Oxycodone

Summary

Oxycodone (CHEMBL656) is an approved small-molecule opioid analgesic (ATC N02AA05) that acts as a mu opioid receptor agonist, targeting OPRM1; approved for 2 indications (substance-related disorder and drug dependence), and in clinical trials for 19 other conditions.

At a glance

• Status: FDA-approved (also PMDA)
• Modality: Small molecule
• ATC class: N02AA05
• Targets: 1 (OPRM1)
• Indications: 36 conditions (top 5% of drugs corpus-wide)
• Clinical trials: 304
• Chemistry: 315.4 Da · C18H21NO4
• Target biology: 1 curated target implicated as cohort gene in 1 disease corpus-wide; indicated or in trials for 26 (0 on both)
• Competitive landscape: target OPRM1 is also targeted by 44 other curated drugs in the corpus

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL656
Name	Oxycodone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5284603
ChEBI	CHEBI:7852
ATC	N02AA05
Molecular formula	C18H21NO4
Molecular weight	315.4
InChIKey	BRUQQQPBMZOVGD-XFKAJCMBSA-N

SMILES: CN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)OC)O4)O

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

ChEBI definition: A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain.

Pharmacological roles (ChEBI): opioid analgesic, μ-opioid receptor agonist, antitussive.

Also known as: Dihydrone, IDS-NO-002, N02AA05, NSC-19043, Oxicodona, Oxicone, Oxycodone, Oxycodone cii, Pavinal, PF-00345439, Proladone, Pti 821

Parent form; salt/anhydrous children: CHEMBL1200890, CHEMBL3989826

Patent coverage: ubiquitous in the patent literature (a reference / commodity compound named in millions of filings — the raw count carries no drug-specific signal).

Targets

Targets

Mechanism of action (ChEMBL curated)

Target gene: OPRM1

Mechanism of action	Action type	Target	Target type
Mu opioid receptor agonist	AGONIST	Mu-type opioid receptor	SINGLE PROTEIN

Broader ChEMBL bioactivity targets: 10 (assay-derived screening hits — not curated targets; per-target potencies are in the ChEMBL bioactivities table below).

Bioactivity

ChEMBL activities: 20 potent at pChembl ≥ 5 of 24 total. Top 16 distinct by potency (10 = 0.1 nM, 6 = 1 µM):

Protein	UniProt	Gene	pChembl	Type	Value	Activity ID
Mu-type opioid receptor (Norway rat)	P33535		8.05	Ki	8.9 nM	CHEMBL_ACT_19067517
Mu-type opioid receptor	P35372	OPRM1	7.92	Ki	12 nM	CHEMBL_ACT_19055856
Mu-type opioid receptor	P35372	OPRM1	7.77	EC50	17 nM	CHEMBL_ACT_19055913
Mu-type opioid receptor (Norway rat)	P33535		7.6	EC50	25 nM	CHEMBL_ACT_19067695
Mu-type opioid receptor (Norway rat)	P33535		7.36	Ki	43.6 nM	CHEMBL_ACT_1485564
Mu-type opioid receptor	P35372	OPRM1	6.88	Ki	133.5 nM	CHEMBL_ACT_17744417
Mu-type opioid receptor (house mouse)	P42866		6.8	EC50	160 nM	CHEMBL_ACT_13437592
Mu-type opioid receptor	P35372	OPRM1	6.64	AC50	230 nM	CHEMBL_ACT_25147119
Kappa-type opioid receptor (domestic guinea pig)	P41144		6.49	Ki	325 nM	CHEMBL_ACT_19067551
Mu-type opioid receptor	P35372	OPRM1	6.32	EC50	478 nM	CHEMBL_ACT_17744471
Delta-type opioid receptor (Norway rat)	P33533		6.31	Ki	487 nM	CHEMBL_ACT_19067534
Mu-type opioid receptor	P35372	OPRM1	6.3	EC50	500 nM	CHEMBL_ACT_13437588
Delta-type opioid receptor (Norway rat)	P33533		5.96	Ki	1087 nM	CHEMBL_ACT_1485565
Kappa-type opioid receptor	P41145	OPRK1	5.7	AC50	2000 nM	CHEMBL_ACT_25129735
Kappa-type opioid receptor (Norway rat)	P34975		5.58	Ki	2658 nM	CHEMBL_ACT_1485566
Delta-type opioid receptor	P41143	OPRD1	5.4	EC50	4000 nM	CHEMBL_ACT_13437564

Target pathways

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

Predicted targets — Sugi Predict

This molecule is SureChEMBL compound SCHEMBL8386507 — see its predicted protein targets + similar patent compounds on Sugi Predict.

Indications & clinical

Indications

2 approved indications. FDA phase 4.

Indication	Phase	MONDO	EFO
substance-related disorder	4	MONDO:0002494
drug dependence	4	MONDO:0005303	EFO:0003890

19 diseases in clinical trials (phase 2–3, 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	3	MONDO:0005416	EFO:0004616
restless legs syndrome	3	MONDO:0005391	EFO:0004270
arthropathy	3	MONDO:0006816	EFO:1000999
nephrolithiasis	3	MONDO:0008171	EFO:0004253
diabetic neuropathy	3	MONDO:0006626
hypospadias	3	MONDO:0005345	EFO:0004209
osteoarthritis, hip	3	MONDO:0006629	EFO:1000786
female reproductive organ cancer	3	MONDO:0001416	EFO:1001331
osteoarthritis	3	MONDO:0005178
Parkinson disease	3	MONDO:0005180
neoplasm	3	MONDO:0005070
opiate dependence	2	MONDO:0005530	EFO:0005611
neuralgia	2	MONDO:0021667	EFO:0005762
sinusitis	2	MONDO:0005961	EFO:0007486
preeclampsia	2	MONDO:0005081	EFO:0000668
nutritional disorder	2	MONDO:0005137	EFO:0001069
spinal cord injury	2	MONDO:0043797	EFO:1001919
kidney cancer	2	MONDO:0002367
kidney neoplasm	2	MONDO:0021163	EFO:0003865

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

Regulatory approval & mechanism (DrugCentral)

Approved: FDA, PMDA. Curated mechanism: AGONIST · 1 MOA target of 3 total (P35372).

