Halofantrine is a synthetic antimalarial active pharmaceutical ingredient (API) belonging to the phenanthrene methanol class of antimalarial compounds. It has been developed for the treatment of malaria caused by susceptible Plasmodium species. Halofantrine is structurally related to other aryl-amino-alcohol antimalarial compounds.
Halofantrine has the molecular formula C26H30Cl2F3NO and a molecular weight of approximately 500.42 g/mol. Its CAS Number is 69756-53-2.
Halofantrine is a lipophilic antimalarial compound that has activity against the erythrocytic stages of Plasmodium parasites. It has historically been used for the treatment of malaria, particularly infections caused by Plasmodium falciparum.
The compound is generally supplied as halofantrine hydrochloride for pharmaceutical formulation. The hydrochloride salt improves the handling and formulation characteristics of the active ingredient.
Halofantrine is believed to interfere with parasite processes associated with the digestion of hemoglobin and heme metabolism within infected erythrocytes. Its precise molecular mechanism is not completely established, but its antimalarial activity is associated with effects on the parasite's intraerythrocytic stages.
Halofantrine API has applications in:
Halofantrine is manufactured through controlled chemical synthesis followed by purification, drying and analytical quality testing.
Quality evaluation may include identity, assay, related substances, residual solvents, water content, residue on ignition and elemental impurities according to the applicable approved specification.
Halofantrine is generally described as a white to off-white crystalline solid. The compound is highly lipophilic and has very low water solubility. Pharmaceutical preparations commonly use the hydrochloride salt rather than the free base.
Halofantrine should be stored in a tightly closed container, protected from excessive moisture, heat and direct light. The manufacturer's current CoA, SDS and validated storage conditions should be followed.
Depending on grade and intended application, documentation may include:
Halofantrine is an established synthetic antimalarial pharmaceutical compound belonging to the phenanthrene methanol class. Its chemical identity, antimalarial activity and pharmaceutical history make it relevant for malaria-related pharmaceutical research and formulation development.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |
| Melting Point | Approximately 132–134°C |