halofantrine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 6.30 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GAK,GRK2,GSK3B,INSR,ITK,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM1,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 65
kinase-selectivity-class AXL,EIF2AK3,EPHB4,MAPK7,PDK4,STK33,TTK 7
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.108 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 1
rat-kpuu-brain Rat brain Kpuu 3.926 % High 1

Approvals:

DateAgencyCompanyOrphan
July 24, 1992 FDA GLAXOSMITHKLINE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

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
CHEBI has role CHEBI:38068 antimalarial

Related Drugs by ATC class:

P01BX Other antimalarials 2 drugs
arterolanepiperaquine

Drug Use | Suggest Off label Use Form| |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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
D02485 KEGG_DRUG
36167-63-2 SECONDARY_CAS_RN
4021108 VANDF
4024114 VANDF
C0120726 UMLSCUI
CHEBI:5612 CHEBI
CHEMBL1107 ChEMBL_ID
CHEMBL1200901 ChEMBL_ID
DB01218 DRUGBANK_ID
C023768 MESH_SUPPLEMENTAL_RECORD_UI
10019 IUPHAR_LIGAND_ID
4749 INN_ID
Q2OS4303HZ UNII
37393 PUBCHEM_CID
151844 RXNORM
17110 MMSL
46102 MMSL
d04842 MMSL
003977 NDDF
003978 NDDF
108681001 SNOMEDCT_US
108682008 SNOMEDCT_US
372527008 SNOMEDCT_US

Pharmaceutical products:

None