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oliceridine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| analgesics, pethidine derivatives and other synthetic small molecule miu-opioid receptor agonists | 5406 | 1401028-24-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Oliceridine is a full opioid agonist and is relatively selective for the mu-opioid receptor. The principal therapeutic action of oliceridine is analgesia. Like all full opioid agonists, there is no ceiling effect to analgesia for oliceridine. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory, and CNS depression. The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.031 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.323 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 19.815 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 34.356 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 27.820 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 33.280 | % | High | 1 |
| herg | hERG pIC50 | 5.378 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 67.920 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 295.121 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 20.750 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1 | 21 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,PDK4 | 4 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.890 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 205.589 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 36.740 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 15.241 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 50.980 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 197.697 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 76.680 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 38.520 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 901.571 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 7, 2020 | FDA | TREVENA INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02AX07 | NERVOUS SYSTEM ANALGESICS OPIOIDS Other opioids |
| CHEBI has role | CHEBI:35480 | analgesic |
Related Drugs by ATC class:
N02AX Other opioids 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Moderate pain | indication | 50415004 | |
| Severe pain | indication | 76948002 | |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Decreased respiratory function | contraindication | 80954004 | |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 1MG/ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 11077098 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 1MG/ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 11931350 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 1MG/ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 8835488 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 1MG/ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 9309234 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 1MG/ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 9642842 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 2MG/2ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 11077098 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 2MG/2ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 11931350 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 2MG/2ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 8835488 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 2MG/2ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 9309234 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 2MG/2ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 9642842 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 30MG/30ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 11077098 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 30MG/30ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 11931350 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 30MG/30ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 8835488 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 30MG/30ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 9309234 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
| 30MG/30ML (1MG/ML) | OLINVYK | TREVENA | N210730 | Oct. 30, 2020 | DISCN | SOLUTION | INTRAVENOUS | 9642842 | March 23, 2032 | MANAGEMENT OF ACUTE PAIN BY INTRAVENOUS INJECTION |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | AGONIST | Ki | 8.22 | DRUG LABEL | DRUG LABEL | |||
| D(2) dopamine receptor | GPCR | Ki | 4.08 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.21 | CHEMBL | |||||
| Cytochrome P450 3A4 | Enzyme | IC50 | 4.87 | CHEMBL | |||||
| Sodium channel protein type 5 subunit alpha | Ion channel | IC50 | 5.33 | CHEMBL | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 5.34 | CHEMBL | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | IC50 | 4.44 | CHEMBL | |||||
| Nociceptin receptor | GPCR | AGONIST | EC50 | 7.40 | SCIENTIFIC LITERATURE | ||||
| D(3) dopamine receptor | GPCR | Ki | 5.16 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D11214 | KEGG_DRUG |
| MCN858TCP0 | UNII |
| C4508938 | UMLSCUI |
| CHEBI:747294 | CHEBI |
| WH2 | PDB_CHEM_ID |
| CHEMBL2443262 | ChEMBL_ID |
| 66553195 | PUBCHEM_CID |
| DB14881 | DRUGBANK_ID |
| 10250 | INN_ID |
| C586842 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7334 | IUPHAR_LIGAND_ID |
| 897038008 | SNOMEDCT_US |
| 897041004 | SNOMEDCT_US |
| 4039828 | VANDF |
| 341480 | MMSL |
| d09691 | MMSL |
| 018475 | NDDF |
| 2392230 | RXNORM |
| MCN858TCP0 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| OLINVYK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71308-011 | INJECTION, SOLUTION | 1 mg | INTRAVENOUS | NDA | 32 sections |
| OLINVYK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71308-021 | INJECTION, SOLUTION | 2 mg | INTRAVENOUS | NDA | 32 sections |
| OLINVYK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71308-301 | INJECTION, SOLUTION | 30 mg | INTRAVENOUS | NDA | 32 sections |