Buprenorphine

Summary

Buprenorphine (CHEMBL511142) is an approved small molecule (ATC N07BC01) targeting OPRK1 and OPRM1; indicated across 28 conditions including opiate dependence and drug dependence.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N07BC01 (+2 more)
• Targets: 2 (OPRK1, OPRM1)
• Indications: 28 conditions
• Clinical trials: 335
• Chemistry: 467.6 Da · C29H41NO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL511142
Name	Buprenorphine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	9848990
ATC	N07BC01, N07BC51, N02AE01
Molecular formula	C29H41NO4
Molecular weight	467.6
InChIKey	RMRJXGBAOAMLHD-CTAPUXPBSA-N

SMILES: C[C@]([C@H]1C[C@@]23CC[C@]1([C@H]4[C@@]25CCN([C@@H]3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)(C(C)(C)C)O

IUPAC name: (1S,2S,6R,14R,15S,16R)-5-(cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11-trien-11-ol

Also known as: Brixadi, Bupeaze, Buplast, Buprenorfina, Buprenorphin, Buprenorphine, BUPRENORPHINE COMPONENT OF ALKS-5461, Butec, Butrans, Buvidal, Hapoctasin, Panitaz

Parent form; salt/anhydrous children: CHEMBL2368861

Patent coverage: 13,293 distinct patent families (51,203 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 50,716 (99%) 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
OPRK1	κ receptor	Antagonist	10.2	0%	P41145
OPRM1	μ receptor	Partial agonist	8.8	0%	P35372

Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Nociceptin receptor, Opioid receptor, Mu-type opioid receptor, Delta-type opioid receptor, Kappa-type opioid receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Delta-type opioid receptor, Mu-type opioid receptor, Mu-type opioid receptor, Kappa-type opioid receptor, Mu-type opioid receptor.

