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nalmefene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists related to normorphine | 1876 | 55096-26-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 18 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 124 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 9.60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.80 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 40 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 8.20 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 15 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.65 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 8.80 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.615 | High | 0.81 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.905 | High | 0.81 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 26.853 | 10^-6 cm/s | High | 0.81 |
| dh-clint | Dog hepatocyte intrinsic clearance | 26.730 | uL/min/10^6 cells | High | 0.81 |
| dppb | Dog plasma protein binding (% unbound) | 20.190 | % | High | 0.81 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 42.570 | % | High | 0.81 |
| herg | hERG pIC50 | 5.239 | pIC50 | High | 0.81 |
| hh-clint | Human hepatocyte intrinsic clearance | 8.035 | uL/min/10^6 cells | High | 0.81 |
| hlm-clint | Human liver microsomal intrinsic clearance | 29.512 | uL/min/mg protein | High | 0.81 |
| hppb | Human plasma protein binding (% unbound) | 26.230 | % | High | 0.81 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PRKDC,TEK,TGFBR1 | 21 | |||
| kinase-selectivity-class | EIF2AK3,GRK2,MAP2K6,MAP3K14 | 4 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.069 | High | 0.81 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.466 | High | 0.81 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 61.660 | High | 0.81 | |
| mppb | Mouse plasma protein binding (% unbound) | 22.990 | High | 0.81 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.091 | High | 0.81 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | High | 0.81 | |
| pppb | Pig plasma protein binding (% unbound) | 36.470 | % | High | 0.81 |
| rat-kpuu-brain | Rat brain Kpuu | 0.233 | % | High | 0.81 |
| rh-clint | Rat hepatocyte intrinsic clearance | 103.753 | uL/min/10^6 cells | High | 0.81 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 56.750 | % | High | 0.81 |
| rppb | Rat plasma protein binding (% unbound) | 15.970 | % | High | 0.81 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 659.174 | uM | High | 0.81 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 1, 2019 | PMDA | OTSUKA PHARMACEUTICAL CO., LTD. | |
| April 17, 1995 | FDA | EUROHLTH INTL SARL |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Coma | 104.08 | 90.60 | 29 | 357 | 72603 | 90555458 |
FDA Adverse Event Reporting System (Male)
| 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 | 117.55 | 72.76 | 30 | 422 | 21519 | 42599364 |
| Coma | 106.97 | 72.76 | 34 | 418 | 53520 | 42567363 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Coma | 198.51 | 68.31 | 61 | 794 | 117808 | 110470636 |
| Drug withdrawal syndrome | 162.70 | 68.31 | 41 | 814 | 38013 | 110550431 |
| Drug interaction | 83.12 | 68.31 | 50 | 805 | 500133 | 110088311 |
| Respiratory depression | 77.26 | 68.31 | 22 | 833 | 31979 | 110556465 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07BB05 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS DRUGS USED IN ADDICTIVE DISORDERS Drugs used in alcohol dependence |
