PMID- 29368402
OWN - NLM
STAT- MEDLINE
DCOM- 20190619
LR  - 20240321
IS  - 2163-8306 (Electronic)
IS  - 2163-8306 (Linking)
VI  - 7
IP  - 3
DP  - 2018 Mar
TI  - Comprehensive PBPK Model of Rifampicin for Quantitative Prediction of Complex 
      Drug-Drug Interactions: CYP3A/2C9 Induction and OATP Inhibition Effects.
PG  - 186-196
LID - 10.1002/psp4.12275 [doi]
AB  - This study aimed to construct a physiologically based pharmacokinetic (PBPK) 
      model of rifampicin that can accurately and quantitatively predict complex 
      drug-drug interactions (DDIs) involving its saturable hepatic uptake and 
      auto-induction. Using in silico and in vitro parameters, and reported clinical 
      pharmacokinetic data, rifampicin PBPK model was built and relevant parameters for 
      saturable hepatic uptake and UDP-glucuronosyltransferase (UGT) auto-induction 
      were optimized by fitting. The parameters for cytochrome P450 (CYP) 3A and CYP2C9 
      induction by rifampicin were similarly optimized using clinical DDI data with 
      midazolam and tolbutamide as probe substrates, respectively. For validation, our 
      current PBPK model was applied to simulate complex DDIs with glibenclamide (a 
      substrate of CYP3A/2C9 and hepatic organic anion transporting polypeptides 
      (OATPs)). Simulated results were in quite good accordance with the observed data. 
      Altogether, our constructed PBPK model of rifampicin demonstrates the robustness 
      and utility in quantitatively predicting CYP3A/2C9 induction-mediated and/or OATP 
      inhibition-mediated DDIs with victim drugs.
CI  - (c) 2018 The Authors CPT: Pharmacometrics & Systems Pharmacology published by Wiley 
      Periodicals, Inc. on behalf of American Society for Clinical Pharmacology and 
      Therapeutics.
FAU - Asaumi, Ryuta
AU  - Asaumi R
AD  - Pharmacokinetic Research Laboratories, Ono Pharmaceutical Co., Ltd., Tsukuba, 
      Ibaraki, Japan.
FAU - Toshimoto, Kota
AU  - Toshimoto K
AD  - Sugiyama Laboratory, RIKEN Innovation Center, RIKEN, Yokohama, Kanagawa, Japan.
FAU - Tobe, Yoshifusa
AU  - Tobe Y
AD  - Pharmacokinetic Research Laboratories, Ono Pharmaceutical Co., Ltd., Tsukuba, 
      Ibaraki, Japan.
FAU - Hashizume, Kenta
AU  - Hashizume K
AD  - Drug Development Solutions Division, Sekisui Medical Co., Ltd., Ibaraki, Japan.
FAU - Nunoya, Ken-Ichi
AU  - Nunoya KI
AD  - Pharmacokinetic Research Laboratories, Ono Pharmaceutical Co., Ltd., Tsukuba, 
      Ibaraki, Japan.
FAU - Imawaka, Haruo
AU  - Imawaka H
AD  - Pharmacokinetic Research Laboratories, Ono Pharmaceutical Co., Ltd., Tsukuba, 
      Ibaraki, Japan.
FAU - Lee, Wooin
AU  - Lee W
AD  - College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul 
      National University, Seoul, Korea.
FAU - Sugiyama, Yuichi
AU  - Sugiyama Y
AD  - Sugiyama Laboratory, RIKEN Innovation Center, RIKEN, Yokohama, Kanagawa, Japan.
LA  - eng
PT  - Journal Article
DEP - 20180205
PL  - United States
TA  - CPT Pharmacometrics Syst Pharmacol
JT  - CPT: pharmacometrics & systems pharmacology
JID - 101580011
RN  - EC 1.14.13.- (CYP2C9 protein, human)
RN  - EC 1.14.13.- (Cytochrome P-450 CYP2C9)
RN  - EC 1.14.14.1 (CYP3A protein, human)
RN  - EC 1.14.14.1 (Cytochrome P-450 CYP3A)
RN  - EC 2.4.1.17 (Glucuronosyltransferase)
RN  - SX6K58TVWC (Glyburide)
RN  - VJT6J7R4TR (Rifampin)
SB  - IM
MH  - Computer Simulation
MH  - Cytochrome P-450 CYP2C9/*metabolism
MH  - Cytochrome P-450 CYP3A/*metabolism
MH  - Drug Interactions
MH  - Enzyme Induction/drug effects
MH  - Glucuronosyltransferase/metabolism
MH  - Glyburide/pharmacokinetics/pharmacology
MH  - Humans
MH  - Models, Biological
MH  - Rifampin/*pharmacokinetics/pharmacology
PMC - PMC5869557
EDAT- 2018/01/26 06:00
MHDA- 2019/06/20 06:00
PMCR- 2018/03/01
CRDT- 2018/01/26 06:00
PHST- 2017/10/02 00:00 [received]
PHST- 2017/12/27 00:00 [revised]
PHST- 2017/12/28 00:00 [accepted]
PHST- 2018/01/26 06:00 [pubmed]
PHST- 2019/06/20 06:00 [medline]
PHST- 2018/01/26 06:00 [entrez]
PHST- 2018/03/01 00:00 [pmc-release]
AID - PSP412275 [pii]
AID - 10.1002/psp4.12275 [doi]
PST - ppublish
SO  - CPT Pharmacometrics Syst Pharmacol. 2018 Mar;7(3):186-196. doi: 
      10.1002/psp4.12275. Epub 2018 Feb 5.