Some inducers of CYP2C8 in vitro
| Inducer | Therapeutic Use and/or Drug Class | CYP2C8 mRNA | CYP2C8 Protein in Hepatocytes | CYP2C8 Activity in Hepatocytes | References |
|---|---|---|---|---|---|
| CITCO | 2.5-fold in primary hepatocytes | Ferguson et al., 2005 | |||
| 1-fold in primary hepatocytes | Thomas et al., 2015 | ||||
| Clofibric acid | Antihyperlipidemic | 2-to 3-fold in primary hepatocytes | Prueksaritanont et al., 2005 | ||
| Cyclophosphamide | Anticancer, alkylating agent | + | Chang et al., 1997 | ||
| Dexamethasone | Anti-inflammatory, glucucortidcoid | + | Chang et al., 1997 | ||
| 3-fold in primary hepatocytes | 2-fold | Gerbal-Chaloin et al., 2001 | |||
| 5-fold in primary hepatocytes | 4-fold | Raucy et al., 2002 | |||
| <2-fold in primary hepatocytes | Ferguson et al., 2005 | ||||
| Fenofibric acid | Antihyperlipidemic | 2- to 6-fold in primary hepatocytes | Prueksaritanont et al., 2005 | ||
| Gemfibrozil | Antihyperlipidemic, PPARα agonist | 1.1- to 5-fold in primary hepatocytes | Prueksaritanont et al., 2005 | ||
| Hyperforin | Constituent of St. John’s wort | + in primary hepatocytes | Dussault et al., 2001 | ||
| 5-fold in primary hepatocytes | Ferguson et al., 2005 | ||||
| + | Komoroski et al., 2005 | ||||
| Idelalisib | Anticancer, PKI | 3.9-fold in human hepatocytes | FDA, 2014h | ||
| Idelalisib metabolite GS-563117 | Drug metabolite | 1.4-fold in human hepatocytes | FDA, 2014h | ||
| Ifosfamide | Anticancer, alkylating agent | + | Chang et al., 1997 | ||
| Lithocholic acid | Bile acid | <2-fold in primary hepatocytes | Ferguson et al., 2005 | ||
| Nelfinavir | Antiviral, protease inhibitor | 5-fold in primary hepatocytes | 2-fold | Dixit et al., 2007 | |
| Nilotinib | Anticancer, PKI | No induction of CYP2C8 mRNA | >2-fold | FDA, 2007c | |
| Paclitaxel | Anticancer, taxane | 4-fold in primary hepatocytes | Ferguson et al., 2005 | ||
| + in primary hepatocytes | Synold et al., 2001 | ||||
| Phenobarbital | Antiepileptic, barbiturate | + | Chang et al., 1997 | ||
| 3-fold in primary hepatocytes | 3-fold | Gerbal-Chaloin et al., 2001 | |||
| 7-fold in primary hepatocytes | Raucy et al., 2002 | ||||
| 3- to 6-fold | Madan et al., 2003 | ||||
| 2-fold in primary hepatocytes | Ferguson et al., 2005 | ||||
| Phenytoin | Antiepileptic | 2-fold in primary hepatocytes | Ferguson et al., 2005 | ||
| Progesterone | Hormonal replacement therapy | 1.4- to 9.2-fold in primary hepatocytes | Choi et al., 2013 | ||
| Rifampin (rifampicin) | Antibiotic | + | Chang et al., 1997 | ||
| 6-fold in primary hepatocytes | 3-fold | Gerbal-Chaloin et al., 2001 | |||
| 6.5-fold in primary hepatocytes | Rae et al., 2001 | ||||
| + in primary hepatocytes | Dussault et al., 2001 | ||||
| + in primary hepatocytes | Synold et al., 2001 | ||||
| 7- to 12-fold in primary hepatocytes | 6-fold (1- to 17-fold) | Raucy et al., 2002 | |||
| 4- to 8-fold in primary hepatocytes | Madan et al., 2003 | ||||
| 3-fold in primary hepatocytes | 3- to 10-fold | Ferguson et al., 2005 | |||
| 4- to 9-fold in primary hepatocytes | Prueksaritanont et al., 2005 | ||||
| 7-fold in primary hepatocytes | 4-fold | Dixit et al., 2007 | |||
| 6.5-fold in primary hepatocytes | Rana et al., 2010 | ||||
| 0.7- to 3-old in primary hepatocytes | Yajima et al., 2014 | ||||
| 5-fold in HepaRG cells | Thomas et al., 2015 | ||||
| Ritonavir | Antiviral, protease inhibitor | + in primary hepatocytes | Dussault et al., 2001 | ||
| + in primary hepatocytes | Synold et al., 2001 | ||||
| 7-fold in primary hepatocytes | 2-fold | Dixit et al., 2007 | |||
| SR12813 | Antihyperlipidemic, HMG-CoA reductase inhibitor | + in primary hepatocytes | Synold et al., 2001 | ||
| Tasimelteon | Circadian regulator | 4.4-fold | FDA, 2014m | ||
| WY14,643 | Antihyperlipidemic,PPARα agonist | 4-fold in HepaRG cells | Thomas et al., 2015 |
CITCO, [6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl)oxime; HMG-CoA, 3-hydroxy-3-methylglutaryl-coenzyme A; PKI, protein kinase inhibitor, HepaRG, hepatocyte-like cells from the human hepatoma HepaRG cell line; mRNA, messenger RNA; PPAR, peroxisome proliferator-activated receptor; SR12813, tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate; WY14,643, 4-Chloro-6-(2,3-xylidino)-2-pyrimidinylthioacetic acid.