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QuickView for Halofantrine (compound)


PubChem
Name: halofantrine
PubChem Compound ID: 37392
Molecular formula: C26H31Cl3F3NO
Molecular weight: 536.884 g/mol
Synonyms:
1,3-Dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)phenanthren-1-methanol hydrochloride; Halfan (TN); 9-Phenanthrenemethanol, 1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-, hydrochloride; 1-(1,3-Dichloro-6-trifluoromethyl-9-phenanthryl)-3-(di-n-butylamino)propanol hydrochloride; Halfan; 1,3-Dichloro-6-trifluoromethyl-9-(3-(dibutylamino)-1-hydroxypropyl)phenanthrene HCl; Halofantrino [Spanish]; 36167-63-2; 1,3-Dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-9-phenanthrenemethanol hydrochloride; 106927-11-1.
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DrugBank
Identification
Name: halofantrine
Name (isomeric): DB01218
Drug Type: small molecule
Synonyms:
Halofantrinum [INN-Latin]; Halofantrine [Usan]; Halofantrina [INN-Spanish]
Brand: Halfan
Category: Antimalarials, Antiprotozoals
CAS number: 69756-53-2
Pharmacology
Indication: For treatment of Severe malaria
Pharmacology: Halofantrine is a synthetic antimalarial which acts as a blood schizonticide. It is effective against multi drug resistant (including mefloquine resistant) P. falciparum malaria.
Mechanism of Action: The mechanism of action of Halofantrine may be similar to that of chloroquine, quinine, and mefloquine; by forming toxic complexes with ferritoporphyrin IX that damage the membrane of the parasite.
Protein binding: 60-70%;
Biotransformation: Hepatic
Half Life: 6-10 days
Toxicity: Side effects incldue coughing noisy, rattling, troubled breathing, loss of appetite, aches and pain in joints, indigestion,and skin itching or rash.
Affected organisms: Plasmodium
Interactions
Food interaction:
Take on an empty stomach, bioavailability is 6 times higher when drug is taken with high fat meals. Risks of cardiac toxicity are then increased.
Drug interaction:
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
ThioridazineIncreased risk of cardiotoxicity and arrhythmias
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
BicalutamideCYP3A4 Inhibitors like bicalutamide may increase the serum concentration of halofantrine. Extreme caution, with possibly increased monitoring of cardiac status (e.g., ECG), should be used with concurrent use of halofantrine with any moderate CYP3A4 inhibitor(s).
ClotrimazoleCYP3A4 Inhibitors (Moderate) such as clotrmazole may increase the serum concentration of halofantrine. Extreme caution, with possibly increased monitoring of cardiac status (e.g., ECG), should be used with concurrent use of halofantrine with any moderate CYP3A4 inhibitor(s).
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