Bioactivity

ChEMBL activities: 83 potent at pChembl ≥ 5 of 83 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
OPRK1	10.4	Ki	0.04	nM	CHEMBL_ACT_17762300
OPRK1	10.4	Ki	0.04	nM	CHEMBL_ACT_18686314
OPRK1	10.17	Ki	0.07	nM	CHEMBL_ACT_12699675
OPRK1	10.15	Ki	0.07	nM	CHEMBL_ACT_14716292
OPRK1	10.05	Ki	0.09	nM	CHEMBL_ACT_14670624
OPRM1	10.05	Ki	0.09	nM	CHEMBL_ACT_14716285
OPRK1	10.05	Ki	0.09	nM	CHEMBL_ACT_15617281
OPRM1	9.96	EC50	0.11	nM	CHEMBL_ACT_2263730
P33535	9.89	Ki	0.13	nM	CHEMBL_ACT_14670676
P33535	9.89	Ki	0.13	nM	CHEMBL_ACT_15617264
OPRK1	9.74	EC50	0.18	nM	CHEMBL_ACT_2263728
P33535	9.72	Ki	0.19	nM	CHEMBL_ACT_12699714
OPRM1	9.68	Ki	0.21	nM	CHEMBL_ACT_2263733
P33535	9.57	EC50	0.27	nM	CHEMBL_ACT_12699623
OPRM1	9.52	Ki	0.3	nM	CHEMBL_ACT_17762286
OPRM1	9.52	EC50	0.3	nM	CHEMBL_ACT_27465575
OPRM1	9.52	EC50	0.3	nM	CHEMBL_ACT_27578909
OPRM1	9.52	EC50	0.3	nM	CHEMBL_ACT_28079213
P97266	9.4	Ki	0.4	nM	CHEMBL_ACT_12699642
P33533	9.39	IC50	0.41	nM	CHEMBL_ACT_261009
OPRM1	9.39	IC50	0.41	nM	CHEMBL_ACT_26618459
OPRM1	9.39	Ki	0.41	nM	CHEMBL_ACT_27465572
OPRM1	9.39	Ki	0.41	nM	CHEMBL_ACT_27578906
OPRM1	9.39	Ki	0.41	nM	CHEMBL_ACT_28072799
OPRM1	9.39	Ki	0.41	nM	CHEMBL_ACT_28079210
OPRM1	9.39	Ki	0.41	nM	CHEMBL_ACT_28876814
P33533	9.36	IC50	0.44	nM	CHEMBL_ACT_261010
OPRM1	9.35	EC50	0.45	nM	CHEMBL_ACT_17762291
OPRM1	9.35	IC50	0.45	nM	CHEMBL_ACT_27578912
OPRM1	9.35	IC50	0.45	nM	CHEMBL_ACT_28079216
OPRM1	9.35	IC50	0.45	nM	CHEMBL_ACT_28876817
P33533	9.32	Ki	0.48	nM	CHEMBL_ACT_14670712
P33533	9.32	Ki	0.48	nM	CHEMBL_ACT_15617315
P41144	9.3	Ki	0.5	nM	CHEMBL_ACT_12699637
OPRK1	9.25	EC50	0.56	nM	CHEMBL_ACT_17762309
OPRM1	9.23	IC50	0.59	nM	CHEMBL_ACT_2263729
OPRK1	9.21	Ki	0.62	nM	CHEMBL_ACT_2263731
P33535	9.15	EC50	0.7	nM	CHEMBL_ACT_15617170
OPRK1	9.1	Ki	0.8	nM	CHEMBL_ACT_1071833
OPRK1	9.1	Ki	0.8	nM	CHEMBL_ACT_1928235
OPRD1	9.07	EC50	0.85	nM	CHEMBL_ACT_25868788
OPRD1	8.94	Ki	1.15	nM	CHEMBL_ACT_14716289
P97266	8.89	Ki	1.3	nM	CHEMBL_ACT_12160369
P97266	8.89	Ki	1.3	nM	CHEMBL_ACT_134336
OPRM1	8.82	Ki	1.5	nM	CHEMBL_ACT_1071832
P41144	8.82	Ki	1.5	nM	CHEMBL_ACT_12160351
P41144	8.82	Ki	1.5	nM	CHEMBL_ACT_134338
OPRM1	8.82	Ki	1.5	nM	CHEMBL_ACT_14670735
OPRM1	8.82	Ki	1.5	nM	CHEMBL_ACT_1928211
OPRM1	8.82	Ki	1.5	nM	CHEMBL_ACT_6377345
OPRD1	8.8	Ki	1.6	nM	CHEMBL_ACT_134337
OPRM1	8.8	Ki	1.58	nM	CHEMBL_ACT_16427796
P41144	8.7	IC50	2	nM	CHEMBL_ACT_12696764
OPRM1	8.7	EC50	2	nM	CHEMBL_ACT_13515461
OPRM1	8.64	EC50	2.3	nM	CHEMBL_ACT_1071835
OPRM1	8.64	EC50	2.3	nM	CHEMBL_ACT_134343
OPRM1	8.62	EC50	2.37	nM	CHEMBL_ACT_25868680
OPRK1	8.6	Ki	2.5	nM	CHEMBL_ACT_14670738
OPRK1	8.6	Ki	2.5	nM	CHEMBL_ACT_6378302
OPRD1	8.54	Ki	2.9	nM	CHEMBL_ACT_2263732
OPRK1	8.5	IC50	3.16	nM	CHEMBL_ACT_25868879
P42866	8.44	EC50	3.6	nM	CHEMBL_ACT_15172127
OPRK1	8.44	EC50	3.62	nM	CHEMBL_ACT_25868792
OPRD1	8.35	Ki	4.5	nM	CHEMBL_ACT_1071834
OPRD1	8.35	Ki	4.5	nM	CHEMBL_ACT_1928260
OPRD1	8.21	Ki	6.1	nM	CHEMBL_ACT_14670723
OPRD1	8.21	Ki	6.1	nM	CHEMBL_ACT_6378289
P41144	8.09	IC50	8.1	nM	CHEMBL_ACT_12696808
OPRM1	7.99	EC50	10.2	nM	CHEMBL_ACT_14670741
OPRM1	7.99	EC50	10.2	nM	CHEMBL_ACT_6378341
OPRM1	7.83	EC50	14.8	nM	CHEMBL_ACT_1928604
OPRK1	7.82	IC50	15	nM	CHEMBL_ACT_2263727
P41144	7.68	EC50	21	nM	CHEMBL_ACT_12160319
P97266	7.68	EC50	21	nM	CHEMBL_ACT_12160321
OPRL1	7.27	EC50	53.43	nM	CHEMBL_ACT_25868794
OPRL1	7.11	Ki	77	nM	CHEMBL_ACT_14670753
OPRL1	7.11	Ki	77.4	nM	CHEMBL_ACT_6378315
OPRL1	6.94	EC50	116	nM	CHEMBL_ACT_6378355
OPRL1	6.67	Ki	212	nM	CHEMBL_ACT_14670752
OPRL1	6.67	Ki	212	nM	CHEMBL_ACT_15617298
OPRL1	5.83	EC50	1480	nM	CHEMBL_ACT_15617250
KCNH2	5.12	IC50	7586	nM	CHEMBL_ACT_1523707
KCNH2	5.1	IC50	7943	nM	CHEMBL_ACT_5219056