| FDA MoA | N0000000154 | Opioid Antagonists |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D009292 | Narcotic Antagonists |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| FDA EPC | N0000175691 | Opioid Antagonist |
Related Drugs by ATC class:
N07BB Drugs used in alcohol dependence 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Alcoholism | indication | 7200002 | |
| Poisoning by opiate analgesic drug | indication | 241749009 | |
| Opiate-Induced Respiratory Depression | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.73 | acidic |
| pKa2 | 8.16 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 2.7MG BASE/SPRAY | OPVEE | INDIVIOR | N217470 | May 22, 2023 | RX | SPRAY | NASAL | 11458091 | July 10, 2038 | TREATING OPIOID OVERDOSE |
| EQ 1.5MG BASE/0.5ML (EQ 1.5MG BASE/0.5ML) | ZURNAI (AUTOINJECTOR) | KNOA PHARMA | N218590 | Aug. 7, 2024 | RX | SOLUTION | INTRAMUSCULAR, SUBCUTANEOUS | 11865112 | Nov. 5, 2039 | TREATING OPIOID OVERDOSE |
| EQ 2.7MG BASE/SPRAY | OPVEE | INDIVIOR | N217470 | May 22, 2023 | RX | SPRAY | NASAL | 12290596 | Aug. 4, 2042 | EMERGENCY TREATMENT OF A KNOWN OR SUSPECTED OPIOID OVERDOSE/SYMPTOM THEREOF IN A HUMAN CAUSED BY NATURAL OR SYNTHETIC OPIOIDS, SUCH AS REMIFENTANIL-INDUCED RESPIRATORY DEPRESSION, WITH 2.7MG NALMEFENE, ADMINISTERED AS 3MG NALMEFENE HYDROCHLORIDE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 2.7MG BASE/SPRAY | OPVEE | INDIVIOR | N217470 | May 22, 2023 | RX | SPRAY | NASAL | May 22, 2026 | NEW PRODUCT |
| EQ 1.5MG BASE/0.5ML (EQ 1.5MG BASE/0.5ML) | ZURNAI (AUTOINJECTOR) | KNOA PHARMA | N218590 | Aug. 7, 2024 | RX | SOLUTION | INTRAMUSCULAR, SUBCUTANEOUS | Aug. 7, 2027 | NEW PRODUCT |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | ANTAGONIST | Kd | 9.53 | CHEMBL | CHEMBL | |||
| Kappa-type opioid receptor | GPCR | ANTAGONIST | Ki | 9.92 | CHEMBL | CHEMBL | |||
| Delta-type opioid receptor | GPCR | ANTAGONIST | Kd | 9.04 | CHEMBL | CHEMBL | |||
| Mu-type opioid receptor | GPCR | Ki | 9.54 | CHEMBL | |||||
| Delta-type opioid receptor | GPCR | Ki | 8.47 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 8.70 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| TOV02TDP9I | UNII |
| 4023995 | VUID |
| N0000022000 | NUI |
| D05111 | KEGG_DRUG |
| 1228646-70-5 | SECONDARY_CAS_RN |
| 4020923 | VANDF |
| 4023995 | VANDF |
| C0068377 | UMLSCUI |
| CHEBI:7457 | CHEBI |
| CHEMBL982 | ChEMBL_ID |
| 5284594 | PUBCHEM_CID |
| DB06230 | DRUGBANK_ID |
| CHEMBL5315055 | ChEMBL_ID |
| CHEMBL1201152 | ChEMBL_ID |
| 5189 | INN_ID |
| C038981 | MESH_SUPPLEMENTAL_RECORD_UI |
| 1628 | IUPHAR_LIGAND_ID |
| 58895-64-0 | SECONDARY_CAS_RN |
| 236069 | RXNORM |
| 357929 | MMSL |
| 42151 | MMSL |
| 5149 | MMSL |
| d03834 | MMSL |
| 005023 | NDDF |
| 005024 | NDDF |
| 109098006 | SNOMEDCT_US |
| 361000220103 | SNOMEDCT_US |
| 412252005 | SNOMEDCT_US |
| 764607009 | SNOMEDCT_US |
| TOV02TDP9I | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| OPVEE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 12496-0003 | SPRAY | 2.70 mg | NASAL | NDA | 29 sections |
| NALMEFENE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59011-960 | INJECTION, SOLUTION | 1 mg | INTRAMUSCULAR | ANDA | 22 sections |
| Zurnai | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59011-962 | INJECTION, SOLUTION | 1.50 mg | INTRAMUSCULAR | NDA | 29 sections |
| nalmefene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82432-101 | SOLUTION | 0.10 mg | INTRAVENOUS | ANDA | 17 sections |
| nalmefene hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82432-102 | SOLUTION | 2 mg | INTRAVENOUS | ANDA | 17 sections |