DrugCentral (CC BY-SA): authoritative regulatory-approval status + curated mechanism. The drug’s full target set is in Targets above.

Clinical trials

Total trials: 304.

Phase distribution

Phase	Trials
Phase 4	115
Not specified	53
Phase 3	50
Phase 1	36
Phase 2	30
Early Phase 1	11
Phase 1/2	5
Phase 2/3	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02044497	Phase 4	ACTIVE_NOT_RECRUITING	Population Pharmacokinetics and Pharmacogenomics of Oral Oxycodone in Pediatric Surgical Patients
NCT03054831	Phase 4	ACTIVE_NOT_RECRUITING	The Effect of General Anesthesia on Pharmacokinetics of Oxycodone in Pediatric
NCT03105518	Phase 4	ACTIVE_NOT_RECRUITING	Predictors of Postoperative Pain Following Oocyte Retrieval for Assisted Reproduction
NCT03759028	Phase 4	RECRUITING	Supracondylar Post-Operative Pain Study
NCT05488847	Phase 4	ACTIVE_NOT_RECRUITING	Opioid-Free Pain Protocol After Shoulder Arthroplasty
NCT06186141	Phase 4	RECRUITING	Nausea and Vomiting in Postoperative Paediatric Patients With Patient-Controlled Analgesia (PCA): Morphine vs Oxycodone
NCT06434233	Phase 4	RECRUITING	Opioid Use After Laparoscopic Salpingectomy
NCT06669650	Phase 4	ACTIVE_NOT_RECRUITING	Personalized Post-Operative Pain Management
NCT06897917	Phase 4	NOT_YET_RECRUITING	Real World Study of Oxycodone/Naloxone Sustained-Release Tablets (Mimeixin) for Patients With Severe Cancer Pain
NCT07153003	Phase 4	ENROLLING_BY_INVITATION	Efficacy And Safety Of Tramadol And Oxycodone Versus Oxycodone Monotherapy For Pain Control After Primary Total Knee And Total Hip Arthroplasty
NCT07219888	Phase 4	ENROLLING_BY_INVITATION	Comparison of Suzetrigine and Oxycodone for Postoperative Pain After Primary Total Knee Arthroplasty
NCT07435077	Phase 4	NOT_YET_RECRUITING	Examining Analgesic Synergy and Efficacy in Trauma Care
NCT07750639	Phase 4	ENROLLING_BY_INVITATION	Reducing Opioid Use After Upper Extremity Surgery: Testing Lower Prescriptions and Pill Quantity
NCT07773155	Phase 4	RECRUITING	Pain Control With Ketorolac and Nerve Block After Wrist and Hand Surgery
NCT07813026	Phase 4	RECRUITING	Abuse Potential of Gabapentin Taken Orally Concomitantly With Oxycodone Hydrochloride in Healthy, Non-Drug-Dependent, Recreational Opioid Users
NCT07820969	Phase 4	NOT_YET_RECRUITING	Post-op Analgesia of Nail Unit Procedures
NCT07821931	Phase 4	NOT_YET_RECRUITING	Suzetrigine in Tonsillectomy for Opioid-sparing Pain Management
NCT00027014	Phase 4	COMPLETED	Herb-Opioid Interactions
NCT00260260	Phase 4	COMPLETED	OXY-1: The Pharmacogenetics of Oxycodone Analgesia in Postoperative Pain
NCT00271973	Phase 4	COMPLETED	OXY-2: The Pharmacogenetics of Oxycodone Analgesia in Human Experimental Pain Models
NCT00369811	Phase 4	COMPLETED	Oxycodone vs Fentanyl for Pain Treatment After Laparoscopic Cholecystectomy
NCT00414453	Phase 4	TERMINATED	Trial of Analgesia With Lidocaine or Extended-release Oxycodone for Neuropathic Pain Treatment in Multiple Sclerosis
NCT00480142	Phase 4	UNKNOWN	Controlled Release of Oxycodone 10 mg In Pre-Medication For The Post Operative Analgesia In Elective Laparoscopic Bilateral Inguinal Hernia And Elective Laparoscopic Cholecystectomy
NCT00484718	Phase 4	TERMINATED	Measuring Gait And Self-Reported Pain In Patients With Osteoarthritis Of The Knee Using Placebo/Oxycodone/Celecoxib.
NCT00499460	Phase 4	COMPLETED	Effects of Garlic Supplements on Opioids in Healthy Volunteers
NCT00528177	Phase 4	COMPLETED	Morphine vs. Oxycodone for Postoperative Pain Management
NCT00681174	Phase 4	TERMINATED	Controlled-Release Oxycodone For Postoperative Analgesia After Video-Assisted Thoracic Surgery
NCT00784810	Phase 4	COMPLETED	A 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
NCT00916890	Phase 4	SUSPENDED	Prospective Study About Clinical and Pharmacogenetic Safety of Opioid Use for Chronic Pain
NCT00964808	Phase 4	COMPLETED	Norspan Versus Oxycontin as Postoperative Painkiller to Proximal Extracapsular Fractures of the Femur
NCT01083485	Phase 4	COMPLETED	OXN PR Compared to OXY PR in Subjects With Postoperative Pain After Knee Arthroplasty
