Oxymorphone

Summary

Oxymorphone (CHEMBL963) is an approved small molecule (ATC N02AA11); indicated across 2 conditions.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02AA11
• Indications: 2 conditions
• Clinical trials: 6
• Chemistry: 301.34 Da · C17H19NO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL963
Name	Oxymorphone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5284604
ATC	N02AA11
Molecular formula	C17H19NO4
Molecular weight	301.34
InChIKey	UQCNKQCJZOAFTQ-ISWURRPUSA-N

SMILES: CN1CC[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-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one

Also known as: Dihydroxymorphinone, IDS-NO-003, NIH 10323, NSC-19045, Oximorfona, Oxycodone hydrochloride impurity, oxymorphone-, Oxymorphone, Oxymorphone cii, oxymorphone, OXYMORPHONE

Parent form; salt/anhydrous children: CHEMBL1200794

Patent coverage: 6,202 distinct patent families (25,955 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 25,954 (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: 13 (assay-derived). Sample: Opioid receptor, Opioid receptors; mu/kappa/delta, Opioid receptors; mu and 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, Delta-type opioid receptor.

Bioactivity

ChEMBL activities: 34 potent at pChembl ≥ 5 of 34 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P33533	10.89	IC50	0.01	nM	CHEMBL_ACT_909440
P33533	9.82	IC50	0.15	nM	CHEMBL_ACT_909441
P97266	9.27	Ki	0.54	nM	CHEMBL_ACT_6255730
P97266	9.11	Ki	0.78	nM	CHEMBL_ACT_480978
P33535	9.01	Ki	0.97	nM	CHEMBL_ACT_1506907
P33533	9	EC50	1	nM	CHEMBL_ACT_14602737
P97266	8.85	IC50	1.4	nM	CHEMBL_ACT_403537
OPRM1	8.75	Ki	1.79	nM	CHEMBL_ACT_18144514
P32300	8.33	Ki	4.68	nM	CHEMBL_ACT_12051644
P42866	8.3	Ki	5.01	nM	CHEMBL_ACT_12051635
OPRM1	8.11	EC50	7.8	nM	CHEMBL_ACT_18144554
P97266	7.82	Ki	15	nM	CHEMBL_ACT_931753
P33535	7.76	Ki	17.4	nM	CHEMBL_ACT_584189
P33535	7.64	Ki	23.1	nM	CHEMBL_ACT_584190
OPRK1	7.6	Ki	25.3	nM	CHEMBL_ACT_18144530
P33535	7.58	Ki	26.2	nM	CHEMBL_ACT_584191
OPRD1	7.35	IC50	45	nM	CHEMBL_ACT_403539
OPRD1	7.3	Ki	50	nM	CHEMBL_ACT_480979
P41144	7.24	Ki	57.6	nM	CHEMBL_ACT_6255750
P41144	7.21	Ki	61.6	nM	CHEMBL_ACT_1506909
OPRD1	7.16	Ki	70	nM	CHEMBL_ACT_18144522
P33533	7.09	Ki	80.5	nM	CHEMBL_ACT_1506908
OPRM1	7.05	IC50	90	nM	CHEMBL_ACT_403536
P34975	7.02	Ki	95	nM	CHEMBL_ACT_584196
P41144	6.86	Ki	137	nM	CHEMBL_ACT_480980
OPRD1	6.84	Ki	145	nM	CHEMBL_ACT_931755
P34975	6.68	Ki	208	nM	CHEMBL_ACT_584194
P34975	6.36	Ki	435	nM	CHEMBL_ACT_584195
P32300	6.29	Ki	512.9	nM	CHEMBL_ACT_12051617
P32300	6.21	Ki	610	nM	CHEMBL_ACT_584193

Target pathways

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

Indications & clinical

Indications

2 indications (1 at ChEMBL trial phase 4).

The 2 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 6.

Phase distribution

Phase	Trials
PHASE1	2
Not specified	2
PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04681027	PHASE3	SUSPENDED	Safety, Tolerability, Effectiveness, and Pharmacokinetic Data in Opioid-experienced Children
NCT00857428	PHASE1	COMPLETED	Bioavailability of Oxymorphone Hydrochloride 40 mg Extended Release Tablets Under Fasted Conditions
NCT01210638	PHASE1	COMPLETED	Bioequivalency Study of Oxymorphone Hydrochloride 10 mg Tablets Under Fasted Conditions
NCT03579446	EARLY_PHASE1	TERMINATED	Levorphanol as a Second Line Opioid in Reducing Pain in Patients With Cancer
NCT00580294	Not specified	COMPLETED	A Pilot Study of Switching From One Pain Medication to Another (Opioid Rotation)
NCT02625181	Not specified	COMPLETED	Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 4 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).