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Naloxone

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Also known as Dbl naloxoneNaloxonaNSC-70413Nalaxone(-)-naloxoneNaloxaneSID144205559SID170465008NACO-ADD:0136632NALOXONE HYDROCHLORIDE(+)-Naloxone

Summary

Naloxone (CHEMBL80) is an approved small-molecule μ-opioid receptor antagonist (ATC A06AH04) targeting OPRD1, OPRK1, and OPRM1; indicated across 28 conditions including constipation disorder and epilepsy.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A06AH04 (+1 more)
  • Targets: 3 (OPRD1, OPRK1, OPRM1)
  • Indications: 28 conditions
  • Clinical trials: 185
  • Chemistry: 327.4 Da · C19H21NO4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL80
NameNaloxone
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID5284596
ChEBICHEBI:7459
ATCA06AH04, V03AB15
Molecular formulaC19H21NO4
Molecular weight327.4
InChIKeyUZHSEJADLWPNLE-GRGSLBFTSA-N

SMILES: C=CCN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O

IUPAC name: (4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one

ChEBI definition: A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.

Pharmacological roles (ChEBI): μ-opioid receptor antagonist, central nervous system depressant, antidote to opioid poisoning.

Also known as: Dbl naloxone, Naloxona, Naloxone, NSC-70413, Nalaxone, naloxone, (-)-naloxone, Naloxane, SID144205559, (-)-Naloxone, SID170465008, NA

Parent form; salt/anhydrous children: CHEMBL1718, CHEMBL1512507, CHEMBL3186613, CHEMBL5315056

Patent coverage: 10,866 distinct patent families (38,742 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 38,724 (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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
OPRD1δ receptorAntagonist7.20.2%P41143
OPRK1κ receptorAntagonist8.60%P41145
OPRM1μ receptorAntagonist8.90%P35372

Broader ChEMBL bioactivity targets: 18 (assay-derived). Sample: NADPH oxidase 2, Opioid receptor, Opioid receptors; mu & kappa, Opioid receptors; mu/kappa/delta, Mu-type opioid receptor, Delta-type opioid receptor, Kappa-type opioid receptor, Delta-type opioid receptor, Mu-type opioid receptor, Mu-type opioid receptor.

Bioactivity

ChEMBL activities: 181 potent at pChembl ≥ 5 of 182 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
OPRM19.66Kd0.22nMCHEMBL_ACT_1817095
OPRM19.66Kd0.22nMCHEMBL_ACT_2077893
OPRM19.64Ki0.23nMCHEMBL_ACT_6192896
OPRK19.6Ki0.25nMCHEMBL_ACT_6192882
P335359.4Kd0.4nMCHEMBL_ACT_227820
OPRM19.25Ki0.56nMCHEMBL_ACT_6227808
OPRM19.24Ki0.57nMCHEMBL_ACT_6262898
OPRM19.18Ki0.66nMCHEMBL_ACT_2263839
P972669.17Ki0.68nMCHEMBL_ACT_1925997
P972669.17Ki0.68nMCHEMBL_ACT_360237
OPRM19.1Ki0.79nMCHEMBL_ACT_1859778
OPRM19.01Ki0.98nMCHEMBL_ACT_2987274
P335339Kd1nMCHEMBL_ACT_14615767
P349759Kd1nMCHEMBL_ACT_227823
OPRM19Ki1nMCHEMBL_ACT_23282395
P335358.97Ki1.07nMCHEMBL_ACT_61398
OPRK18.96Ki1.1nMCHEMBL_ACT_1859786
P972668.96Ki1.1nMCHEMBL_ACT_276831
OPRM18.94Ki1.15nMCHEMBL_ACT_16427807
OPRK18.92Ki1.2nMCHEMBL_ACT_2263841
OPRK18.92Ki1.2nMCHEMBL_ACT_472847
OPRM18.9Ki1.26nMCHEMBL_ACT_16427813
P335338.85IC501.4nMCHEMBL_ACT_240633
P335358.85Ki1.4nMCHEMBL_ACT_472845
OPRK18.82IC501.5nMCHEMBL_ACT_105736
P335338.82EC501.5nMCHEMBL_ACT_14602738
OPRM18.82Ki1.5nMCHEMBL_ACT_2941396
OPRM18.8IC501.6nMCHEMBL_ACT_1611130
OPRM18.8Ki1.6nMCHEMBL_ACT_2439806
OPRM18.73IC501.87nMCHEMBL_ACT_13839304

Target pathways

Aggregated over 3 target gene(s): OPRD1, OPRK1, OPRM1.

Top Reactome pathways

6 total, by targets touching each:

PathwayTargetsGenes
Peptide ligand-binding receptors3OPRD1, OPRK1, OPRM1
G alpha (i) signalling events3OPRD1, OPRK1, OPRM1
Interleukin-4 and Interleukin-13 signaling2OPRD1, OPRM1
MECP2 regulates neuronal receptors and channels2OPRK1, OPRM1
Opioid Signalling1OPRM1
G-protein activation1OPRM1

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway3
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway3
phospholipase C-activating G protein-coupled receptor signaling pathway3
neuropeptide signaling pathway3
G protein-coupled opioid receptor signaling pathway3
signal transduction3
immune response2
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger2
response to nicotine2
eating behavior2
response to ethanol2
sensory perception2
sensory perception of pain2
adult locomotory behavior1
negative regulation of gene expression1

Indications & clinical

Indications

28 indications (1 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).

