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

Stem definitionDrug idCAS RN
antihypertensives, clonidine derivatives 1593 31036-80-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lofexidine hydrochloride
  • lofexidine
  • (+/-)-Lofexidine
  • lofexidine HCl
  • lofexadine
Lofexidine is a central alpha-2 adrenergic agonist that binds to receptors on adrenergic neurons. This reduces the release of norepinephrine and decreases sympathetic tone.
  • Molecular weight: 259.13
  • Formula: C11H12Cl2N2O
  • CLOGP: 3.46
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 33.62
  • ALOGS: -3.25
  • ROTB: 3

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
1.40 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
May 16, 2018 FDA US WORLDMEDS LLC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07BC04 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in opioid dependence
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
CHEBI has role CHEBI:35569 alpha-adrenergic agonist
CHEBI has role CHEBI:35674 antihypertensive agent
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D009292 Narcotic Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Opioid withdrawal indication 87132004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.49 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.18MG BASE LUCEMYRA US WORLDMEDS LLC N209229 May 16, 2018 RX TABLET ORAL May 16, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-2A adrenergic receptor GPCR AGONIST Ki 8.36 CHEMBL SCIENTIFIC LITERATURE
Alpha-2B adrenergic receptor GPCR Ki 7.17 CHEMBL
Alpha-2C adrenergic receptor GPCR Ki 7.16 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 6.90 CHEMBL
Adrenergic receptor alpha-2 GPCR IC50 8.60 CHEMBL
Adrenergic receptor alpha-1 GPCR IC50 6.18 CHEMBL

External reference:

IDSource
4025252 VUID
N0000171822 NUI
C0771049 UMLSCUI
D04765 KEGG_DRUG
d04956 MMSL
349934008 SNOMEDCT_US
4025251 VANDF
28863 RXNORM
395989000 SNOMEDCT_US
004132 NDDF
CHEBI:51368 CHEBI
CHEMBL17860 ChEMBL_ID
UI82K0T627 UNII
3766 INN_ID
21498-08-8 SECONDARY_CAS_RN
DB04948 DRUGBANK_ID
30668 PUBCHEM_CID
CHEMBL1788132 ChEMBL_ID
9868 IUPHAR_LIGAND_ID
C025655 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Lucemyra HUMAN PRESCRIPTION DRUG LABEL 1 27505-050 TABLET, FILM COATED 0.20 mg ORAL NDA 18 sections