved)	OPRM1
CASPOFUNGIN	ChEMBL	Phase 4 (approved)	OPRM1
CETRORELIX	ChEMBL	Phase 4 (approved)	OPRM1
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	OPRM1
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	OPRM1
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	OPRM1
CINACALCET	ChEMBL	Phase 4 (approved)	OPRM1
CINNARIZINE	ChEMBL	Phase 4 (approved)	OPRM1
CITALOPRAM	ChEMBL	Phase 4 (approved)	OPRM1
CLEMASTINE	ChEMBL	Phase 4 (approved)	OPRM1
CLOMIPHENE	ChEMBL	Phase 4 (approved)	OPRM1
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	OPRM1
CLOPIDOGREL	ChEMBL	Phase 4 (approved)	OPRM1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	OPRM1
COBIMETINIB	ChEMBL	Phase 4 (approved)	OPRM1
CODEINE	ChEMBL	Phase 4 (approved)	OPRM1
CYCLIZINE	ChEMBL	Phase 4 (approved)	OPRM1
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	OPRM1
DANAZOL	ChEMBL	Phase 4 (approved)	OPRM1