Target pathways

Aggregated over 2 target gene(s): OPRK1, OPRM1.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Peptide ligand-binding receptors	2	OPRK1, OPRM1
G alpha (i) signalling events	2	OPRK1, OPRM1
MECP2 regulates neuronal receptors and channels	2	OPRK1, OPRM1
Opioid Signalling	1	OPRM1
G-protein activation	1	OPRM1
Interleukin-4 and Interleukin-13 signaling	1	OPRM1

Dominant GO biological processes

GO term	Targets
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	2
phospholipase C-activating G protein-coupled receptor signaling pathway	2
neuropeptide signaling pathway	2
sensory perception	2
sensory perception of pain	2
G protein-coupled opioid receptor signaling pathway	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
immune response	1
chemical synaptic transmission	1
locomotory behavior	1
adenylate cyclase-inhibiting opioid receptor signaling pathway	1
response to insulin	1
positive regulation of dopamine secretion	1
negative regulation of luteinizing hormone secretion	1

Indications & clinical

Indications

3 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
opiate dependence	4	MONDO:0005530	EFO:0005611
drug dependence	4	MONDO:0005303	EFO:0003890
substance-related disorder	4	MONDO:0002494	MONDO:0002491

17 diseases 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
heroin dependence	3	MONDO:0005367	EFO:0004240
neonatal abstinence syndrome	3	MONDO:0005566	EFO:0005799
HIV infectious disease	3	MONDO:0005109	EFO:0000764
cocaine dependence	3	MONDO:0005186	EFO:0002610
morphine dependence	3	MONDO:0005531	EFO:0005612
substance withdrawal syndrome	3	MONDO:0005567	EFO:0005800
neuralgia	3	MONDO:0021667	EFO:0005762
intervertebral disk degenerative disorder	3	MONDO:0011385	HP:0008419
major depressive disorder	3	MONDO:0002009	MONDO:0002009
depressive disorder	3	MONDO:0002050	MONDO:0002050
osteoarthritis	3	MONDO:0005178	MONDO:0005178
rotator cuff syndrome	2	MONDO:0007028	EFO:1001250
post-traumatic stress disorder	2	MONDO:0005146	EFO:0001358
head and neck squamous cell carcinoma	2	MONDO:0010150	EFO:0000181
methamphetamine dependence	2	MONDO:0005419	EFO:0004701
sickle cell disease	2	MONDO:0011382	MONDO:0011382
hepatitis C virus infection	1	MONDO:0005231	EFO:0003047

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

Clinical trials

Total trials: 335.

Phase distribution

Phase	Trials
PHASE2	76
PHASE4	72
PHASE3	67
Not specified	45
PHASE1	43
PHASE2/PHASE3	14
PHASE1/PHASE2	13
EARLY_PHASE1	5

