| Identification | Back Directory | [Name]
9-Phenanthrenemethanol, 1,3-dichloro-α-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-, (-)- | [CAS]
66051-76-1 | [Synonyms]
L-WR-171669
Halofantrine, ( ) ,Halofantrine, ()
9-Phenanthrenemethanol, 1,3-dichloro-α-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-, (-)- | [Molecular Formula]
C26H30Cl2F3NO | [MOL File]
66051-76-1.mol | [Molecular Weight]
500.43 |
| Hazard Information | Back Directory | [Uses]
(-)-Halofantrine ((-)-SKF-102886 free base; (-)-WR-171669) is an inhibitor of the malignant malaria parasite (P. falciparum) and targets multidrug-resistant P. falciparum. The pharmacokinetic parameters of (-)-Halofantrine in rats vary depending on the route of administration, distinguishing it from other isomers[1]. | [Definition]
ChEBI: 3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthrenyl]-1-propanol is a member of phenanthrenes. | [in vivo]
Pharmacokinetic data from rats of Halofantrine HCl under fasting conditions[1]
| Route | Dose (mg/kg) | Compound | AUC0-∞ (mg·h/L) | Cl (mL/h/kg) | Vdss (L/kg) | Vdβ (L/kg) | t1/2 (h) | Cmax (ng/mL) | tmax (h) | | i.v. | 2; n=5 | (-)-Halofantrine | 5.02 | 199 | 3.22 | 4.64 | 16.8 | / | / | | (+)-Halofantrine | 9.06 | 113 | 2.38 | 3.13 | 20.8 | / | / | | (±)-Halofantrine | 14.1 | 143 | 3.53 | 3.60 | 18.0 | / | / | | p.o. | 14; n=5 | (-)-Halofantrine | 5.49 | / | / | / | 16.6 | 556 | 2.20 | | (+)-Halofantrine | 16.3 | / | / | / | 16.5 | 917 | 4.20 | | (±)-Halofantrine | 22.5 | / | / | / | 16.4 | 1420 | 3.60 |
| [References]
[1] Brocks DR, et al. Pharmacokinetics of halofantrine in the rat: stereoselectivity and interspecies comparisons. Biopharm Drug Dispos. 1999 Apr;20(3):165-9. DOI:10.1002/(sici)1099-081x(199904)20:3<165::aid-bdd170>3.0.co;2-z |
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