IndicationTrial phaseMONDOEFO
constipation disorder4MONDO:0002203HP:0002019
epilepsy3MONDO:0005027EFO:0000474
drug dependence3MONDO:0005303EFO:0003890
heroin dependence3MONDO:0005367EFO:0004240
opiate dependence3MONDO:0005530EFO:0005611
morphine dependence3MONDO:0005531EFO:0005612
substance withdrawal syndrome3MONDO:0005567EFO:0005800
Sezary syndrome3MONDO:0017844EFO:1000785
mycosis fungoides3MONDO:0009691EFO:1001051
restless legs syndrome3MONDO:0005391EFO:0004270
osteoarthritis3MONDO:0005178MONDO:0005178
Parkinson disease3MONDO:0005180MONDO:0005180
irritable bowel syndrome2MONDO:0005052EFO:0000555
obesity disorder2MONDO:0011122EFO:0001073
eating disorder2MONDO:0005451EFO:0005203
neuralgia2MONDO:0021667EFO:0005762
diabetic neuropathy2MONDO:0006626MONDO:0001583
hypogonadism2MONDO:0002146MONDO:0018555
type 1 diabetes mellitus2MONDO:0005147MONDO:0005147
hepatitis C virus infection1MONDO:0005231EFO:0003047
intestinal obstruction1MONDO:0004565MONDO:0004565
reproductive system disorder1MONDO:0005039EFO:0000512
pain agnosia0MONDO:0000675EFO:1001484

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

Clinical trials

Total trials: 185.

Phase distribution

PhaseTrials
PHASE442
PHASE234
Not specified34
PHASE130
PHASE322
EARLY_PHASE110
PHASE2/PHASE37
PHASE1/PHASE26

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05944952PHASE4ACTIVE_NOT_RECRUITINGLow-dose Versus a High-dose Sublingual Buprenorphine Induction
NCT06666621PHASE4RECRUITINGEndogenous Opioid Response to Injections
NCT07439549PHASE4RECRUITINGSymptom-Inhibited Naloxone Induction (SINI) for Buprenorphine Initiation: A Feasibility Trial
NCT00007527PHASE4COMPLETEDDetermine the Safety of a Sublingual Tablet Formulation of Buprenorphine and Naloxone by Extending the Combination Tablet Availability to Physicians in Office-Based Practice
NCT00015340PHASE4COMPLETEDBuprenorphine/Naloxone in the Treatment of Heroin Dependence - 14
NCT00315341PHASE4COMPLETEDStarting Treatment With Agonist Replacement Therapies (START)
NCT00552578PHASE4TERMINATEDBuprenorphine as a Treatment in Opiate Dependent Pain Patients
NCT00684073PHASE4COMPLETEDPreference for Subutex® (Buprenorphine) Versus Suboxone® (Buprenorphine/Naloxone) in Opioid Dependent Patients on Subutex® (Study P05094)(COMPLETED)
NCT00784810PHASE4COMPLETEDA Study to Compare Oxycodone/Naloxone Prolonged Release Against Codeine/Paracetamol in the Treatment of Moderate to Severe Chronic Low Back Pain or Pain Due to Osteoarthritis
NCT00799201PHASE4TERMINATEDEnteral Naloxone Versus a Traditional Bowel Regimen for the Prevention of Opioid Induced Constipation in Trauma Patients
NCT00879996PHASE4COMPLETEDBuprenorphine and Methadone for Opioid Dependent Chronic Pain Patients
NCT00921765PHASE4TERMINATEDReversal of Ketamine Pharmacodynamic Effects With Naloxone
NCT01015066PHASE4WITHDRAWNComparison of Buprenorphine/Naloxone With Naltrexone in Opioid Dependent Adolescents
NCT01109511PHASE4COMPLETEDA Comparison of Oxycodone/Naloxone and Oxycodone After Laparoscopic Hysterectomy
NCT01191645PHASE4COMPLETEDOpioid Effects on Swallowing and Esophageal Sphincter Pressure
NCT01313780PHASE4COMPLETEDA Study to Evaluate Efficacy and Safety of Oxycodone/Naloxone Compared to OxyContin in Korean Cancer Patients
NCT01374763PHASE4COMPLETEDA Comparison of PR Oxycodone/Naloxone and PR Oxycodone After Cardiac Surgery
NCT01559454PHASE4COMPLETEDBuprenorphine and Methadone for Opioid-dependent Chronic Back Pain Patients
NCT01719757PHASE4COMPLETEDPROspective Non-interventional Open laBEl Trial for TARGIN in Korean Patients With Cancer Pain
NCT01811186PHASE4COMPLETEDAn Interventional Study to Compare the Efficacy and Tolerability With Targin® in Non-malignant Chronic Pain (GLORY)
NCT01811238PHASE4COMPLETEDAn Interventional Study to Assess the Efficacy and Safety of Oxycodone/Naloxone in Korean Patients With Spinal Disorders
NCT01841931PHASE4TERMINATEDBuprenorphine Treatment: A Safe Alternative for Opioid Dependent Pain Patients
NCT01875848PHASE4TERMINATEDBuprenorphine vs. Opioid Dose Escalation Among Patients With Chronic Pain
NCT01912573PHASE4UNKNOWNNasal Naloxone for Narcotic Overdose
NCT01936857PHASE4COMPLETEDBuprenorphine to Improve HIV Care Engagement and Outcomes
NCT02032927PHASE4WITHDRAWNTreatment of Chronic Pain From Osteoarthritis
NCT02516059PHASE4COMPLETEDEarly Postoperative Administration of Oxycodone +/- Naloxone and Duration of Epidural Analgesia
NCT02885948PHASE4COMPLETEDThe Use of Low Dose Prophylactic Naloxone Infusion to Prevent Respiratory Depression With Intrathecal Morphine.
NCT02939248PHASE4COMPLETEDInfluence of Naloxone on Ticagrelor Pharmacokinetics and Pharmacodynamics in Patients With Unstable Angina Pectoris on Concomitant Treatment With Morphine
NCT03176316PHASE4TERMINATEDThe Use of Oral Naloxone to Prevent Post Spinal Fusion Ileus
NCT03266445PHASE4UNKNOWNEffect of Buprenorphine/Naloxone Continuation on Pain Control and Opioid Use
NCT03608163PHASE4TERMINATEDNovel Approach for the Prevention of Hypoglycemia Associated Autonomic Failure (HAAF)
NCT03740243PHASE4WITHDRAWNBuprenorphine vs Buprenorphine/Naloxone on the Effects of Maternal Symptomatology
NCT03908437PHASE4COMPLETEDRapid Initiation of Drug Treatment Engagement
NCT04091009PHASE4WITHDRAWNEffect of Standard of Care Reduced Dose Versus Full Dose Buprenorphine/Naloxone in the Perioperative Period on Pain Control and Post-Operative Opioid Use Disorder Symptoms
NCT04234516PHASE4WITHDRAWNAnti-suicidal Effects of Buprenorphine in Opioid Use Disorder
NCT04283500PHASE4COMPLETEDBuprenorphine Loading in the Emergency Department
NCT04771689PHASE4WITHDRAWNBuprenorphine/Naloxone Micro-Dosing for Postoperative Pain Management in Opioid-Tolerant Patients
NCT05301712PHASE4COMPLETEDA Phase 4 Clinical Study to Investigate the Efficacy and Safety of Naloxone HCI IV in Patients With Stroke
NCT05644587PHASE4TERMINATEDNovel Induction to Buprenorphine/Naloxone

