CAS Number: 69756-53-2
Halofantrine
Halofantrine is an antimalarial drug that is primarily used for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum. It belongs to the class of drugs known as arylamino-alcohols and works by inhibiting the growth and replication of the malaria parasite. In addition to its use in the treatment of malaria, halofantrine has also been investigated for its potential use in the treatment of other parasitic infections, such as schistosomiasis and filariasis. However, more research is needed to determine its efficacy in these areas.
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References
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Mechanistic Oral Absorption Modeling of Halofantrine: Exploring the Role of Intestinal Lymphatic Transport
This literature describes the development of a mechanistic physiologically-based pharmacokinetic (PBPK) model using halofantrine, a highly lipophilic antimalarial drug, to explore the role of intestinal lymphatic transport in oral absorption. Using the Simcyp simulator with the multi-layer gut wall (M-ADAM) model, the authors successfully incorporated lymphatic absorption into the PBPK framework, validating the model with in vitro data and clinical pharmacokinetic studies. The final model adequately captured halofantrine’s pharmacokinetics in the fasted state and the food effect on total exposure, although it slightly underpredicted the food effect on peak exposure, potentially due to transient postprandial changes in protein binding. In the fed state, the model simulated that 26% of the absorbed fraction occurred via the lymph, accounting for 62% of the increase in absorption due to food. This work demonstrates that PBPK modeling can mechanistically describe oral absorption involving intestinal lymphatic transport, offering improved understanding for lipophilic drugs that evade hepatic first-pass metabolism.
DOI: 10.1016/j.xphs.2020.12.023