Detailed Information

Cited 18 time in webofscience Cited 19 time in scopus
Metadata Downloads

Pharmacokinetics of Oltipraz and Its Major Metabolite (RM) in Patients With Liver Fibrosis or Cirrhosis: Relationship With Suppression of Circulating TGF-beta 1

Authors
Kim, S. G.Kim, Y. M.Choi, Y. H.Lee, M. G.Choi, J. Y.Han, J. Y.Cho, S. H.Jang, J. W.Um, S. H.Chon, C. Y.Lee, D. H.Jang, J. J.Yu, E. S.Lee, Y. S.
Issue Date
Sep-2010
Publisher
WILEY
Citation
CLINICAL PHARMACOLOGY & THERAPEUTICS, v.88, no.3, pp 360 - 368
Pages
9
Indexed
SCI
SCIE
SCOPUS
Journal Title
CLINICAL PHARMACOLOGY & THERAPEUTICS
Volume
88
Number
3
Start Page
360
End Page
368
URI
https://scholarworks.korea.ac.kr/kumedicine/handle/2020.sw.kumedicine/14583
DOI
10.1038/clpt.2010.89
ISSN
0009-9236
1532-6535
Abstract
Oltipraz is a potential candidate drug for the treatment of liver fibrosis (LF) and liver cirrhosis (LC). The pharmacokinetics of oltipraz and its major rearranged metabolite (7-methyl-6,8-bis(methylthio) H-pyrrolo[1,2-a]pyrazine (RM)) were evaluated after single-dose (30-90 mg) and multiple-dose (60 mg b.i.d. or 90 mg q.d. for 24 weeks) oral administration of oltipraz to patients with LF or LC. Oltipraz was safe and well tolerated in both studies. In the single-dose study, the area under the plasma concentration-time curve (AUC), peak plasma concentration (C-max), and terminal half-life (t(1/2)) of oltipraz as well as the AUC of its RM were dose dependent. Oltipraz was rapidly absorbed; the time to reach C-max (T-max) was 2-4 h. The conversion of oltipraz to RM was also rapid and substantial (AUC of RM from time 0 to the last measured concentration (AUC(last,RM))/AUC(last,oltipraz') 42-61%). In the multiple-dose study, the level of transforming growth factor-beta 1 (TGF-beta 1) (a blood fibrosis marker) was suppressed at steady-state plasma concentrations of similar to 20-60 ng/ml of oltipraz or of similar to 60-140 ng/ml of oltipraz plus RM. Overall, the pharmacokinetics, safety, and efficacy of oltipraz suggest that it may be helpful in the treatment of patients with LF or LC, at an optimal dosing regimen.
Files in This Item
There are no files associated with this item.
Appears in
Collections
2. Clinical Science > Department of Gastroenterology and Hepatology > 1. Journal Articles

qrcode

Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.

Altmetrics

Total Views & Downloads

BROWSE