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03396276	PHASE4	ENROLLING_BY_INVITATION	Houston Emergency Opioid Engagement System
NCT04375033	PHASE4	RECRUITING	A Study Comparing Oral Buprenorphine and Injectable Buprenorphine for the Treatment of Opioid Use Disorder
NCT04811014	PHASE4	RECRUITING	Young Houston Emergency Opioid Engagement System
NCT05944952	PHASE4	ACTIVE_NOT_RECRUITING	Low-dose Versus a High-dose Sublingual Buprenorphine Induction
NCT06133114	PHASE4	RECRUITING	Psychopharmacological Treatment of Emotional Distress
NCT06323824	PHASE4	RECRUITING	Office-based Methadone Versus Buprenorphine to Address Retention in Medication for Opioid Use Disorder Treatment.
NCT06574009	PHASE4	RECRUITING	Better Options for Chronic Cancer Pain
NCT06742554	PHASE4	ACTIVE_NOT_RECRUITING	Comparative Efficacy of Buprenorphine Transdermal Patch Versus Tramadol in Postoperative Analgesia for Shoulder Arthroscopy
NCT06854029	PHASE4	NOT_YET_RECRUITING	NOTRE: Optimizing Long-Acting Pre-Exposure Prophylaxis and Medications for Opioid Use Disorder Interventions in Carceral Settings
NCT06880718	PHASE4	RECRUITING	Injectable Buprenorphine in Prison: A Preference Trial
NCT06949826	PHASE4	RECRUITING	Buprenorphine as a Post-operative Analgesic in Opioid-Naive Patients After Ankle Fracture Surgery
NCT07176351	PHASE4	NOT_YET_RECRUITING	Acceptability and Feasibility of Extended-Release Subcutaneous Buprenorphine on a Mobile Pharmacy Clinic
NCT07435077	PHASE4	NOT_YET_RECRUITING	Examining Analgesic Synergy and Efficacy in Trauma Care
NCT07469501	PHASE4	NOT_YET_RECRUITING	Comparing Outpatient Treatment Retention Among Individuals Using Fentanyl Randomized to Low-dose and Direct-to-inject Buprenorphine Initiation
NCT07485335	PHASE4	NOT_YET_RECRUITING	A Bundled Intervention to End Opioid Overdoses
NCT00007527	PHASE4	COMPLETED	Determine the Safety of a Sublingual Tablet Formulation of Buprenorphine and Naloxone by Extending the Combination Tablet Availability to Physicians in Office-Based Practice
NCT00015340	PHASE4	COMPLETED	Buprenorphine/Naloxone in the Treatment of Heroin Dependence - 14
NCT00124358	PHASE4	UNKNOWN	Buprenorphine and Integrated HIV Care Evaluation
NCT00279565	PHASE4	TERMINATED	Buprenorphine Versus Methadone Maintenance in Hepatitis C Patients Receiving Peg-Intron and Rebetol (Study P04279)(TERMINATED)
NCT00310934	PHASE4	COMPLETED	A Stepwise Strategy Utilizing Buprenorphine and Methadone
NCT00315341	PHASE4	COMPLETED	Starting Treatment With Agonist Replacement Therapies (START)
NCT00324038	PHASE4	COMPLETED	Buprenorphine in the Treatment of Osteoarthritis (OA) in the Elderly
NCT00367874	PHASE4	COMPLETED	Treatment of Polydrug-Using Opiate Dependents During Withdrawal
NCT00426647	PHASE4	COMPLETED	Norspan® Patches Versus Tramadol in Subjects With Chronic, Moderate to Severe Osteoarthritis Pain in the Hip Knee and/or Lumbar Spine
NCT00552578	PHASE4	TERMINATED	Buprenorphine as a Treatment in Opiate Dependent Pain Patients
NCT00605033	PHASE4	COMPLETED	A Randomized Acceptability and Safety Study of the Transfer From Subutex to Suboxone in Opioid- Dependent Subjects (Study P04843)(COMPLETED)
NCT00684073	PHASE4	COMPLETED	Preference for Subutex® (Buprenorphine) Versus Suboxone® (Buprenorphine/Naloxone) in Opioid Dependent Patients on Subutex® (Study P05094)(COMPLETED)
NCT00763958	PHASE4	COMPLETED	Relapse Prevention to Reduce HIV Among Women Prisoners
NCT00879996	PHASE4	COMPLETED	Buprenorphine and Methadone for Opioid Dependent Chronic Pain Patients
NCT00901875	PHASE4	COMPLETED	Multicentre Trial of Suboxone in Opiate-dependent Subjects in Taiwan
NCT00916890	PHASE4	SUSPENDED	Prospective Study About Clinical and Pharmacogenetic Safety of Opioid Use for Chronic Pain
NCT00949299	PHASE4	TERMINATED	Effects of Buprenorphine on Ulnar Nerve Motor Block
