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Drug-Target Interaction

Drug

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PubChem ID:34698
Structure:
Synonyms:
(5R-(5alpha,5abeta,8aalpha,9beta(R*)))-5,8,8a,9-Tetrahydro-5-(4-hydroxy-3,5-dimethoxyphenyl)-9-((4-6-O-(2-thienylmethylene)-beta-D-glucopyranosyl)oxy)furo(3',4':6,7)naphtho(2,3-d)-1,3-dioxol-6(5aH)-one
23362-13-2
29767-20-2
31514-29-1
35317-44-3
4'-Demethyl
4'-Demethyl 1-O-(4,6-O,O-(2-thenylidene)-beta-D-glucopyranosyl)epipodophyllotoxin
4'-Demethyl-epipodophyllotoxin-beta-D-thenylidene-glucoside
4'-Demethylepipodophyllotoxin 9-(4,6-O-(R)-2-thenylidene-beta-D-glucopyranoside)
4'-Demethylepipodophyllotoxin 9-(4,6-O-2-thenylidene-beta-D-glucopyranoside)
4'-Demethylepipodophyllotoxin-beta-D-thenylidine glucoside
4'-Dimethyl-9-(4,6-O-2-thenyid)-epipodophyllotoxin
AC1L1S3X
CCRIS 2058
DB00444
EINECS 249-831-2
Epipodophyllotoxin, 4'-demethyl-, 9-(4,6-O-2-thenylidene-beta-D-glucopyranoside)
Epipodophyllotoxin, 4'-demethyl-, 9-(4,6-O-2-thenylidene-beta-D-glucopyranoside) (8CI)
Epipodophyllotoxin-beta-D-thenylidene-glucoside, 4'-demethyl-
EPT
Furo(3',4':6,7)naphtho(2,3-d)-1,3-dioxol-6(5aH)-one, 5,8,8a,9-tetrahydro-5-(4-hydroxy-3,5-dimethoxyphenyl)-9-((4,6-O-((R)-2-thienylmethylene)-beta-D-glucopyranosyl)oxy)-, (5R,5aR,8aR,9S)-
HSDB 6546
NSC 122819
NSC-122819
TENIPOSIDE
Teniposide [USAN:BAN:INN]
Teniposido
Teniposido [INN-Spanish]
Teniposidum
Teniposidum [INN-Latin]
UNII-957E6438QA
Vee M-26
Veham-Sandoz
Vehem
VM-26
Vumon
ATC-Codes:
Side-Effects:
Side-EffectFrequency
abdominal pain0
hypotension0
infection0
leukemia0
aml0
leukopenia0
nausea0
tumor0
neutropenia0
pruritus0
stomatitis0
sweating0
tachycardia0
thrombocytopenia0
urticaria0
vomiting0
chills0
neuropathy0
hypertension0
hypersensitivity0
hemorrhage0
alopecia0
anemia0
hemolytic anemia0
anorexia0
arrhythmia0
asthenia0
brain tumor0
bronchospasm0
cancer0
confusion0
diarrhea0
dyspnea0
edema0
rash0
fever0
flushing0
headache0
allergic reaction0

Target

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Uniprot ID:CP3A4_HUMAN
Synonyms:
Albendazole monooxygenase
Albendazole sulfoxidase
CYPIIIA3
CYPIIIA4
Cytochrome P450 3A3
Cytochrome P450 3A4
HLp
NF-25
Nifedipine oxidase
P450-PCN1
Quinine 3-monooxygenase
Taurochenodeoxycholate 6-alpha-hydroxylase
EC-Numbers:1.14.13.32
1.14.13.67
1.14.13.97
Organism:Homo sapiens
Human
PDB IDs:1TQN 1W0E 1W0F 1W0G 2J0D 2V0M
Structure:
2V0M

Binding Affinities:

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

References:

11770832
Screening for inhibitory effects of antineoplastic agents on CYP3A4 in human liver microsomes.. M Baumhäkel; D Kasel; R A Rao-Schymanski; R Böcker; K T Beckurts; M Zaigler; D Barthold; U Fuhr (2001) International journal of clinical pharmacology and therapeutics display abstract
BACKGROUND: The human cytochrome P450 enzyme CYP3A4 is involved in the metabolism of many anticancer drugs. Since these drugs are usually administered in a polychemotherapy regimen, the objective of this study was to examine their inhibitory potency on CYP3A4 with regard to possible mutual drug interactions. METHOD: CYP3A4 activities in human liver microsomes from 2 donors were determined using the oxidation of the dihydropyridine denitronifedipine, a specific CYP3A4 substrate, at a concentration of 50 microM (= KM). Formation of the pyridine metabolite was measured using HPLC. Inhibitor concentrations used were 0.5, 5 and 50 microg/ml, except for cyclophosphamide and ifosfamide (0.5, 2.5 and 5 mg/ml) and for paclitaxel (0.05, 0.15, 0.5, 1.5 and 5 microg/ml). RESULTS: The following substances showed an inhibitory effect on CYP3A4 (IC50 values for the 2 microsome samples are parenthesized): cyclophosphamide (12.3/9.2 mmol/l), mafosfamide generated 4-OH-cyclophosphamide (152/163 [micromol/l), ifosfamide (3.6/2.5 mmol/l), vinblastine sulfate (20/44 micromol/l), vincristine sulfate (67/176 micromol/l), daunorubicin hydrochloride (206/200 micromol/l), doxorubicin hydrochloride (160/215 micromol/l), teniposide (64/84 micromol/l) and docetaxel (6.4/12.7 micromol/l). No inhibitory effect on CYP3A4 was observed with epirubicin, etoposide, paclitaxel, cytarabine, 5-FU, 6-mercaptopurine, methotrexate, cisplatin, carboplatin, bleomycin, busulfan, chlorambucil and mitomycin. CONCLUSION: Comparing IC50 values with plasma concentrations present during antineoplastic therapy, the agents cyclophosphamide, ifosfamide, vinblastine, teniposide and docetaxel could possibly cause clinical drug interactions by inhibition of CYP3A4. Some recently described clinical interactions with antineoplastic agents may be explained by these results.
8114683