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

Stem definitionDrug idCAS RN
1617 82186-77-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lumefantrine
  • benflumelol
  • benflumetol
Lumefantrine is an antimalarial agent. Available data suggest lumefantrine inhibits the formation of beta-hematin by forming a complex with hemin.
  • Molecular weight: 528.94
  • Formula: C30H32Cl3NO
  • CLOGP: 10.20
  • LIPINSKI: 2
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -7.23
  • ROTB: 10

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.28 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 7, 2009 FDA NOVARTIS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC P01BF01 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTIPROTOZOALS
ANTIMALARIALS
Artemisinin and derivatives, combinations
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000962 Antimalarials
MeSH PA D000977 Antiparasitic Agents
MeSH PA D000981 Antiprotozoal Agents
CHEBI has role CHEBI:38068 antimalarial

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Falciparum malaria indication 62676009 DOID:14067
Torsades de pointes contraindication 31722008
Hypokalemia contraindication 43339004
Bradycardia contraindication 48867003
Prolonged QT interval contraindication 111975006
Hypomagnesemia contraindication 190855004
Congenital long QT syndrome contraindication 442917000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.94 acidic
pKa2 8.77 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
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.09 CHEMBL

External reference:

IDSource
D000078102 MESH_DESCRIPTOR_UI
4028722 VUID
N0000178418 NUI
C0531104 UMLSCUI
D03821 KEGG_DRUG
421180001 SNOMEDCT_US
420307001 SNOMEDCT_US
847728 RXNORM
18118 MMSL
d05144 MMSL
4028722 VANDF
009715 NDDF
CHEMBL38827 ChEMBL_ID
CHEMBL422330 ChEMBL_ID
F38R0JR742 UNII
7610 INN_ID
DB06708 DRUGBANK_ID
CHEBI:156095 CHEBI
6437380 PUBCHEM_CID
9969 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
COARTEM HUMAN PRESCRIPTION DRUG LABEL 2 0078-0568 TABLET 120 mg ORAL NDA 17 sections
COARTEM HUMAN PRESCRIPTION DRUG LABEL 2 76413-154 TABLET 120 mg ORAL NDA 17 sections