NCT01109511	Phase 4	COMPLETED	A Comparison of Oxycodone/Naloxone and Oxycodone After Laparoscopic Hysterectomy
NCT01313780	Phase 4	COMPLETED	A Study to Evaluate Efficacy and Safety of Oxycodone/Naloxone Compared to OxyContin in Korean Cancer Patients
NCT01344720	Phase 4	UNKNOWN	Evaluation of the Efficacy and Tolerability of Etoricoxib Monotherapy Versus Combination Oxycodone-etoricoxib in Moderate to Severe Pain From Chronic Low Back Pain
NCT01374763	Phase 4	COMPLETED	A Comparison of PR Oxycodone/Naloxone and PR Oxycodone After Cardiac Surgery
NCT01381120	Phase 4	COMPLETED	Therapeutic Merit of Solifenacin in the Mitigation of Ureteral Stent-induced Pain and Lower Urinary Tract Symptoms
NCT01458015	Phase 4	TERMINATED	Tapentadol Versus Oxycodone - a Mechanism-based Treatment Approach in Neuropathic Pain
NCT01500317	Phase 4	COMPLETED	Comparison of the Effects of Tapentadol and Oxycodone on Gastrointestinal and Colonic Transit in Humans
NCT01502644	Phase 4	COMPLETED	Opioid Treatment for Chronic Low Back Pain and the Impact of Mood Symptoms
NCT01536301	Phase 4	COMPLETED	Oxycodone Versus Intravenous Morphine for Postoperative Analgesia After Hip Surgery
NCT01587274	Phase 4	COMPLETED	A Randomized Study of Three Medication Regimens for Acute Low Back Pain
NCT01672112	Phase 4	COMPLETED	Comparison of the Efficacy of Oral Oxycodone and Oral Codeine in the Treatment of Postcraniotomy Pain
NCT01719757	Phase 4	COMPLETED	PROspective Non-interventional Open laBEl Trial for TARGIN in Korean Patients With Cancer Pain
NCT01809106	Phase 4	COMPLETED	RCT Comparing the Analgesic Efficacy of 4 Therapeutic Strategies Based on 4 Different Major Opioids (Fentanyl, Oxycodone, Buprenorphine vs Morphine) in Cancer Patients With Moderate/Severe Pain, at the Moment of Starting 3rd Step of WHO Analgesic Ladder.
NCT01811186	Phase 4	COMPLETED	An Interventional Study to Compare the Efficacy and Tolerability With Targin® in Non-malignant Chronic Pain (GLORY)
NCT01811238	Phase 4	COMPLETED	An Interventional Study to Assess the Efficacy and Safety of Oxycodone/Naloxone in Korean Patients With Spinal Disorders
NCT01838616	Phase 4	COMPLETED	Tapentadol Prolonged Release (PR) Versus Oxycodone/Naloxone Prolonged Release in Severe Chronic Low Back Pain With a Neuropathic Component.
NCT01959204	Phase 4	COMPLETED	Evaluate The Pharmacokinetics and Safety Of Oxycodone Oral Solution In Pediatric and Adolescent Subjects
NCT02032927	Phase 4	WITHDRAWN	Treatment of Chronic Pain From Osteoarthritis
NCT02110719	Phase 4	COMPLETED	Decreasing Narcotics in Advanced Pelvic Surgery
NCT02160301	Phase 4	WITHDRAWN	Effect of a Multimodal Pain Regimen on Pain Control, Patient Satisfaction and Narcotic Use in Orthopaedic Trauma Patients
NCT02238340	Phase 4	COMPLETED	Oxycodone Extended-release in the Treatment of Perioperative Pain in Patients Undergoing Orthopaedic Surgery
NCT02295124	Phase 4	COMPLETED	Nausea in Patients Receiving Hydromorphone vs Oxycodone After Total Hip Replacement Surgery
NCT02391844	Phase 4	COMPLETED	Open-Label Study of Oxycodone/APAP to Treat Post-Operative Pain Following Arthroscopic Knee Surgery
NCT02426463	Phase 4	COMPLETED	Clinical Trial on Individual Characteristics Affecting Pain Drug Therapy in Neonates
NCT02449369	Phase 4	COMPLETED	Intra-Venous Acetaminophen and Muscle Relaxants After Total Knee
NCT02452437	Phase 4	UNKNOWN	Opioids in Chronic Kidney Disease Patients Undergoing Hemodialysis
NCT02454881	Phase 4	COMPLETED	Dose Response Study of Dexmedetomidine in Orthopaedic Spine Surgery Patients
NCT02455518	Phase 4	COMPLETED	Comparative Efficacy of 4 Oral Analgesics
NCT02464813	Phase 4	COMPLETED	Effect of Pregabalin on Immediate Post-operative and Longterm Pain
NCT02479165	Phase 4	COMPLETED	Pain Management After Cardiac Surgery - Opioids or NSAID
NCT02516059	Phase 4	COMPLETED	Early Postoperative Administration of Oxycodone +/- Naloxone and Duration of Epidural Analgesia
