Nefopam

Summary

Nefopam (CHEMBL465026) is an approved small molecule (ATC N02BG06); indicated across 4 conditions including gastric neoplasm and burn.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02BG06
• Indications: 4 conditions
• Clinical trials: 33
• Chemistry: 253.34 Da · C17H19NO

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL465026
Name	Nefopam
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4450
ChEBI	CHEBI:88318
ATC	N02BG06
Molecular formula	C17H19NO
Molecular weight	253.34
InChIKey	RGPDEAGGEXEMMM-UHFFFAOYSA-N

SMILES: CN1CCOC(C2=CC=CC=C2C1)C3=CC=CC=C3

IUPAC name: 5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine

ChEBI definition: A member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively.

Also known as: Nefopam, nefopam, SID26748505, NEFOPAM

Parent form; salt/anhydrous children: CHEMBL1407915

Patent coverage: 1,462 distinct patent families (5,643 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

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Survival motor neuron protein, 5-hydroxytryptamine receptor 2B, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2C.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 17 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC6A4	7.02	AC50	96	nM	CHEMBL_ACT_25150746
SLC6A2	6.7	AC50	200	nM	CHEMBL_ACT_25145417
HRH1	6.19	AC50	650	nM	CHEMBL_ACT_25212942
TDP1	5.95	Potency	1122	nM	CHEMBL_ACT_3927934
KCNH2	5.75	AC50	1800	nM	CHEMBL_ACT_25118471
SLC6A3	5.75	AC50	1800	nM	CHEMBL_ACT_25124372
HTR2B	5.58	AC50	2600	nM	CHEMBL_ACT_25227926
OPRK1	5.43	AC50	3700	nM	CHEMBL_ACT_25129819
OPRM1	5.43	AC50	3700	nM	CHEMBL_ACT_25147182
HTR2C	5.42	AC50	3800	nM	CHEMBL_ACT_25132217
CHRM1	5.39	AC50	4100	nM	CHEMBL_ACT_25135889
HTR2A	5.23	AC50	5900	nM	CHEMBL_ACT_25225559
ADRA2B	5.12	AC50	7600	nM	CHEMBL_ACT_25144119
CHRM3	5.1	AC50	8000	nM	CHEMBL_ACT_25137100

Target pathways

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

Indications & clinical

Indications

4 indications (2 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
gastric neoplasm	3	MONDO:0021085	MONDO:0001056
burn	2	MONDO:0043519	EFO:0009516

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

Clinical trials

Total trials: 33.

Phase distribution

Phase	Trials
Not specified	13
PHASE3	7
PHASE4	5
PHASE2/PHASE3	3
PHASE2	3
PHASE1	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07423650	PHASE4	RECRUITING	Continous Infusion of Nefopam for Patients Undergoing Pancreatoduodenectomy
NCT01882530	PHASE4	TERMINATED	Non-opioid Analgesic Combination With Morphine for Postoperative Analgesia.
NCT02493231	PHASE4	UNKNOWN	Effect of Intraoperative Nefopam on Acute Pain After Remifentanil Based Anesthesia
NCT04110665	PHASE4	COMPLETED	Multimodal Analgesia Strategies After Major Shoulder Ambulatory Surgery
NCT04241640	PHASE4	COMPLETED	Nefopam for Post Video-Assisted Thoracoscopic Lobectomy
NCT06349798	PHASE3	NOT_YET_RECRUITING	Early and Late Effects of Nefopam in Multimodal Analgesia After Total Hip Arthroplasty (NEFARTHRO)
NCT00413257	PHASE2/PHASE3	COMPLETED	Effects of Nefopam on Hyperalgesia After Cardiac Surgery
NCT01577407	PHASE3	COMPLETED	Non Opioid Treatment for Experimental Dyspnea
NCT02126332	PHASE3	COMPLETED	Epidural Analgesia for Pancreatitis (Epipan Study)
NCT02444897	PHASE3	COMPLETED	The Comparison Between Epidural and Intravenous Patient-controlled Analgesia for Laparoscopic Gastrectomy
NCT02596269	PHASE2/PHASE3	COMPLETED	Nefopam/Fentanyl Postoperative Intravenous Patient-Controlled-Analgesia
NCT03626753	PHASE2/PHASE3	COMPLETED	Comparison of Two Routes of Administration of a Multimodal Analgesic Protocol in Postoperative Cesarean Section
NCT04622813	PHASE3	COMPLETED	Nonopioid Analgesics and Cholecystectomy
NCT05071352	PHASE3	COMPLETED	Adjuvant Continuous Infusion of Nefopam Versus Standard of Care in Mechanically Ventilated Critically Ill Patients: Randomized Double-blind Controlled Study
NCT05648058	PHASE3	UNKNOWN	Role of Nefopam in Rituximab Transfusion Reaction
NCT04576078	PHASE2	RECRUITING	Post-operative Analgesic Effect of Oral Nefopam
NCT02441673	PHASE2	UNKNOWN	Nefopam vs Tramadol in the Prevention of Post Anaesthetic Shivering
NCT04685577	PHASE2	COMPLETED	Safety, Tolerability and Efficacy of Nefopam Cream in Burn Patients
NCT02174068	PHASE1	COMPLETED	A Pharmacokinetic Drug Interaction and Tolerance Study of Paracetamol and Nefopam
NCT06680609	EARLY_PHASE1	COMPLETED	The Analgesic Efficacy of Nefopam in Orthopedics Surgery
NCT01461031	Not specified	COMPLETED	Effect of Nefopam on Acute Postoperative Pain in Patients Undergoing Orthognathic Surgery
NCT01622881	Not specified	COMPLETED	Analgesic Efficacy of Nefopam in Patients Undergoing Kidney Transplantation
NCT01732666	Not specified	COMPLETED	Effect of Nefopam on Remifentanil Induced Postoperative Hyperalgesia
NCT01808014	Not specified	UNKNOWN	The Analgesic Effect of Nefopam on the Fentanyl Based PCA (Patient-controlled Analgesia) After Lumbar Spinal Surgery
NCT02561468	Not specified	COMPLETED	The Preemptive Analgesic Efficacy of Nefopam
NCT02561494	Not specified	COMPLETED	Postoperative Analgesic Effect of Nefopam
NCT02577068	Not specified	COMPLETED	Combination Effect of Nefopam With Propacetamol for Postoperative Pain After Thyroidectomy
NCT02949310	Not specified	UNKNOWN	Effectiveness of Nefopam in Breast Cancer Surgery
NCT03619538	Not specified	COMPLETED	Interest of the Nefopam and PCA Morphine Combination for Postoperative Analgesia in Patients Undergoing Colon Surgery
NCT03955705	Not specified	UNKNOWN	Analgesic Effectiveness of Nefopam in Patients Undergoing Anterior Cervical Spine Surgery
NCT04450355	Not specified	COMPLETED	Effects of Continuous Infusion of Intravenous Nefopam on Postoperative Pain and Opioid Consumption After VATS
NCT05173337	Not specified	COMPLETED	Nefopam as a Multimodal Analgesia for Thoracic Surgery
NCT06627816	Not specified	COMPLETED	Efficacy of Intravenous Nefopam, Dexmedetomidine, and Meperidine in Preventing Post-Spinal Anesthesia Shivering in Adult Patients Undergoing Lower Abdominal and Lower Limb Surgeries.

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).