Drug Information

Drug (ID: DG00098) and It's Reported Resistant Information

• Name: Halofantrine
• Synonyms: Halfan; Halofantrino; HALOFANTRINE HYDROCHLORIDE; Halofantrine HCl; Halofantrine Hydrochloride [USAN]; Halofantrine [USAN]; Halofantrino [Spanish]; WR 171669; Dl-WR 171669; Halfan (TN); Halofantrine hydrochloride (USAN); WR 171,699; WR-171669; WR-171699; SK&F-102866; WR-171,669; (+-)-Halofantrine hydrochloride; (1)-Halofantrine; 1,3-Dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-9-phenanthrene-methanol; 1,3-Dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-9-phenathrenemethanol; 1,3-Dichloro-6-trifluoromethyl-9-(3-(dibutylamino)-1-hydroxypropyl)phenanthrene HCl; 1,3-Dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-9-phenanthrenemethanol hydrochloride; 1,3-Dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)phenanthren-1-methanol hydrochloride; 1-(1,3-Dichloro-6-trifluoromethyl-9-phenanthryl)-3-(di-n-butylamino)propanol hydrochloride; 1-(1,3-dichloro-6-trifluoromethyl-9-phenanthryl)-3-di(n-butyl)aminopropanol HCl; 3-(Dibutylamino)-1-(1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl)propan-1-ol hydrochloride; 3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol; 3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol hydrochloride; 9-(3-(dibutylamino)-1-hydroxypropyl)-1,3-dichloro-6-(trifluoromethyl)phenanthrene hydrochloride; 9-Phenanthrenemethanol, 1,3-dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-(1); 9-Phenanthrenemethanol, 1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-, hydrochloride; 9-Phenanthrenemethanol, 1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-,hydrochloride
• Indication:
  In total 1 Indication(s)
  Malaria [ICD-11: 1F45]; Approved; [1]
• Target: Calmodulin (CALM); CALM1_HUMAN CALM2_HUMAN CALM3_HUMAN; [1]
• Formula: C26H30Cl2F3NO
• IsoSMILES: CCCCN(CCCC)CCC(C1=C2C=CC(=CC2=C3C=C(C=C(C3=C1)Cl)Cl)C(F)(F)F)O
• InChI: 1S/C26H30Cl2F3NO/c1-3-5-10-32(11-6-4-2)12-9-25(33)23-16-22-21(14-18(27)15-24(22)28)20-13-17(26(29,30)31)7-8-19(20)23/h7-8,13-16,25,33H,3-6,9-12H2,1-2H3
• InChIKey: FOHHNHSLJDZUGQ-UHFFFAOYSA-N
• PubChem CID: 37393
• ChEBI ID: CHEBI:94392
• TTD Drug ID: D07MVK
• VARIDT ID: DR00770
• INTEDE ID: DR0799
• DrugBank ID: DB01218

Type(s) of Resistant Mechanism of This Drug

  IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Astrocytoma [ICD-11: 2F36]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Multidrug resistance protein 1 (ABCB1) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Malaria [ICD-11: 1F45.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Plasmodium falciparum strains; 5833
• Experiment for Drug Resistance: SYBR Green I detection assay
• Mechanism Description: The presence of non-toxic concentrations of Mk571 sensitized both chloroquine-sensitive and -resistant parasites to mefloquine and halofantrine, likely by competing against PfMDR1-mediated sequestering of the drugs into the DV compartment and away from the drugs' cytosolic targets.

References

• Ref 1: A 2-amino quinoline, 5-(3-(2-(7-chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid, interacts with PfMDR1 and inhibits its drug transport in Plasmodium falciparum. Mol Biochem Parasitol. 2014 Jun;195(1):34-42. doi: 10.1016/j.molbiopara.2014.05.006. Epub 2014 Jun 8.