NCT02519023	Phase 4	COMPLETED	TAP vs Surgical Infiltration of Local Anesthetic in Laparoscopic and Robotic Hysterectomy
NCT02571881	Phase 4	UNKNOWN	Opioid Induced Bowel Dysfunction in Patients Undergoing Cesarean Section
NCT02573831	Phase 4	UNKNOWN	The Effect of Oxycodone to the Placental Circulation at Early Labour
NCT02573909	Phase 4	UNKNOWN	The Safety and Efficacy of Epidural Oxycodone
NCT02573922	Phase 4	COMPLETED	Opioid Induced Bowel Dysfunction in Patients Undergoing Spinal Surgery
NCT02703610	Phase 4	WITHDRAWN	Randomized Trial of Two Analgesics in Elderly ED Patients
NCT02728648	Phase 4	COMPLETED	Population Pharmacokinetic-Pharmacodynamic Study of Intravenous Oxycodone in Malaysian Population
NCT02936934	Phase 4	UNKNOWN	Comparison of Adverse Drug Reactions Associated for Oxycodone and Morphine in Postoperative Pain After Abdominal Hysterectomy
NCT02987920	Phase 4	TERMINATED	Dextromethorphan Use in Multimodal Analgesia Regimens for Total Knee Arthroplasty
NCT02994173	Phase 4	COMPLETED	Dose-response of Ketamine in Patient Controlled Analgesia in Orthopaedic Surgery Patients
NCT03019562	Phase 4	UNKNOWN	Oxycodone vs. Fentanyl in Early Postoperative Pain After Total Hip Replacement
NCT03121963	Phase 4	WITHDRAWN	Pain Management in Head and Neck Surgery Patients
NCT03145272	Phase 4	UNKNOWN	Population Pharmacokinetics and Pharmacogenomics of Oral Oxycodone in Thai Pediatric Surgical Patients
NCT03176121	Phase 4	COMPLETED	Study Evaluating Safety and Tolerability of Oxycodone in Patients With Moderate to Severe Cancer Pain
NCT03176199	Phase 4	COMPLETED	A Study to Compare the Titration Efficacy and Safety of Control-released Oxycodone and Immediate-released Oxycodone in Patients With Moderate to Severe Cancer Pain
NCT03202550	Phase 4	COMPLETED	Oral Sedation During Cervical Dilator Placement
NCT03314792	Phase 4	COMPLETED	Effects of Tapentadol Versus Oxycodone After Hysterectomy.
NCT03415555	Phase 4	COMPLETED	Postoperative Analgesia After Minithoracotomy
NCT03454217	Phase 4	COMPLETED	Impact of Tramadol and Oxycodone on Sleep Apnea
NCT03529331	Phase 4	WITHDRAWN	A Study Comparing Recurrent Use of MSIR, Percocet, and Vicodin at Discharge From the ED
NCT03592485	Phase 4	COMPLETED	ESP vs ESP With PECS
NCT03616639	Phase 4	TERMINATED	Neurotoxic Adverse Effects of Morphine and Oxycodone for Pain in Terminal Patients With Diminished Renal Function
NCT03859024	Phase 4	COMPLETED	Efficacy of Opioid-limiting Pain Management Protocol in Men Undergoing Urethroplasty
NCT03888144	Phase 4	COMPLETED	Study of Ketorolac Versus Opioid for Pain After Endoscopy
NCT04015908	Phase 4	COMPLETED	A Multimodal Analgesia Protocol Adapted for Ambulatory Surgery
NCT04110665	Phase 4	COMPLETED	Multimodal Analgesia Strategies After Major Shoulder Ambulatory Surgery
NCT04122443	Phase 4	COMPLETED	Acetaminophen (APAP) +/- Oxycodone
NCT04177342	Phase 4	UNKNOWN	Post Operative Pain Control of POEM Procedure
NCT04246697	Phase 4	COMPLETED	Multimodal Pain Study in Free Flap Patients
NCT04285853	Phase 4	COMPLETED	Are Opioids Needed After ACL Reconstruction
NCT04396587	Phase 4	COMPLETED	Non-analgesic Effects Produced by Equipotent Analgesic Doses of Sufentanil, Hydromorphone, and Oxycodone
NCT04399122	Phase 4	COMPLETED	Post-operative Pain Control After Photorefractive Keratectomy Comparing Acetaminophen/Codeine vs Acetaminophen/Oxycodone
NCT04726878	Phase 4	COMPLETED	ESP in Breast Surgery Due to Cancer
NCT04761302	Phase 4	COMPLETED	Postoperative Pain Management in Patients Undergoing Intramedullary Nail Fixation After Tibia and Femoral Fractures
NCT05053126	Phase 4	COMPLETED	Study Evaluating Abuse Potential of Lyrica® in Healthy Non-Drug Dependent Recreational Opioid Users
NCT05076110	Phase 4	COMPLETED	Nonopioid Pain Control Regimen After Arthroscopic Hip Procedures
NCT05142267	Phase 4	COMPLETED	Stress and Opioid Misuse Risk: The Role of Endogenous Opioid and Endocannabinoid Mechanisms
NCT05319756	Phase 4	COMPLETED	Study Evaluating the Abuse Potential of NEURONTIN® in Healthy Non-drug Dependent, Recreational Opioid Users

