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In vitro study of the inhibition and induction of human cytochromes P450 by crystalline glucosamine sulfate.

Takafumi Akabane, Kohichiro Tanaka, Megumi Irie, Shigeyuki Terashita, and Toshio Teramura

Drug Metabol Drug Interact 24(2-4):195-209 (2009) PMID 20408500

The induction and inhibition of human hepatic cytochrome P450 (CYP) isoforms by crystalline glucosamine sulfate (CGS) was investigated in vitro. Inhibition of CYP1A2, CYP2E1, CYP2C19, CYP2C9, CYP2D6, and CYP3A4 by CGS was assessed using recombinant human enzymes incubated with CGS (up to 3 mM expressed as free base). Induction of CYP1A2, CYP2B6, CYP2C9, CYP2C19 and CYP3A4 by CGS (0.01, 0.3 and 3 mM) was evaluated in cryopreserved human hepatocytes, by determining CYP mRNA expression using quantitative RT-PCR. CGS produced no inhibition or induction of any the CYP enzymes tested at concentrations hundred folds higher than the steady state peak plasma concentrations (approximately 10 microM) observed in man after therapeutic doses of CGS of 1500 mg once a day. Therefore, no clinically relevant metabolic interactions are expected between CGS and co-administered drugs that are substrates of the CYP enzymes investigated.

DOI: 10.1515/DMDI.2009.24.2-4.195
Version: za2963e q8za7 q8zbc q8zc1 q8zdb q8ze7 q8zf7 q8zge

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