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Drug-Target Interaction

Drug

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PubChem ID:37393
Structure:
Synonyms:
(1)-Halofantrine
1,3-Dichloro-.alpha.-[2-(dibutylamino)ethyl]-6- (trifluoromethyl)-9-phenathrenemethanol
1,3-Dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-9-phenanthrene-methanol
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propa
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol
36167-63-2 (HYDROCHLORIDE)
69756-53-2
9-Phenanthrenemethanol, 1,3-dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-
9-Phenanthrenemethanol, 1,3-dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-(1)
AB00514703
AIDS-008015
AIDS008015
BPBio1_001366
BSPBio_001241
C07634
DB01218
dl-WR 171669
Halofantrina [Inn-Spanish]
Halofantrine
Halofantrine [Usan]
Halofantrinum [Inn-Latin]
LS-187198
NCGC00179250-01
NCI60_002593
Prestwick0_001031
Prestwick1_001031
Prestwick2_001031
Prestwick3_001031
SPBio_003092
ATC-Codes:
Side-Effects:
Side-EffectFrequency
dysrhythmias0.0010
anaphylactic reactions0.0010
edema0.0010
hemolytic anemia0.0010
urticaria0.0010
pulmonary edema0
pruritus0
paresthesia0
abdominal distention0
palpitations0
nausea0
stomatitis0
cerebrovascular accident0
tetany0
tinnitus0
abnormal vision0
vomiting0
malaise0
myalgia0
urinary frequency0
postural hypotension0
headache0
fatigue0
abdominal pain0
anemia0
anorexia0
arthralgia0
asthenia0
back pain0
chest pain0
confusion0
constipation0
convulsions0
cough0
diarrhea0
dizziness0
dyspepsia0
rash0
sleep disorder0

Target

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Uniprot ID:Q38LG2_HUMAN
Synonyms:
Cytochrome P450 2D6
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

8554939
An investigation of the interaction between halofantrine, CYP2D6 and CYP3A4: studies with human liver microsomes and heterologous enzyme expression systems.. R C Halliday; B C Jones; D A Smith; N R Kitteringham; B K Park (1995) British journal of clinical pharmacology display abstract
1. We have assessed the interaction of the antimalarial halofantrine with cytochrome P450 (CYP) enzymes in vitro, with the use of microsomes from human liver and recombinant cell lines. 2. Rac-halofantrine was a potent inhibitor (IC50 = 1.06 microM, Ki = 4.3 microM) of the 1-hydroxylation of bufuralol, a marker for CYP2D6 activity. Of a group of structurally related antimalarials tested, only quinidine (IC50 = 0.04 microM) was more potent. 3. Microsomes prepared from recombinant CYP2D6 and CYP3A4 cell lines were shown to catalyse halofantrine N-debutylation. 4. The metabolism of halofantrine to its N-desbutyl metabolite by human liver microsomes showed no correlation with CYP2D6 genotypic or phenotypic status and there was no consistent inhibition by quinidine. 5. The rate of halofantrine metabolism showed a significant correlation with both CYP3A4 protein levels (r = 0.88, P = 0.01) and the rate of felodipine metabolism (r = 0.86, P = 0.013), a marker substrate for CYP3A4 activity. Inhibition studies showed that ketoconazole is a potent inhibitor of halofantrine metabolism (IC50 = 1.57 microM). 6. In conclusion, we have demonstrated that halofantrine is a potent inhibitor of CYP2D6 in vitro and can also be metabolised by the enzyme. However, in human liver microsomes it appears to be metabolised largely by CYP3A4.