Clinical evidence (CIViC)

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

Pharmacology

MeSH pharmacological classification

Definition (MeSH): A semisynthetic derivative of CODEINE.

Pharmacological action: Analgesics, Opioid; Narcotics.

Broader MeSH heading: Codeine.

MeSH descriptor D010098 “Oxycodone” — exact-name match.

Pharmacogenomics

PharmGKB dosing guidelines — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

2 guidelines:

Guideline	Source	Gene(s)	Dosing?	Recommendation?
Annotation of CPIC Guideline for methadone, oxycodone and COMT, CYP2D6	CPIC	COMT;CYP2D6;OPRM1
Annotation of DPWG Guideline for oxycodone and CYP2D6	DPWG	CYP2D6

PGx drug labels — PharmGKB annotations of regulatory drug labels (FDA / EMA / PMDA / Health Canada (HCSC) / Swissmedic) that carry pharmacogenomic information, ordered by the label’s PGx level (Testing Required strongest → No Clinical PGx; — = no level recorded). Label guidance = the label gives PGx prescribing / dosing / alternate-drug information.

1 label annotations:

Agency	PGx level	Gene(s)	Label guidance	PharmGKB
Swissmedic	Actionable PGx	CYP2D6		PA166184177

Pharmacogenomic clinical annotations (21) — variant × gene × association × phenotype, ranked by PharmGKB evidence level (1 strongest → 4):

Gene	Variant	Association	Phenotype	Level
CYP2D6	CYP2D6*1, CYP2D6*1xN, CYP2D6*2, CYP2D6*2xN, CYP2D6*3, CYP2D6*4, CYP2D6*5, CYP2D6*6, CYP2D6*7	Metabolism/PK	Pain	2A
ABCB1	rs1045642	Dosage	Pain	3
COMT	rs4680	Efficacy		3
COMT	rs4680	Toxicity	Vomiting	3
COMT	rs4680	Toxicity	Erythema	3
CYP2D6	CYP2D6*1, CYP2D6*3, CYP2D6*4	Toxicity	Opioid-Related Disorders	3
CYP3A4	CYP3A4*1, CYP3A4*2, CYP3A4*3, CYP3A4*4, CYP3A4*5, CYP3A4*6, CYP3A4*7, CYP3A4*8, CYP3A4*9, CYP3A4*10, CYP3A4*11, CYP3A4*12, CYP3A4*13, CYP3A4*14, CYP3A4*15, CYP3A4*16, CYP3A4*17, CYP3A4*18, CYP3A4*19, CYP3A4*20, CYP3A4*21, CYP3A4*22, CYP3A4*23, CYP3A4*24, CYP3A4*26, CYP3A4*28, CYP3A4*29, CYP3A4*30, CYP3A4*31, CYP3A4*32, CYP3A4*33, CYP3A4*34	Metabolism/PK		3
CYP3A5	CYP3A5*1, CYP3A5*3	Dosage		3
OPRD1	rs581111	Efficacy		3
OPRM1	rs1799971	Efficacy		3
OPRM1	rs1799971	Dosage	Pain;Pain;Postoperative	3
OPRM1	rs1799971	Toxicity	Erythema	3
OPRM1	rs62436463	Toxicity	adverse events	3
RHBDF2	rs12948783	Efficacy	Neoplasms	3
SEPTIN3	rs739296	Toxicity	adverse events	3
UGT2B7	rs7439366	Efficacy	Pain	3
WBP2NL	rs739296	Toxicity	adverse events	3
COMT	rs4680	Toxicity	adverse events;Constipation;Delirium;Nausea;Pruritus;Somnolence;Urinary Retention	4
CYP2D6	CYP2D6*1, CYP2D6*2, CYP2D6*2xN, CYP2D6*3, CYP2D6*4, CYP2D6*6	Efficacy	Pain	4
CYP2D6	CYP2D6*1, CYP2D6*2, CYP2D6*2xN, CYP2D6*3, CYP2D6*4, CYP2D6*6	Toxicity	CNS depression;Drug Toxicity	4
OPRM1	rs1799971	Toxicity	adverse events;Constipation;Delirium;Nausea;Pruritus;Somnolence;Urinary Retention	4

Published variant annotations — per-publication pharmacogenomic findings for this drug (significant associations only), each from a curated PharmGKB literature annotation:

38 published findings:

