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The molecular mechanism underlying the induction of hepatic MRP3 expression and function by omeprazole
This study aimed to assess changes in fold‐induction of MRP3 mRNA and protein expression over controls in omeprazole‐treated HepG2 cells after transient transfection of human MRP3 siRNA, or after pretreatment of actinomycin D (Act‐D). Furthermore, MRP3 siRNA knock‐down or MRP‐specific inhibition (indomethacin) was used to determine whether induced MRP3 protein by omeprazole could possess enhanced efflux transport. The results demonstrated that omeprazole induced MRP3 mRNA and protein expression in a concentration‐ and time‐dependent manner. Moreover, that induction was almost completely abolished by addition ...
Source: Biopharmaceutics and Drug Disposition - December 1, 2014 Category: Drugs & Pharmacology Authors: Yu‐Qin Pan, Qiong‐Yu Mi, Bang‐Shun He, Shu‐Li Zhao, Ting Tai, Hong‐Guang Xie Tags: Original Paper Source Type: research

Dealing with the complex drug‐drug interactions: towards mechanistic models
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - December 1, 2014 Category: Drugs & Pharmacology Authors: Manthena V. Varma, K. Sandy Pang, Nina Isoherranen, Ping Zhao Tags: Invited Review Source Type: research

Screening of non‐steroidal anti‐inflammatory drugs for inhibitory effects on the activities of six UDP‐glucuronosyltransferases (UGT1A1, 1A3, 1A4, 1A6, 1A9, and 2B7) using LC‐MS/MS
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - December 1, 2014 Category: Drugs & Pharmacology Authors: Jeongmin Joo, Yang‐Weon Kim, Zhexue Wu, Jung‐Hoon Shin, Boram Lee, Jong Cheol Shon, Eun Young Lee, Nguyen Minh Phuc, Kwang‐Hyeon Liu Tags: Short Communication Source Type: research

Human pharmacokinetic profiling of the dipeptidyl peptidase‐IV inhibitor teneligliptin using physiologically based pharmacokinetic modeling
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - November 28, 2014 Category: Drugs & Pharmacology Authors: Yoshinobu Nakamaru, Chie Emoto, Makiko Shimizu, Hiroshi Yamazaki Tags: Original Paper Source Type: research

Absorption, distribution, metabolism and excretion of novel phosphodiesterase type 4 inhibitor ASP3258 in rats
ABSTRACT The potent and selective phosphodiesterase 4 inhibitor ASP3258 is a novel therapeutic agent for asthma and chronic obstructive pulmonary disease (COPD). After a single oral administration to rats, ASP3258 is rapidly absorbed with a bioavailability of 106%. In situ absorption data indicated that ASP3258 is mainly absorbed in the small intestine. Tissue distribution data after oral administration of 14C‐ASP3258 showed rapid and extensive distribution to various tissues. Excluding the gastrointestinal tract, the tissues with the highest concentrations were liver, heart and plasma. Liquid chromatography‐nuclear ma...
Source: Biopharmaceutics and Drug Disposition - November 22, 2014 Category: Drugs & Pharmacology Authors: Yoshiaki Ohtsu, Takuya Sonoda, Yoko Susaki, Toshifumi Tohda, Yasuhisa Fukunaga, Takafumi Iwatsubo, Kiyoshi Noguchi Tags: Original Paper Source Type: research