Alfentanil

Summary

Alfentanil (CHEMBL634) is an approved small-molecule opioid analgesic (ATC N01AH02).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N01AH02
• Clinical trials: 38
• Chemistry: 416.5 Da · C21H32N6O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL634
Name	Alfentanil
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	51263
ChEBI	CHEBI:2569
ATC	N01AH02
Molecular formula	C21H32N6O3
Molecular weight	416.5
InChIKey	IDBPHNDTYPBSNI-UHFFFAOYSA-N

SMILES: CCC(=O)N(C1=CC=CC=C1)C2(CCN(CC2)CCN3C(=O)N(N=N3)CC)COC

IUPAC name: N-[1-[2-(4-ethyl-5-oxotetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl]-N-phenylpropanamide

ChEBI definition: A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.

Pharmacological roles (ChEBI): opioid analgesic, μ-opioid receptor agonist, intravenous anaesthetic, central nervous system depressant, peripheral nervous system drug.

Also known as: Afentanyl, Alfentanil, Alfentanilo, Alfentanyl, IDS-NA-014, alfentanil, ALFENTANIL

Parent form; salt/anhydrous children: CHEMBL1200531

Patent coverage: 4,057 distinct patent families (16,965 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 16,964 (100%) 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

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Opioid receptor, Mu-type opioid receptor, Mu-type opioid receptor.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
P33533	8.09	Ki	8.21	nM	CHEMBL_ACT_314733
P33535	8.09	Ki	8.21	nM	CHEMBL_ACT_93798
P97266	7.82	IC50	15	nM	CHEMBL_ACT_146856
P33535	7.41	IC50	38.9	nM	CHEMBL_ACT_19128511

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 38.

Phase distribution

Phase	Trials
Not specified	20
PHASE4	16
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06563297	PHASE4	NOT_YET_RECRUITING	To Explore the Optimal Dose of Alfentanil for Skull Pin Fixation in Intracranial Surgery
NCT07347496	PHASE4	NOT_YET_RECRUITING	A Randomized, Controlled Clinical Trial Comparing Remimazolam Besylate Combined With Alfentanil Versus Propofol Combined With Alfentanil for Anesthesia in Thoracic Surgery
NCT07395596	PHASE4	RECRUITING	Remimazolam for Bronchoscopy in High-Risk Patients
NCT07581665	PHASE4	NOT_YET_RECRUITING	Effective Dose of Alfentanil Combined With Propofol for Laryngeal Mask Airway Insertion in Children
NCT00440960	PHASE4	COMPLETED	Anesthesia in Flexible Bronchoscopy for Lung Cancer Diagnostic
NCT00997113	PHASE4	COMPLETED	Stress During Deep Sedation With Propofol With and Without Alfentanil
NCT00997126	PHASE4	COMPLETED	Propofol Versus Alfentanil Versus Nitrous Oxide for Moderate Procedural Sedation
NCT01199458	PHASE4	COMPLETED	The Effect of an Opioid on the Lower Esophageal Sphincter During Anesthesia Induction
NCT01350037	PHASE4	COMPLETED	Alfentanil Versus Remifentanil in Patient-controlled Sedation During Endoscopic Retrograde Cholangiopancreatography (ERCP)
NCT01470170	PHASE4	COMPLETED	Regimen of Alfentanil in Propofol Sedative Fibro-bronchoscopy
NCT01518608	PHASE4	COMPLETED	Alfentanil and the Elimination of Sympathetic Responses to Tracheal Intubation During Rapid Sequence Induction of Anesthesia: A Probability-based Approach
NCT02022488	PHASE4	COMPLETED	Sevoflurane Induced Emergence Agitation
NCT02267681	PHASE4	COMPLETED	Opioid Effects on Cognitive Function Following Colonoscopy
NCT02358057	PHASE4	COMPLETED	Can we Get Conscious Sedation by Combining Dexmedetomidine With Alfentanil?
NCT03359395	PHASE4	COMPLETED	Pre-medication With Alfentanil vs Placebo During ECT
NCT05688384	PHASE4	COMPLETED	Patient-Controlled Sedation in Port Implantation (PACSPI-2)
NCT01235637	PHASE3	COMPLETED	Alfentanil Versus Sufentanil for Pain in Children During for Tracheal Suction
NCT01805726	PHASE3	COMPLETED	Sedation During Bronchoscopy:Dexmedetomidine vs Alfentanil
NCT00226564	Not specified	COMPLETED	Genetic Determinants of Opioids Analgesia
NCT00434382	Not specified	UNKNOWN	Neuronal Mechanisms of Sensory Processing During General Anesthesia
NCT00566683	Not specified	COMPLETED	Comparison Between Nurse-Administered Propofol Sedation and Diazemuls / Pethidine in Outpatient Colonoscopy
NCT00672438	Not specified	COMPLETED	Heritability of Opioid Effects: A Twin Study
NCT00991809	Not specified	COMPLETED	Study on the Development of Opioid Induced Hyperalgesia (OIH) After Exposure to Alfentanil
NCT01008059	Not specified	COMPLETED	Alfentanil: Simultaneous Testing Pilot
NCT01049672	Not specified	COMPLETED	Diamorphine or Alfentanil for Subcutaneous Use in Hospice In-patients?
NCT01094574	Not specified	COMPLETED	Evaluation of Propranolol’s Effect on Pain and Inflammation.
NCT01371968	Not specified	COMPLETED	Optimal Dose of Alfentanil for Removal of Supreme Laryngeal Mask Airway During Emergence From Desflurane Anaesthesia
NCT01436799	Not specified	COMPLETED	Desflurane Versus Propofol in the Sitting Position
NCT01550354	Not specified	COMPLETED	Comparison Among Propofol, Alfentanil and Rocuronium as Adjunct to Sevoflurane Anesthesia for Endotracheal Intubation in Children With Frenectomy
NCT02000206	Not specified	UNKNOWN	Comparison of Propofol/Alfentanil With Propofol/Ketamine
NCT02486926	Not specified	COMPLETED	The Effects of Remifentanil and Remifentanil-Alfentanil Administration in Children
NCT02625181	Not specified	COMPLETED	Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis
NCT02646592	Not specified	COMPLETED	Effect of a Bolus of 10 µg/kg of Alfentanil on the Pupillary Pain Index
NCT03813875	Not specified	COMPLETED	Modeling and Application of Triple Drug Response Surface Models
NCT04631393	Not specified	COMPLETED	Patient-controlled Sedation in Port Implantation (PACSPI-1)
NCT05525351	Not specified	UNKNOWN	The Application and Validation of Triple Drug Response Surface Models on Density Spectral Array in Clinical Anesthesia
NCT06212622	Not specified	COMPLETED	Is the Rate of Early Mobilisation in Hip Fracture Patients Using Alfentanil Better Than Standard Opioid Analgesia?
NCT06414018	Not specified	COMPLETED	Effect of Equivalent Dose of Alfentanil and Sufentanil in Bronchoscopic Treatment

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 4 clinical and 8 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).