Stem definition | Drug id | CAS RN |
---|---|---|
opioid receptor antagonists/agonists, morphinan derivates | 434 | 52485-79-7 |
Dose | Unit | Route |
---|---|---|
1.20 | mg | P |
1.20 | mg | SL |
1.20 | mg | TD |
1.60 | mg | implant |
2.10 | mg | P |
8 | mg | SL |
8 | mg | SL |
Property | Value | Reference |
---|---|---|
Vd (Volume of distribution) | 4.90 L/kg | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 3.20 hours | Lombardo F, Berellini G, Obach RS |
BA (Bioavailability) | 28 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
CL (Clearance) | 19 mL/min/kg | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 17 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.04 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
fu (Fraction unbound in plasma) | 0.04 % | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 29, 1981 | FDA | RECKITT BENCKISER | |
June 19, 2019 | EMA | L. Molteni & C. dei Fratelli Alitti Societร di Esercizio S.p.A. |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Application site pruritus | 1723.75 | 12.70 | 407 | 34522 | 3577 | 63450516 |
Product adhesion issue | 1716.21 | 12.70 | 419 | 34510 | 4300 | 63449793 |
Drug withdrawal syndrome | 1527.96 | 12.70 | 571 | 34358 | 26623 | 63427470 |
Application site erythema | 1212.11 | 12.70 | 319 | 34610 | 4516 | 63449577 |
Application site rash | 944.63 | 12.70 | 229 | 34700 | 2269 | 63451824 |
Inadequate analgesia | 707.98 | 12.70 | 188 | 34741 | 2755 | 63451338 |
Application site pain | 704.83 | 12.70 | 202 | 34727 | 3980 | 63450113 |
Application site vesicles | 701.65 | 12.70 | 162 | 34767 | 1273 | 63452820 |
Application site burn | 559.81 | 12.70 | 122 | 34807 | 712 | 63453381 |
Drug abuse | 543.10 | 12.70 | 391 | 34538 | 72127 | 63381966 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug abuse | 1799.74 | 14.74 | 1133 | 31969 | 97963 | 34825866 |
Drug withdrawal syndrome | 1757.28 | 14.74 | 672 | 32430 | 19162 | 34904667 |
Drug dependence | 1120.36 | 14.74 | 517 | 32585 | 23700 | 34900129 |
Intentional product misuse | 788.14 | 14.74 | 507 | 32595 | 45104 | 34878725 |
Substance abuse | 636.65 | 14.74 | 248 | 32854 | 7393 | 34916436 |
Product adhesion issue | 582.79 | 14.74 | 159 | 32943 | 1441 | 34922388 |
Toxicity to various agents | 573.08 | 14.74 | 818 | 32284 | 199544 | 34724285 |
Miosis | 560.37 | 14.74 | 241 | 32861 | 9294 | 34914535 |
Drug withdrawal syndrome neonatal | 548.85 | 14.74 | 183 | 32919 | 3436 | 34920393 |
Injection site pain | 450.83 | 14.74 | 339 | 32763 | 38666 | 34885163 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug abuse | 2105.40 | 11.99 | 1303 | 49836 | 161388 | 79531861 |
Drug withdrawal syndrome | 1627.02 | 11.99 | 667 | 50472 | 34051 | 79659198 |
Drug dependence | 1175.73 | 11.99 | 557 | 50582 | 40212 | 79653037 |
Application site pruritus | 1122.40 | 11.99 | 295 | 50844 | 3515 | 79689734 |
Product adhesion issue | 990.12 | 11.99 | 249 | 50890 | 2455 | 79690794 |
Application site erythema | 820.18 | 11.99 | 246 | 50893 | 4864 | 79688385 |
Toxicity to various agents | 735.15 | 11.99 | 1110 | 50029 | 420430 | 79272819 |
Intentional product misuse | 724.81 | 11.99 | 551 | 50588 | 94614 | 79598635 |
Substance abuse | 671.17 | 11.99 | 253 | 50886 | 10273 | 79682976 |
Miosis | 610.91 | 11.99 | 265 | 50874 | 15524 | 79677725 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug withdrawal syndrome neonatal | 58.63 | 35.09 | 43 | 167 | 2076 | 87506 |
Poor feeding infant | 38.65 | 35.09 | 13 | 197 | 97 | 89485 |
Source | Code | Description |
---|---|---|
ATC | N02AE01 | NERVOUS SYSTEM ANALGESICS OPIOIDS Oripavine derivatives |
ATC | N07BC01 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS DRUGS USED IN ADDICTIVE DISORDERS Drugs used in opioid dependence |
ATC | N07BC51 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS DRUGS USED IN ADDICTIVE DISORDERS Drugs used in opioid dependence |
CHEBI has role | CHEBI:35482 | narcotic analgesic |
CHEBI has role | CHEBI:55322 | mu-opioid agonists |
CHEBI has role | CHEBI:59283 | delta-opioid antagonists |
CHEBI has role | CHEBI:167165 | kappa-opioid receptor antagonists |
CHEBI has role | CHEBI:59282 | kappa-opioid receptor agonists |
FDA EPC | N0000175689 | Partial Opioid Agonist |
FDA MoA | N0000175685 | Partial Opioid Agonists |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Opioid dependence | indication | 75544000 | DOID:2559 |
Severe pain | indication | 76948002 | |
Chronic pain | indication | 82423001 | |
Prevention of opioid abuse | indication | 426928008 | |
Acute postoperative pain | indication | 107401000119105 | |
Chronic Pain with Opioid Tolerance | indication | ||
Opioid withdrawal | off-label use | 87132004 | |
Dependent drug abuse | contraindication | 6525002 | |
Alcohol withdrawal delirium | contraindication | 8635005 | |
Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
Species | Use | Relation |
---|---|---|
Cats | Postoperative pain associated with surgical procedures | Indication |
Product | Applicant | Ingredients |
---|---|---|
Simbadol | Zoetis Inc. | 1 |
Zorbium | Elanco US Inc. | 1 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.97 | acidic |
pKa2 | 8.88 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 10198218 | June 6, 2031 | TREATMENT OF MODERATE TO SEVERE OPIOID USE DISORDER |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 10592168 | June 6, 2031 | TREATMENT OF MODERATE TO SEVERE OPIOID USE DISORDER |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9272044 | June 6, 2031 | TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9272044 | June 6, 2031 | TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE COMPOSITION WITH 28 DAY DOSE DURATION |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9272044 | June 6, 2031 | TREATING OPIOID ADDICTION BY ADMINISTERING BUPRENORPHINE ONCE PER MONTH |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9272044 | June 6, 2031 | TREATING OPIOID ADDICTION BY SUBCUTANEOUS INJECTION OF BUPRENORPHINE |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9498432 | June 6, 2031 | IN SITU FORMATION OF SOLID BUPRENORPHINE COMPOSITION |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9782402 | June 6, 2031 | TREATING ADDICTION BY ONCE PER MONTH ADMINISTRATION OF BUPRENORPHINE |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9782402 | June 6, 2031 | TREATING ADDICTION BY SUBCUTANEOUS INJECTION OF BUPRENORPHINE |
100MG/0.5ML (100MG/0.5ML) | SUBLOCADE | INDIVIOR | N209819 | Nov. 30, 2017 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | 9782402 | June 6, 2031 | TREATING ADDICTION WITH 100 MG OR 300 MG DOSE OF BUPRENORPHINE |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
128MG/0.36ML (356MG/ML) | BRIXADI | BRAEBURN | N210136 | May 23, 2023 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | May 23, 2026 | NEW PRODUCT |
16MG/0.32ML (50MG/ML) | BRIXADI | BRAEBURN | N210136 | May 23, 2023 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | May 23, 2026 | NEW PRODUCT |
24MG/0.48ML (50MG/ML) | BRIXADI | BRAEBURN | N210136 | May 23, 2023 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | May 23, 2026 | NEW PRODUCT |
32MG/0.64ML (50MG/ML) | BRIXADI | BRAEBURN | N210136 | May 23, 2023 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | May 23, 2026 | NEW PRODUCT |
64MG/0.18ML (356MG/ML) | BRIXADI | BRAEBURN | N210136 | May 23, 2023 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | May 23, 2026 | NEW PRODUCT |
8MG/0.16ML (50MG/ML) | BRIXADI | BRAEBURN | N210136 | May 23, 2023 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | May 23, 2026 | NEW PRODUCT |
96MG/0.27ML (356MG/ML) | BRIXADI | BRAEBURN | N210136 | May 23, 2023 | RX | SOLUTION, EXTENDED RELEASE | SUBCUTANEOUS | May 23, 2026 | NEW PRODUCT |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Kappa-type opioid receptor | GPCR | ANTAGONIST | Ki | 9.01 | WOMBAT-PK | CHEMBL | |||
Mu-type opioid receptor | GPCR | PARTIAL AGONIST | Ki | 8.29 | WOMBAT-PK | CHEMBL | |||
Delta-type opioid receptor | GPCR | ANTAGONIST | Ki | 8.07 | WOMBAT-PK | ||||
Nociceptin receptor | GPCR | Ki | 7.11 | CHEMBL | |||||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.10 | CHEMBL | |||||
Mu-type opioid receptor | GPCR | Ki | 9.89 | CHEMBL | |||||
Mu-type opioid receptor | GPCR | Ki | 9.40 | CHEMBL | |||||
Delta-type opioid receptor | GPCR | Ki | 9.32 | CHEMBL | |||||
Kappa-type opioid receptor | GPCR | Ki | 9.30 | CHEMBL |
ID | Source |
---|---|
001573 | NDDF |
004632 | NDDF |
11186 | MMSL |
1670 | IUPHAR_LIGAND_ID |
1819 | RXNORM |
21066009 | SNOMEDCT_US |
257949 | MMSL |
27271 | MMSL |
31684002 | SNOMEDCT_US |
31700 | MMSL |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3239 | PATCH, EXTENDED RELEASE | 7.50 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3239 | PATCH, EXTENDED RELEASE | 7.50 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3656 | PATCH, EXTENDED RELEASE | 5 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3656 | PATCH, EXTENDED RELEASE | 5 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3657 | PATCH, EXTENDED RELEASE | 10 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3657 | PATCH, EXTENDED RELEASE | 10 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3658 | PATCH, EXTENDED RELEASE | 15 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3658 | PATCH, EXTENDED RELEASE | 15 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3659 | PATCH, EXTENDED RELEASE | 20 ug | TRANSDERMAL | ANDA | 31 sections |
Buprenorphine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3659 | PATCH, EXTENDED RELEASE | 20 ug | TRANSDERMAL | ANDA | 31 sections |