Gene	Variant	Category	Finding	PMID
ABCB1	rs1045642	Dosage	Allele A is associated with decreased dose of buprenorphine, dihydrocodeine, fentanyl, hydromorphone, methadone, morphine, oxycodone, piritramide, tilidine or tramadol in people with Pain as compared to allele G.	PMID:19514130
ABCB1	rs1045642	Toxicity	Genotypes AA + AG is associated with increased likelihood of adverse events when treated with oxycodone in people with Pain and Neoplasms as compared to genotype GG.	PMID:37990344
COMT	rs4680	Efficacy	Genotypes AA + AG are associated with increased response to oxycodone as compared to genotype GG.	PMID:31493434
COMT	rs4680	Toxicity	Genotype GG is associated with increased likelihood of somnolence due to morphine or oxycodone in people with Lung Neoplasms as compared to genotypes AA + AG.	PMID:34871222
COMT	rs4680	Toxicity	Genotype AA is associated with increased likelihood of Vomiting when treated with naloxone and oxycodone in people with Pain as compared to genotypes AG + GG.	PMID:35710811
CYP2C19	CYP2C19 poor metabolizers and intermediate metabolizers	Metabolism/PK	CYP2C19 poor metabolizers and intermediate metabolizers are associated with decreased metabolism of oxycodone as compared to CYP2C19 normal metabolizer and ultrarapid metabolizer.	PMID:34480108
CYP2D6	CYP2D6 poor metabolizer	Efficacy	CYP2D6 poor metabolizer is associated with decreased clinical benefit to codeine, hydrocodone, oxycodone or tramadol in people with Pain as compared to CYP2D6 normal metabolizer.	PMID:40816377
CYP2D6	CYP2D6 poor metabolizer and intermediate metabolizer genotypes	Metabolism/PK	CYP2D6 poor metabolizer and intermediate metabolizer genotypes are associated with increased concentrations of noroxycodone or oxycodone as compared to CYP2D6 normal metabolizer and ultrarapid metabolizer genotypes.	PMID:33799050
CYP2D6	CYP2D6 poor metabolizer genotype	Metabolism/PK	CYP2D6 poor metabolizer is associated with increased exposure to oxycodone in healthy individuals as compared to CYP2D6 normal metabolizer.	PMID:20590587
CYP2D6	CYP2D6 poor metabolizer phenotype	Efficacy	CYP2D6 poor metabolizer is associated with decreased plasma oxymorphone/oxycodone ratio when treated with oxycodone in healthy individuals as compared to CYP2D6 normal metabolizer.	PMID:19281600
CYP2D6	CYP2D6 poor metabolizers and intermediate metabolizers	Efficacy	CYP2D6 intermediate metabolizer and poor metabolizer are associated with decreased response to codeine, fentanyl, hydrocodone, hydromorphone, methadone, morphine, oxycodone or tramadol in people with Neoplasms and Pain as compared to CYP2D6 normal metabolizer.	PMID:34423496
CYP2D6	CYP2D6 poor metabolizers and intermediate metabolizers	Metabolism/PK	CYP2D6 poor metabolizers and intermediate metabolizers are associated with decreased metabolism of oxycodone as compared to CYP2D6 normal metabolizer and ultrarapid metabolizer.	PMID:34480108
CYP2D6	CYP2D6 ultrarapid metabolizer	Dosage	CYP2D6 ultrarapid metabolizer is associated with increased dose of fentanyl, hydromorphone, opioids, oxycodone or tramadol in women with surgery as compared to CYP2D6 normal metabolizer and intermediate metabolizer and poor metabolizer.	PMID:38479169
CYP2D6	CYP2D6*1, CYP2D6*1xN, CYP2D6*2, CYP2D6*2xN, CYP2D6*3, CYP2D6*4, CYP2D6*5, CYP2D6*6, CYP2D6*7	Metabolism/PK	CYP2D6 *3/*4 + *4/*4 + *4/*5 + *4/*6 + *4/*7 (assigned as poor metabolizer phenotype) is associated with decreased Mean oxymorphone/oxycodone ratios when treated with oxycodone as compared to CYP2D6 *1/*1xN + *2/*2xN + *1xN/*2 (assigned as ultrarapid metabolizer phenotype) .	PMID:23555934
CYP2D6	CYP2D6*1, CYP2D6*2, CYP2D6*3, CYP2D6*4	Metabolism/PK	CYP2D6 *4/*4 + *3/*4 are associated with decreased serum concentrations of oxymorphone and noroxymorphone and oxymorphone/oxycodone ratios when treated with oxycodone in people with Neoplasms as compared to CYP2D6 *1/*1 + *2/*2.	PMID:21735164
CYP2D6	CYP2D6*1, CYP2D6*2, CYP2D6*4, CYP2D6*6	Metabolism/PK	CYP2D6 *4/*4 + *4/*6 are associated with decreased serum concentrations of oxymorphone and noroxymorphone and oxymorphone/oxycodone ratios when treated with oxycodone in people with Neoplasms as compared to CYP2D6 *1/*1 + *2/*2.	PMID:21735164
CYP2D6	CYP2D6*1, CYP2D6*3, CYP2D6*4	Metabolism/PK	CYP2D6 *4/*4 + *3/*4 is associated with mean plasma concentration of oxymorphone and lower mean oxymorphone/oxycodone ratio when treated with oxycodone as compared to CYP2D6 *1/*1.	PMID:19719813
