DGIdb - BUPRENORPHINE Drug Record

BUPRENORPHINE chembl:CHEMBL511142 Approved

Alternate Names:

TEPHINE
BUPEAZE
PRENOTRIX
BUTEC
BUTRANS
BUPLAST
RELETRANS
ALKS-5461 COMPONENT BUPRENORPHINE
SUBLOCADE
TEMGESIC
SEVODYNE
TRANSTEC
PANITAZ
BUPRENORPHINE
HAPOCTASIN

Drug Info:

Drug Class	Small Molecule
FDA Approval	approved
Drug Class	Small molecule
Drug Indications	antidepressant,analgesic,for treatment of opioid addiction
Drug Class	analgesics, opioid
Year of Approval	1981

(3 More Sources)

Publications:

Crist RC et al., 2018, Pharmacogenetic analysis of opioid dependence treatment dose and dropout rate., Am J Drug Alcohol Abuse
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
Sánchez-Blázquez et al., 2001, Agonists determine the pattern of G-protein activation in mu-opioid receptor-mediated supraspinal analgesia., Brain Res. Bull.
Kishioka et al., 2000, Buprenorphine and methoclocinnamox: agonist and antagonist effects on respiratory function in rhesus monkeys., Eur. J. Pharmacol.
Ide et al., 2004, Buprenorphine antinociception is abolished, but naloxone-sensitive reward is retained, in mu-opioid receptor knockout mice., Neuropsychopharmacology
Zubieta et al., 2000, Buprenorphine-induced changes in mu-opioid receptor availability in male heroin-dependent volunteers: a preliminary study., Neuropsychopharmacology
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Mizoguchi et al., 2002, Antagonistic property of buprenorphine for putative epsilon-opioid receptor-mediated G-protein activation by beta-endorphin in pons/medulla of the mu-opioid receptor knockout mouse., Neuroscience
Muriel J et al., 2019, Pharmacogenetics and prediction of adverse events in prescription opioid use disorder patients., Basic Clin Pharmacol Toxicol
Sastre JA et al., 2015, Influence of uridine diphosphate-glucuronyltransferase 2B7 (UGT2B7) variants on postoperative buprenorphine analgesia., Pain Pract
Crist RC et al., 2019, Replication of the pharmacogenetic effect of rs678849 on buprenorphine efficacy in African-Americans with opioid use disorder., Pharmacogenomics J
Clarke TK et al., 2014, Genetic variation in OPRD1 and the response to treatment for opioid dependence with buprenorphine in European-American females., Pharmacogenomics J
Crist RC et al., 2013, An intronic variant in OPRD1 predicts treatment outcome for opioid dependence in African-Americans., Neuropsychopharmacology
Lester et al., 2006, Comparison of the in vitro efficacy of mu, delta, kappa and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes., Brain Res.
Induru et al., Buprenorphine for neuropathic pain--targeting hyperalgesia., Am J Hosp Palliat Care
Mégarbane et al., 2006, Buprenorphine is protective against the depressive effects of norbuprenorphine on ventilation., Toxicol. Appl. Pharmacol.
Boothby et al., 2007, Buprenorphine for the treatment of opioid dependence., Am J Health Syst Pharm
Robinson, 2006, Buprenorphine-containing treatments: place in the management of opioid addiction., CNS Drugs
Ettienne EB et al., 2019, Pharmacogenomics and Opioid Use Disorder: Clinical Decision Support in an African American Cohort., J Natl Med Assoc
Blanco F et al., 2016, Influence of UGT2B7, CYP3A4, and OPRM1 Gene Polymorphisms on Transdermal Buprenorphine Pain Control in Patients with Critical Lower Limb Ischemia Awaiting Revascularization., Pain Pract

BUPRENORPHINE ARRB2

Interaction Score: 3.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30549211

Sources:
PharmGKB
BUPRENORPHINE PNOC

Interaction Score: 3.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
BUPRENORPHINE OPRD1

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name V1003

Novel drug target Established target

Trial Name ALKS 5461

PMIDs:
30549211 30368523 24126707 23612435 16443205 19666890 16169027

Sources:
TdgClinicalTrial PharmGKB
BUPRENORPHINE OPRM1

Interaction Score: 0.62

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
11275413 10729371 15100703 10942856 11752352 12435410 30549211

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB
BUPRENORPHINE UGT2B7

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24256307

Sources:
PharmGKB
BUPRENORPHINE OPRK1

Interaction Score: 0.43

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

PMIDs:
17244875 16953647

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
BUPRENORPHINE COMT

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30549211

Sources:
PharmGKB
BUPRENORPHINE SLC6A4

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29333880

Sources:
PharmGKB
BUPRENORPHINE CYP3A5

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
BUPRENORPHINE CYP3A4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31676110 26407542

Sources:
PharmGKB

TdgClinicalTrial: BUPRENORPHINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antidepressant,analgesic,for treatment of opioid addiction

Drug Class Small molecule

FDA Approval approved

Publications:
TEND: BUPRENORPHINE
- Version: 01-August-2011
Alternate Names:

Drug Info:

Year of Approval 1981

Drug Class analgesics, opioid

Publications:

PharmGKB: buprenorphine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Crist RC et al., 2018, Pharmacogenetic analysis of opioid dependence treatment dose and dropout rate., Am J Drug Alcohol Abuse

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

Sastre JA et al., 2015, Influence of uridine diphosphate-glucuronyltransferase 2B7 (UGT2B7) variants on postoperative buprenorphine analgesia., Pain Pract

TTD: Buprenorphine
- Version: 2020.06.01
Alternate Names:

D06AWE TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL511142
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
GuideToPharmacology: 135652673
- Version: 29-September-2020
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL511142
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Trial Name	V1003
Novel drug target	Established target
Trial Name	ALKS 5461

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Partial agonist

Mechanism of Interaction	Kappa opioid receptor agonist
Direct Interaction	yes
Specific Action of the Ligand	Antagonist

partial agonist (activating)
agonist (activating)

agonist (activating)
antagonist (inhibitory)

BUPRENORPHINE Drug Record

BUPRENORPHINE chembl:CHEMBL511142 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30549211

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name V1003 Novel drug target Established target Trial Name ALKS 5461

PMIDs: 30549211 30368523 24126707 23612435 16443205 19666890 16169027

Sources: TdgClinicalTrial PharmGKB

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Partial agonist

PMIDs: 11275413 10729371 15100703 10942856 11752352 12435410 30549211

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24256307

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Kappa opioid receptor agonist Direct Interaction yes Specific Action of the Ligand Antagonist

PMIDs: 17244875 16953647

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30549211

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29333880

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31676110 26407542

Sources: PharmGKB

TdgClinicalTrial: BUPRENORPHINE

Alternate Names:

Drug Info: Drug Indications antidepressant,analgesic,for treatment of opioid addiction Drug Class Small molecule FDA Approval approved

Publications:

TEND: BUPRENORPHINE

Alternate Names:

Drug Info: Year of Approval 1981 Drug Class analgesics, opioid

Publications:

PharmGKB: buprenorphine

Alternate Names:

Drug Info:

TTD: Buprenorphine

Alternate Names: D06AWE TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL511142

Alternate Names:

Drug Info:

Publications:

GuideToPharmacology: 135652673

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL511142

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
30549211

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name V1003

Novel drug target Established target

Trial Name ALKS 5461

PMIDs:
30549211 30368523 24126707 23612435 16443205 19666890 16169027

Sources:
TdgClinicalTrial PharmGKB

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
11275413 10729371 15100703 10942856 11752352 12435410 30549211

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24256307

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

PMIDs:
17244875 16953647

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
30549211

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
29333880

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
31676110 26407542

Sources:
PharmGKB

Drug Info:

Drug Indications antidepressant,analgesic,for treatment of opioid addiction

Drug Class Small molecule

FDA Approval approved

Drug Info:

Year of Approval 1981

Drug Class analgesics, opioid

Alternate Names:

D06AWE TTD Drug ID