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 4 clinical and 7 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

MoleculeSourceStatusShared targets
DihydroergotamineChEMBL + PubChemPhase 4 (approved)OPRD1, OPRK1, OPRM1
PROPOXYPHENEChEMBL + PubChemPhase 4 (approved)OPRD1, OPRK1, OPRM1
TAFAMIDISChEMBL + PubChemPhase 4 (approved)OPRD1, OPRK1, OPRM1
ALVIMOPANChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
AMIODARONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
AMLODIPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
AMOXAPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
ASTEMIZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
BENZTROPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
BUPRENORPHINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
BUTORPHANOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CANNABIDIOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CHLORPROMAZINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CINNARIZINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CLOTRIMAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
CODEINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
ECONAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
FENTANYLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
FLUPHENAZINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
FLUSPIRILENEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
HYDROCODONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
HYDROMORPHONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LANSOPRAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LEVORPHANOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LOPERAMIDEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
LOXAPINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
MEPERIDINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
METHADONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
METHYLNALTREXONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
MICONAZOLEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
MORPHINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NAFTOPIDILChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALBUPHINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALFURAFINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALMEFENEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NALTREXONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
NELFINAVIRChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
OLICERIDINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
OXYCODONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
OXYMORPHONEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PAROXETINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PASIREOTIDEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PENTAZOCINEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
PIMOZIDEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
RALOXIFENEChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
RITONAVIRChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
SAMIDORPHANChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
SAQUINAVIRChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
SUNITINIBChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
TAMOXIFENChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
TRAMADOLChEMBLPhase 4 (approved)OPRD1, OPRK1, OPRM1
ASIMADOLINEChEMBLPhase 3OPRD1, OPRK1, OPRM1
ATICAPRANTChEMBLPhase 3OPRD1, OPRK1, OPRM1
CEBRANOPADOLChEMBLPhase 3OPRD1, OPRK1, OPRM1
NAVACAPRANTChEMBLPhase 3OPRD1, OPRK1, OPRM1
TRIMEBUTINEChEMBLPhase 3OPRD1, OPRK1, OPRM1
BREMAZOCINEChEMBLPhase 2OPRD1, OPRK1, OPRM1
CARFENTANILChEMBLPhase 2OPRD1, OPRK1, OPRM1

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

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Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot