nalmefene Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists related to normorphine 1876 55096-26-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nalmefene
  • nalmefene hydrochloride dihydrate
  • selincro
  • nalmetrene
  • 6-desoxy-6-methylenenaltrexone
  • nalmefene hydrochloride
  • nalmefene HCl
  • ORF-11676
  • nalmefene hydrochloride hydrate
  • Molecular weight: 339.44
  • Formula: C21H25NO3
  • CLOGP: 2.64
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 52.93
  • ALOGS: -2.61
  • ROTB: 2

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
18 mg O

ADMET properties:

PropertyValueReference
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 ┬ÁM/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

Approvals:

DateAgencyCompanyOrphan
April 17, 1995 FDA EUROHLTH INTL SARL
Aug. 1, 2019 PMDA OTSUKA PHARMACEUTICAL CO., LTD.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Alcoholism indication 7200002
Poisoning by opiate analgesic drug indication 241749009
Opiate-Induced Respiratory Depression indication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.73 acidic
pKa2 8.16 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
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
CHEMBL1201152 ChEMBL_ID
C038981 MESH_SUPPLEMENTAL_RECORD_UI
1628 IUPHAR_LIGAND_ID
5189 INN_ID
236069 RXNORM
5149 MMSL
d03834 MMSL
005023 NDDF
005024 NDDF
109098006 SNOMEDCT_US
361000220103 SNOMEDCT_US
412252005 SNOMEDCT_US
764607009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NALMEFENE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 59011-960 INJECTION, SOLUTION 1 mg INTRAMUSCULAR ANDA 22 sections