CYP2D6	CYP2D6*1, CYP2D6*3, CYP2D6*4	Toxicity	CYP2D6 *3/*3 + *4/*4 are associated with decreased risk of Opioid-Related Disorders due to codeine, hydrocodone or oxycodone as compared to CYP2D6 *1/*1 + *1/*3 + *1/*4.	PMID:9352573
CYP2D6	CYP2D6*1, CYP2D6*3, CYP2D6*4, CYP2D6*5, CYP2D6*6, CYP2D6*7	Dosage	CYP2D6 *3/*4 + *4/*4 + *4/*5 + *4/*6 + *4/*7 (assigned as poor metabolizer phenotype) is associated with increased Oxycodone consumption up to the 12(th) hour in postoperative patients when treated with oxycodone as compared to CYP2D6 *1/*1 (assigned as normal metabolizer phenotype) .	PMID:23555934
CYP2D6	rs35742686	Efficacy	Allele DELT is associated with increased clinical benefit to hydrocodone or oxycodone in people with Pain as compared to allele T.	PMID:35102242
CYP3A4	CYP3A4*1, CYP3A4*2, CYP3A4*3, CYP3A4*4, CYP3A4*5, CYP3A4*7, CYP3A4*8, CYP3A4*9, CYP3A4*10, CYP3A4*11, CYP3A4*12, CYP3A4*13, CYP3A4*14, CYP3A4*15, CYP3A4*16, CYP3A4*18, CYP3A4*19, CYP3A4*23, CYP3A4*24, CYP3A4*28, CYP3A4*29, CYP3A4*31, CYP3A4*32, CYP3A4*33, CYP3A4*34	Metabolism/PK	CYP3A4 *2 + *3 + *4+ *5 + *7 + *8 + *9 + *10 + *11 + *12 + *13 + *14 + *15 + *16 + *18 + *19 + *23 + *24 + *28 + *29 + *31 + *32 + *33 + *34 are associated with decreased clearance of oxycodone as compared to CYP3A4 *1.	PMID:33393779
CYP3A4	CYP3A4*1, CYP3A4*22	Metabolism/PK	CYP3A4 *22 is associated with decreased metabolism of oxycodone as compared to CYP3A4 *1.	PMID:34480108
CYP3A4	CYP3A4*1, CYP3A4*6, CYP3A4*17, CYP3A4*20, CYP3A4*21, CYP3A4*26, CYP3A4*30	Metabolism/PK	CYP3A4 *6 + *17 + *20 + *21 + *26 + *30 are associated with decreased clearance of oxycodone as compared to CYP3A4 *1.	PMID:33393779
CYP3A5	CYP3A5*1, CYP3A5*3	Dosage	CYP3A5 *3/*3 is associated with increased dose of oxycodone in people with Neoplasms as compared to CYP3A5 *1/*1 + *1/*3.	PMID:21209234
MACROD2	rs76026520	Efficacy	Allele G is associated with increased clinical benefit to hydrocodone or oxycodone in people with Pain as compared to allele A.	PMID:35102242
OPRD1	rs581111	Efficacy	Genotypes AA + AG are associated with decreased response to oxycodone as compared to genotype GG.	PMID:31493434
OPRM1	rs1799971	Dosage	Genotype GG is associated with increased dose of oxycodone in women with Pain, Postoperative as compared to genotypes AA + AG.	PMID:25239082
OPRM1	rs1799971	Efficacy	Genotypes AG + GG are associated with decreased response to oxycodone in people with Pain, Postoperative as compared to genotype AA.	PMID:31773688
OPRM1	rs1799971	Toxicity	Genotype GG is associated with decreased likelihood of somnolence due to morphine or oxycodone in people with Lung Neoplasms as compared to genotypes AA + AG.	PMID:34871222
OPRM1	rs1799971	Toxicity	Genotype AA is associated with increased likelihood of Erythema when treated with naloxone and oxycodone in people with Pain as compared to genotypes AG + GG.	PMID:35710811
OPRM1	rs1799971	Efficacy	Genotypes AG + GG is associated with increased likelihood of Pain when treated with fentanyl, hydromorphone or oxycodone in people with Neoplasms as compared to genotype AA.	PMID:37757956
OPRM1	rs1799971	Dosage	Genotype AA is associated with increased dose of fentanyl, hydromorphone, opioids, oxycodone or tramadol in women with surgery as compared to genotype AG.	PMID:38479169
OPRM1	rs1799971	Toxicity	Genotype AA is associated with increased likelihood of Urinary Retention, Constipation, Nausea, Vomiting, Abdominal Pain, Exanthema, Wheezing or adverse events when treated with codeine, morphine or oxycodone in people with Neoplasms and Pain as compared to genotypes AG + GG.	PMID:40873551
OPRM1	rs62436463	Toxicity	Allele T is associated with decreased risk of adverse events when treated with codeine, hydrocodone, oxycodone or tramadol as compared to allele C.	PMID:34061827
RHBDF2	rs12948783	Efficacy	Genotypes AA + AG are associated with decreased efficact as measured by lower pain relief to opioids when treated with fentanyl, morphine, opioids or oxycodone in people with Neoplasms as compared to genotype GG.	PMID:21622719
SEPTIN3	rs739296	Toxicity	Allele A is associated with decreased risk of adverse events when treated with codeine, hydrocodone, oxycodone or tramadol as compared to allele G.	PMID:34061827
UGT2B7	rs7439366	Efficacy	Genotype TT is associated with decreased response to oxycodone in people with Neoplasms and Pain as compared to genotype CC.	PMID:29502154
WBP2NL	rs739296	Toxicity	Allele A is associated with decreased risk of adverse events when treated with codeine, hydrocodone, oxycodone or tramadol as compared to allele G.	PMID:34061827

