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

Stem definitionDrug idCAS RN
antihistaminics 1564 79516-68-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • livostin
  • levocabastine hydrochloride
  • levocabastine
  • levophta
  • levocabastine HCl
for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis
  • Molecular weight: 420.53
  • Formula: C26H29FN2O2
  • CLOGP: 1.86
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 64.33
  • ALOGS: -5.08
  • ROTB: 4

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
0.60 mg N

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 70 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.07 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.17 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.43 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.45 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 33 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 10, 1993 FDA NOVARTIS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC R01AC02 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Antiallergic agents, excl. corticosteroids
ATC S01GX02 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Other antiallergics
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D039563 Histamine H1 Antagonists, Non-Sedating
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Allergic conjunctivitis indication 473460002 DOID:11204

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.47 acidic
pKa2 8.56 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
Histamine H1 receptor GPCR ANTAGONIST Ki 7.28 WOMBAT-PK CHEMBL
Neurotensin receptor type 2 GPCR AGONIST Ki 6.80 IUPHAR
Multidrug resistance protein 1 Transporter WOMBAT-PK
Neurotensin receptor 2 Unclassified Ki 7.48 CHEMBL
Neurotensin receptor type 2 GPCR AGONIST IC50 8.70 IUPHAR

External reference:

IDSource
4020853 VUID
N0000022941 NUI
C0771194 UMLSCUI
D01717 KEGG_DRUG
124XMA6YEI UNII
79547-78-7 SECONDARY_CAS_RN
108863001 SNOMEDCT_US
4023908 VANDF
28627 RXNORM
372554006 SNOMEDCT_US
004416 NDDF
DB01106 DRUGBANK_ID
5393 INN_ID
CHEBI:135679 CHEBI
CHEMBL1237102 ChEMBL_ID
CHEMBL1615438 ChEMBL_ID
54385 PUBCHEM_CID
1586 IUPHAR_LIGAND_ID
C047340 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None