NCT00955162	PHASE4	COMPLETED	Effectiveness of Buprenorphine/Naloxone in Reducing Intravenous Buprenorphine Misuse in France (RIME)
NCT00964808	PHASE4	COMPLETED	Norspan Versus Oxycontin as Postoperative Painkiller to Proximal Extracapsular Fractures of the Femur
NCT01015066	PHASE4	WITHDRAWN	Comparison of Buprenorphine/Naloxone With Naltrexone in Opioid Dependent Adolescents
NCT01276431	PHASE4	COMPLETED	Norspan Efficacy and Safety Among Elderly Subjects
NCT01298297	PHASE4	COMPLETED	Efficacy of Buprenorphine for Treatment of Acute Pain
NCT01546701	PHASE4	COMPLETED	Buprenorphine in Acute Renal Colic Pain Management
NCT01559454	PHASE4	COMPLETED	Buprenorphine and Methadone for Opioid-dependent Chronic Back Pain Patients
NCT01733693	PHASE4	COMPLETED	Neurocognitive Effects of Opiate Agonist Treatment
NCT01809106	PHASE4	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.
NCT01818700	PHASE4	COMPLETED	An Interventional Study to Assess the Efficacy and Safety of Buprenorphine in Korean Patients With Spinal Disorders
NCT01841931	PHASE4	TERMINATED	Buprenorphine Treatment: A Safe Alternative for Opioid Dependent Pain Patients
NCT01843023	PHASE4	COMPLETED	Extended Release Naltrexone for Opioid-Dependent Youth
NCT01846455	PHASE4	COMPLETED	Single Dose Pharmacokinetics of Suboxone Study in Hepatic Impaired Subjects
NCT01854489	PHASE4	COMPLETED	Effects of Rifampicin on the Pharmacokinetics and Pharmacodynamics of Sublingual and Intravenous Buprenorphine
NCT01875848	PHASE4	TERMINATED	Buprenorphine vs. Opioid Dose Escalation Among Patients With Chronic Pain
NCT01936857	PHASE4	COMPLETED	Buprenorphine to Improve HIV Care Engagement and Outcomes
NCT01961271	PHASE4	COMPLETED	Evaluation Of Efficacy And Safety Of Norspan In Moderate To Severe Pain Due To Osteoarthritis, Rheumatoid Arthritis, Joint/Muscle Pain
NCT01983111	PHASE4	COMPLETED	Compare the Efficacy and Safety of Norspan to Tramadol/Acetaminophen With Prolonged Postoperative Pain (PASSION)
NCT02162121	PHASE4	COMPLETED	Stimulating Catheter for Lumbar Plexus Block: Better Postoperative Analgesia?
NCT02267057	PHASE4	COMPLETED	Efficacy of Pain Treatment on Depression in Patients With Dementia
NCT02416804	PHASE4	COMPLETED	Postoperative Analgesia With Buprenorphine for Postoperative Pain Control and Quality of Life After Spinal Surgery
NCT02519387	PHASE4	COMPLETED	Efficacy and Safety of Buprenorphine Transdermal Patch in Non-cancer Pain of Moderate Intensity
NCT02575664	PHASE4	COMPLETED	Effects of Low Dose Buprenorphine on Recovery After Hip or Knee Arthroplasty
NCT03174067	PHASE4	COMPLETED	Buprenorphine in the Emergency Department
NCT03266445	PHASE4	UNKNOWN	Effect of Buprenorphine/Naloxone Continuation on Pain Control and Opioid Use
NCT03740243	PHASE4	WITHDRAWN	Buprenorphine vs Buprenorphine/Naloxone on the Effects of Maternal Symptomatology
NCT03908437	PHASE4	COMPLETED	Rapid Initiation of Drug Treatment Engagement
NCT03993392	PHASE4	COMPLETED	SUBLOCADE Rapid Initiation Study
NCT04060654	PHASE4	COMPLETED	SUBLOCADE Rapid Initiation Extension Study
NCT04091009	PHASE4	WITHDRAWN	Effect 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
NCT04212065	PHASE4	WITHDRAWN	Long Acting Subcutaneous vs Short Acting Sublingual Buprenorphine in Pregnant and Lactating Women
NCT04234516	PHASE4	WITHDRAWN	Anti-suicidal Effects of Buprenorphine in Opioid Use Disorder
NCT04254081	PHASE4	COMPLETED	Addition of Buprenorphine to Paracervical Block for Pain Control During Osmotic Dilator Insertion
NCT04276259	PHASE4	COMPLETED	Rapid Antidepressant Improvement Secondary to Excitatory Brain Responses
NCT04283500	PHASE4	COMPLETED	Buprenorphine Loading in the Emergency Department
NCT04771689	PHASE4	WITHDRAWN	Buprenorphine/Naloxone Micro-Dosing for Postoperative Pain Management in Opioid-Tolerant Patients
NCT04981678	PHASE4	TERMINATED	The Effect of Buprenorphine Continuation for Patients With Opioid Use Disorder
