Oxycodegol

Summary

Oxycodegol (CHEMBL4297632) is a phase-3 clinical-stage small molecule targeting OPRD1 and OPRM1; indicated across 3 conditions including osteoarthritis, knee.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 2 (OPRD1, OPRM1)
• Indications: 3 conditions
• Clinical trials: 2
• Chemistry: 595.7 Da · C31H49NO10

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297632
Name	Oxycodegol
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	145993966
Molecular formula	C31H49NO10
Molecular weight	595.7
InChIKey	RQHILGKAOIGUHU-BUCMUWKRSA-N

SMILES: CN1CC[C@]23[C@@H]4[C@H](CCC2([C@H]1CC5=C3C(=C(C=C5)OC)O4)O)OCCOCCOCCOCCOCCOCCOC

IUPAC name: (4R,7S,7aR,12bS)-9-methoxy-7-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-3-methyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-4a-ol

Also known as: Loxicodegol, Nktr-181, NKTR-181, Oxicodegol, Oxycodegol, OXYCODEGOL

Parent form; salt/anhydrous children: CHEMBL4298154

Patent coverage: 23 distinct patent families (74 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
OPRD1	δ receptor	Agonist	5.38	0.2%	P41143
OPRM1	μ receptor	Agonist	6.63	0%	P35372

Bioactivity

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

Target pathways

Aggregated over 2 target gene(s): OPRD1, OPRM1.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Peptide ligand-binding receptors	2	OPRD1, OPRM1
G alpha (i) signalling events	2	OPRD1, OPRM1
Interleukin-4 and Interleukin-13 signaling	2	OPRD1, OPRM1
Opioid Signalling	1	OPRM1
G-protein activation	1	OPRM1
MECP2 regulates neuronal receptors and channels	1	OPRM1

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	2
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	2
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	2
phospholipase C-activating G protein-coupled receptor signaling pathway	2
neuropeptide signaling pathway	2
G protein-coupled opioid receptor signaling pathway	2
signal transduction	2
immune response	1
adult locomotory behavior	1
negative regulation of gene expression	1
negative regulation of protein-containing complex assembly	1
response to nicotine	1
eating behavior	1
response to ethanol	1
regulation of mitochondrial membrane potential	1

Indications & clinical

Indications

1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
osteoarthritis, knee	2	MONDO:0005416	EFO:0004616

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

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01619839	PHASE2	COMPLETED	A Phase 2 Study To Assess The Efficacy, Tolerability, And Safety OF NKTR-181 In Subjects With Chronic OA Knee Pain
NCT03802227	PHASE1	TERMINATED	A Study Using fMRI Imaging to Evaluate the Effect of NKTR-181 on Brain Activity in Healthy, Non-physically Dependent Recreational Opioid Users.

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

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.

449 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
Eluxadoline	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
TAFAMIDIS	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
ALFENTANIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ALVIMOPAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
AMIODARONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
AMLODIPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
AMOXAPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BENZTROPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BUPRENORPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BUTORPHANOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CANNABIDIOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CINNARIZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CODEINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ECONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
FENTANYL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
HYDROCODONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
HYDROMORPHONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LANSOPRAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LEVORPHANOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LOPERAMIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LOXAPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MEPERIDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
METHADONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
METHYLNALTREXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
METHYLNALTREXONE BROMIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MICONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MONTELUKAST	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MORPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NAFTOPIDIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALBUPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALDEMEDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALFURAFINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALMEFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALOXEGOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALOXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALTREXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NELFINAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OLICERIDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OXICONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OXYCODONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OXYMORPHONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PACLITAXEL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PALBOCICLIB	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PAROXETINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PASIREOTIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PENTAZOCINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PERHEXILINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PHENOXYBENZAMINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PIMOZIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RALOXIFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RIFAMPIN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RIFAXIMIN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RITONAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ROTIGOTINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
SAMIDORPHAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
SAQUINAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
SUNITINIB	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
TAMOXIFEN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
TELMISARTAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
TRAMADOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ZIMELDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ASIMADOLINE	ChEMBL	Phase 3	OPRD1, OPRM1
ATICAPRANT	ChEMBL	Phase 3	OPRD1, OPRM1
CEBRANOPADOL	ChEMBL	Phase 3	OPRD1, OPRM1
NAVACAPRANT	ChEMBL	Phase 3	OPRD1, OPRM1
TIANEPTINE	ChEMBL	Phase 3	OPRD1, OPRM1
TRIMEBUTINE	ChEMBL	Phase 3	OPRD1, OPRM1
AXELOPRAN	ChEMBL	Phase 2	OPRD1, OPRM1
AZD-7268	ChEMBL	Phase 2	OPRD1, OPRM1
BREMAZOCINE	ChEMBL	Phase 2	OPRD1, OPRM1
CARFENTANIL	ChEMBL	Phase 2	OPRD1, OPRM1
CLINAFLOXACIN	ChEMBL	Phase 2	OPRD1, OPRM1
CLOTHIAPINE	ChEMBL	Phase 2	OPRD1, OPRM1
CP-866087	ChEMBL	Phase 2	OPRD1, OPRM1
CYCLAZOCINE	ChEMBL	Phase 2	OPRD1, OPRM1
DIPRENORPHINE	ChEMBL	Phase 2	OPRD1, OPRM1
ETORPHINE	ChEMBL	Phase 2	OPRD1, OPRM1
FLUNARIZINE	ChEMBL	Phase 2	OPRD1, OPRM1
METAZOCINE	ChEMBL	Phase 2	OPRD1, OPRM1
NALORPHINE	ChEMBL	Phase 2	OPRD1, OPRM1
NIGULDIPINE	ChEMBL	Phase 2	OPRD1, OPRM1
ORGANON	ChEMBL	Phase 2	OPRD1, OPRM1
PENFLURIDOL	ChEMBL	Phase 2	OPRD1, OPRM1
SPIRADOLINE	ChEMBL	Phase 2	OPRD1, OPRM1
THIOPROPERAZINE	ChEMBL	Phase 2	OPRD1, OPRM1
Afatinib	PubChem	Approved	OPRD1, OPRM1
Apixaban	PubChem	Approved	OPRD1, OPRM1
Binimetinib	PubChem	Approved	OPRD1, OPRM1