Summary for all probe drugs and inhibitors in cassette small dose clinical study
| Drugs | Enzyme/Transportera | Clinical Dose (mg) | Used dose (mg) (Single Oral) |
|---|---|---|---|
| Cassette of probe substrates | |||
| Pitavastatin | OATP1B1 | 1 ∼ 4b | 0.2 |
| Pioglitazone | CYP2C8 | 15 ∼ 30c | 1 |
| Repaglinide | OATP1B1/CYP2C8 | 0.25 ∼ 1d | 0.1 |
| Inhibitors | |||
| Rifampicin | OATPs | 450 ∼ 600e | 600 |
| Trimethoprim | CYP2C8 | 80 ∼ 320f | 200 |
| Clopidogrel | OATP1B1/CYP2C8 | 75 ∼ 300g | 300 |
↵a Elimination pathway for drug-drug interaction in this study
↵b FDA (2009) Drug approval package: LIVALO (pitavastatin calcium), FDA application No., (NDA) 022363
↵c FDA (1999) Drug approval package: ACTOS (pioglitazone hydrochloride), FDA application No., (NDA) 021073
↵d PMDA (2016) Interview Form: SUREPOST (repaglinide) (https://www.pmda.go.jp/PmdaSearch/iyakuDetail/ResultDataSetPDF/430574_6164001M1216_1_07)
↵e RIFADIN (rifampicin) JAPAN PMDA drug label, revised April 2015; Daiichi-Sankyo Co. Accessed via PMDA website (www.pmda.go.jp) on April 13, 2016.
↵f Baktar (sulfamethoxazole and trimethoprim) JAPAN PMDA drug label, revised February 2014; Shionogi & Co. Accessed via PMDA website (www.pmda.go.jp) on April 13, 2016.
↵g Plavix (clopidogrel bisulfate) JAPAN PMDA drug label, revised March 2016; Sanifi. Accessed via PMDA website (www.pmda.go.jp) on April 13, 2016.