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

Stem definitionDrug idCAS RN
1350 69756-53-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • halofantrine hydrochloride
  • halofantrine
  • halfan
  • halofantrine HCl
used in treatment of mild to moderate acute malaria
  • Molecular weight: 500.43
  • Formula: C26H30Cl2F3NO
  • CLOGP: 9.31
  • LIPINSKI: 2
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -6.66
  • ROTB: 11

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
1.50 g O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 49.96 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 6.30 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
July 24, 1992 FDA GLAXOSMITHKLINE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC P01BX01 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTIPROTOZOALS
ANTIMALARIALS
Other antimalarials
FDA EPC N0000175482 Antimalarial
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000962 Antimalarials
MeSH PA D000977 Antiparasitic Agents
MeSH PA D000981 Antiprotozoal Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Vivax malaria indication 27052006 DOID:12978
Falciparum malaria indication 62676009 DOID:14067
Kidney disease contraindication 90708001 DOID:557
Prolonged QT interval contraindication 111975006
Atrioventricular Conduction Defect contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.53 acidic
pKa2 9.06 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 Ki 5.12 CHEMBL

External reference:

IDSource
4021108 VUID
N0000148563 NUI
C0148859 UMLSCUI
D02485 KEGG_DRUG
108681001 SNOMEDCT_US
4024114 VANDF
d04842 MMSL
50749 RXNORM
372527008 SNOMEDCT_US
003977 NDDF
CHEMBL1107 ChEMBL_ID
H77DL0Y630 UNII
36167-63-2 SECONDARY_CAS_RN
4749 INN_ID
DB01218 DRUGBANK_ID
CHEBI:5612 CHEBI
CHEMBL1200901 ChEMBL_ID
37393 PUBCHEM_CID
10019 IUPHAR_LIGAND_ID
C023768 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None