Biliary excretion of imatinib mesylate and its metabolite CGP 74588 in humans.
Pharmacotherapy
; 24(9): 1232-5, 2004 Sep.
Article
em En
| MEDLINE
| ID: mdl-15460185
ABSTRACT
Imatinib mesylate, licensed to treat chronic myelogenous leukemia and gastrointestinal stromal tumors, is metabolized by cytochrome P450 3A and undergoes little renal excretion, but its biliary excretion by humans is uncharacterized. Liquid chromatography-mass spectrometry was used to quantitate imatinib and its metabolite CGP 74588 in the bile of two patients with biliary stents; the ratio of imatinibCGP 74588 in each was approximately 91. In the first patient, who was receiving long-term therapy with imatinib 400 mg/day and had normal liver function tests, biliary imatinib accounted for 17.7% of the daily dose and CGP 74588 accounted for 2.1%. In the second patient, who had elevated liver function tests and was studied after his first dose of imatinib 300 mg, biliary imatinib accounted for only 1.8% of the daily dose and CGP 74588 accounted for 0.2%. These data show both the qualitative similarities and the quantitative variability in biliary excretion of imatinib and its principal metabolite.
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Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Pirimidinas
/
Bile
/
Adenocarcinoma
/
Tumores do Estroma Gastrointestinal
/
Antineoplásicos
Tipo de estudo:
Qualitative_research
Limite:
Adult
/
Humans
/
Male
/
Middle aged
Idioma:
En
Ano de publicação:
2004
Tipo de documento:
Article