PharmGKB pathway — curated pharmacokinetic / pharmacodynamic pathway diagrams for this drug:

• Oxycodone Pathway, Pharmacokinetics — pharmacokinetic

Adverse-event reports (FAERS)

107,591 reports across 2 FAERS drug-name records; 6,391 distinct MedDRA reactions.

openFDA FAERS — spontaneous post-marketing reports. Co-occurrence, not causation: reports are voluntary, unverified, and confounded by indication and reporting bias (the drug’s own indication often appears as a ‘reaction’). PRR is a disproportionality heuristic (reaction rate for this drug vs the FAERS background), NOT a risk estimate. Counts are pooled across the drug’s name records.

Most-reported events

Serious = reports flagged serious (death / life-threatening / hospitalisation / disability / other medically important).

50 reactions by report volume:

Reaction (MedDRA PT)	Reports	Serious	PRR
pain	11,190	9,511 (85%)	3.6×
fatigue	9,835	7,528 (77%)	2.5×
drug ineffective	9,266	6,480 (70%)	1.4×
nausea	8,376	5,861 (70%)	2.1×
off label use	6,906	5,648 (82%)	1.6×
diarrhoea	6,798	5,176 (76%)	2.1×
death	6,636	6,610 (100%)	1.5×
dyspnoea	6,434	5,817 (90%)	2.2×
rash	6,192	5,329 (86%)	2.8×
arthralgia	6,071	5,277 (87%)	2.9×
vomiting	6,055	5,004 (83%)	2.5×
headache	5,621	4,298 (76%)	1.8×
pyrexia	5,392	5,089 (94%)	3.1×
confusional state	5,107	4,887 (96%)	6.3×
drug dependence	5,014	4,988 (99%)	6.2×
peripheral swelling	4,868	4,450 (91%)	6.4×
weight increased	4,691	4,321 (92%)	4.2×
pruritus	4,689	3,971 (85%)	2.4×
joint swelling	4,606	4,385 (95%)	7.7×
asthenia	4,584	3,996 (87%)	2.4×
dizziness	4,190	3,319 (79%)	1.6×
drug abuse	4,102	4,077 (99%)	10.0×
nasopharyngitis	4,081	3,787 (93%)	4.4×
pneumonia	4,069	4,026 (99%)	2.5×
toxicity to various agents	4,056	4,005 (99%)	4.8×
malaise	4,038	3,279 (81%)	1.8×
abdominal discomfort	4,017	3,538 (88%)	4.8×
stomatitis	3,996	3,785 (95%)	13.7×
swelling	3,963	3,809 (96%)	8.6×
alopecia	3,890	3,452 (89%)	3.9×
hypersensitivity	3,870	3,664 (95%)	4.2×
infection	3,822	3,708 (97%)	5.3×
insomnia	3,799	3,145 (83%)	2.8×
rheumatoid arthritis	3,779	3,697 (98%)	6.7×
overdose	3,750	3,647 (97%)	3.4×
decreased appetite	3,675	2,972 (81%)	3.1×
sinusitis	3,602	3,413 (95%)	7.0×
lower respiratory tract infection	3,601	3,590 (100%)	16.8×
impaired healing	3,587	3,554 (99%)	23.8×
condition aggravated	3,574	3,264 (91%)	2.3×
infusion related reaction	3,569	3,523 (99%)	11.1×
blister	3,565	3,399 (95%)	13.2×
folliculitis	3,536	3,532 (100%)	101.2×
irritable bowel syndrome	3,488	3,469 (99%)	37.9×
fall	3,401	3,065 (90%)	2.0×
drug intolerance	3,386	3,235 (96%)	7.1×
anxiety	3,383	2,928 (87%)	2.3×
hepatic enzyme increased	3,377	3,287 (97%)	10.2×
pain in extremity	3,340	2,703 (81%)	2.2×
abdominal pain upper	3,322	2,789 (84%)	3.2×

Strongest disproportionality

Reactions over-reported for this drug vs the FAERS background (PRR), among those with ≥ 10 reports (a high PRR off a few reports is noise, not signal).

50 reactions by disproportionality:

Reaction (MedDRA PT)	Reports	Serious	PRR
foetal biophysical profile score abnormal	22	22 (100%)	467.8×
anti factor v antibody	13	13 (100%)	276.4×
hepatic enzyme	75	75 (100%)	227.8×
c-reactive protein	454	454 (100%)	197.0×
facet joint syndrome	1,434	1,434 (100%)	163.7×
deep vein thrombosis postoperative	807	807 (100%)	136.4×
duodenal ulcer perforation	2,931	2,930 (100%)	129.1×
red blood cell sedimentation rate	107	107 (100%)	119.8×
muscle injury	3,048	3,044 (100%)	114.8×
rheumatic fever	1,569	1,569 (100%)	109.1×
periodontal disease	37	37 (100%)	108.2×
sleep disorder due to general medical condition, insomnia type	2,261	2,255 (100%)	105.5×
anti-cyclic citrullinated peptide antibody positive	2,492	2,491 (100%)	104.7×
folliculitis	3,536	3,532 (100%)	101.2×
swollen joint count increased	1,052	1,052 (100%)	98.8×
swollen joint count	82	82 (100%)	97.5×
multiple lentigines syndrome	12	12 (100%)	88.3×
sleep disorder due to general medical condition, hypersomnia type	31	31 (100%)	87.2×
hypocholesterolaemia	94	94 (100%)	85.7×
sars-cov-2 sepsis	11	11 (100%)	81.0×
anti-cyclic citrullinated peptide antibody	194	194 (100%)	79.8×
adjustment disorder with depressed mood	582	581 (100%)	79.0×
salpingo-oophorectomy unilateral	31	31 (100%)	78.1×
helicobacter infection	2,918	2,916 (100%)	78.0×
lupus vulgaris	341	341 (100%)	78.0×
peripheral venous disease	1,068	1,067 (100%)	70.9×
dislocation of vertebra	567	567 (100%)	66.5×
subcutaneous drug absorption impaired	137	136 (99%)	65.4×
x-ray abnormal	427	426 (100%)	61.2×
c-reactive protein abnormal	1,527	1,527 (100%)	60.9×
pemphigus	2,910	2,909 (100%)	59.2×
foetal vascular malperfusion	11	11 (100%)	58.5×
schizencephaly	10	10 (100%)	56.3×
hand deformity	2,890	2,884 (100%)	55.1×
rheumatoid factor positive	1,234	1,234 (100%)	52.8×
narcotic bowel syndrome	31	31 (100%)	48.2×
retinitis	320	320 (100%)	46.1×
tender joint count	16	16 (100%)	44.4×
synovitis	3,168	3,165 (100%)	41.3×
pericarditis	2,875	2,873 (100%)	40.4×
intestinal sepsis	42	42 (100%)	38.6×
cerebral haemorrhage foetal	10	10 (100%)	38.3×
intestinal atony	10	10 (100%)	38.3×
irritable bowel syndrome	3,488	3,469 (99%)	37.9×
lip dry	1,440	1,422 (99%)	37.3×
opisthotonus	128	128 (100%)	36.9×
grip strength	37	37 (100%)	36.9×
breast cancer stage iii	1,024	1,024 (100%)	36.5×
appetite disorder	68	53 (78%)	35.6×
postmortem blood drug level abnormal	22	22 (100%)	34.5×

Related molecules

Related molecules

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