NCT04995029	PHASE4	COMPLETED	Buprenorphine Extended-Release Subcutaneous Injection (RBP-6000) in High-risk Users
NCT05042648	PHASE4	UNKNOWN	Role of Preoperative Transdermal Buprenorphine Patch in Reducing Postoperative Opioids Consumption in Patients Undergoing Total Knee Arthroplasties - A Randomised Controlled Trial.
NCT05644587	PHASE4	TERMINATED	Novel Induction to Buprenorphine/Naloxone
NCT03646058	PHASE3	RECRUITING	Add-on Buprenorphine at Analgesic Doses for the Treatment of Severe Suicidal Ideas During a Major Depressive Episode
NCT04893525	PHASE2/PHASE3	RECRUITING	Evaluating Buprenorphine/Naloxone Microdosing vs. Standard Dosing in Emergency Departments
NCT05011266	PHASE2/PHASE3	RECRUITING	Efficacy of Buprenorphine and XR-Naltrexone Combination for Relapse Prevention in Opioid Use Disorder
NCT06316830	PHASE2/PHASE3	RECRUITING	Identifying Optimal Buprenorphine Dosing for Opioid Use Disorder Treatment and Prevention of Overdose
NCT06494904	PHASE3	RECRUITING	Standard Versus High Dose ED-Initiated Buprenorphine Induction
NCT00000205	PHASE3	COMPLETED	Buprenorphine Maintenance Protocol - 1
NCT00000207	PHASE3	COMPLETED	Multicenter Clinical Trial of Buprenorphine - 3
NCT00000216	PHASE3	COMPLETED	Buprenorphine Maintenance for Cocaine Abusing Opioid Addicts - 1
NCT00000302	PHASE3	COMPLETED	Study Comparing Liquid and Tablet Buprenorphine Formulations - 5
NCT00000311	PHASE3	COMPLETED	Combining Behavioral Treatment With Agonist Maintenance - 1
NCT00015171	PHASE3	COMPLETED	Buprenorphine and Naloxone for the Treatment of Opiate Dependence - 1
NCT00032955	PHASE3	COMPLETED	Buprenorphine/Naloxone Versus Clonidine for Inpatient Opiate Detoxification - 1
NCT00032968	PHASE3	COMPLETED	Buprenorphine/Naloxone Versus Clonidine for Outpatient Opiate Detoxification - 1
NCT00078117	PHASE3	COMPLETED	Suboxone: (Buprenorphine/Naloxone) Comparison of Two Taper Schedules - 1
NCT00078130	PHASE3	COMPLETED	Buprenorphine/Naloxone - Facilitated Rehabilitation for Opioid Dependent Adolescents - 1
NCT00270257	PHASE3	TERMINATED	Drug Treatment Combined With Drug and Risk Reduction Counseling to Prevent of HIV Infection and Death Among Injection Drug Users
NCT00271219	PHASE3	COMPLETED	RCT Comparing Methadone and Buprenorphine in Pregnant Women
NCT00312195	PHASE3	COMPLETED	Safety and Efficacy of Buprenorphine Transdermal System (BTDS) in Subjects With Chronic Nonmalignant Pain
NCT00312221	PHASE3	TERMINATED	Safety and Efficacy of Buprenorphine Transdermal System (BTDS) in Subjects With Moderate to Severe Osteoarthritis Pain
NCT00312572	PHASE3	COMPLETED	Safety and Efficacy of Dose Conversion From Vicodin® to Buprenorphine Transdermal System (Butrans™) in Subjects With OA Pain
NCT00313014	PHASE3	TERMINATED	Safety and Efficacy of Buprenorphine Transdermal System (BTDS) in Subjects With Moderate to Severe Low Back Pain
NCT00313846	PHASE3	COMPLETED	Safety and Efficacy of Buprenorphine Transdermal System in Subjects With Moderate to Severe Osteoarthritis of Hip or Knee
NCT00315445	PHASE3	COMPLETED	The Safety and Efficacy of the Buprenorphine Transdermal System (BTDS) in Subjects With Chronic Back Pain.
NCT00315458	PHASE3	TERMINATED	Buprenorphine Transdermal Patch in Subjects With Osteoarthritis Pain Requiring Opioids. Includes a 52-Week Safety Extension.
NCT00320801	PHASE3	TERMINATED	Buprenorphine Transdermal Patches (BTDS) in Subjects With Osteoarthritis Pain. Includes a 52-week Extension Phase.
NCT00345787	PHASE3	COMPLETED	Comparison of BTDS (Buprenorphine Transdermal System) and Placebo in Osteoarthritic Pain
NCT00346047	PHASE3	COMPLETED	Comparison of BTDS (Buprenorphine Transdermal System) and Placebo in Low Back Pain
NCT00490919	PHASE3	COMPLETED	Buprenorphine Transdermal System (BTDS) in Subjects With Moderate to Severe Chronic Low Back Pain

