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 |
![9-Phenanthrenemethanol, 1,3-dichloro-α-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-, (-)- Structure](https://www.chemicalbook.com/CAS/20211123/GIF/66051-76-1.gif)