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.

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

Molecule	Source	Status	Shared targets
ALOGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	OPRK1, OPRM1
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	OPRK1, OPRM1
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	OPRK1, OPRM1
Mavorixafor	ChEMBL + PubChem	Phase 4 (approved)	OPRK1, OPRM1
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	OPRK1, OPRM1
ALPIDEM	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
ALVIMOPAN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
AMBENONIUM	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
AMIODARONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
AMLODIPINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
AMOXAPINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
ATOMOXETINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
BENZTROPINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
BEPRIDIL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
BOSUTINIB	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
BROMPERIDOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
BUTORPHANOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CANNABIDIOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CARVEDILOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CINACALCET	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CINNARIZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CLEMASTINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CLOPIDOGREL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
CODEINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DANAZOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DARIFENACIN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DESERPIDINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DEXTROMETHORPHAN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DISULFIRAM	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DOBUTAMINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DOMPERIDONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DOXAZOSIN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
DULOXETINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
ECONAZOLE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
ETHINYL ESTRADIOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
FEDRATINIB	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
FENTANYL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
FLUOXETINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
HALAZEPAM	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
HALOPROGIN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
HYDROCODONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
HYDROMORPHONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
IMIPRAMINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
LANSOPRAZOLE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
LEVALLORPHAN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
LEVORPHANOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
LOPERAMIDE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
LORATADINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
LOXAPINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
MECLIZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
MEFLOQUINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
MEPERIDINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
METHADONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
METHYLNALTREXONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
MIANSERIN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
MICONAZOLE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
MIFEPRISTONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
MORPHINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NAFTOPIDIL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NALBUPHINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NALFURAFINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NALMEFENE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NALOXONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NALTREXONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NEBIVOLOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NEFAZODONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NEFOPAM	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
NELFINAVIR	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
OLICERIDINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
OXYCODONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
OXYMORPHONE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PAROXETINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PASIREOTIDE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PENTAZOCINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PHYSOSTIGMINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PIMOZIDE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PRAZOSIN	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PRENYLAMINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PROMAZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PROMETHAZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PROPIOMAZINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PROPIVERINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
PROPRANOLOL	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
QUETIAPINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
QUINIDINE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1
RALOXIFENE	ChEMBL	Phase 4 (approved)	OPRK1, OPRM1