TABLE 1

Human pharmacokinetic properties, metabolizing enzymes, and transporters of probes tested in this study

Probe for:	BCRP		P-gp			CYP3A
Probe for:	Sulfasalazine	Rosuvastatin	Fexofenadine	Talinolol	Aliskiren	Midazolam
Absolute oral bioavailability	Less than 15%	About 20%	35%	55% ± 22%	About 2.5%	About 35%
Plasma protein binding	>99.3%	88%	60%–70%	78%–79% for serum	47%–51%	96.5%
Metabolism	Degraded by intestinal bacteria	Limited	Limited	Limited	Limited	Extensive
Metabolizing enzyme	−	CYP2C9	−	CYP3A4	CYP3A4	CYP3A4
Substrate of:
BCRP	Yes	Yes	No	No	No	No
P-gp	No	No	Yes	Yes	Yes	No
OATP1A2	−	Yes	Yes	Yes	Yes	−
OATP1B1	−	Yes	Yes	−	−	No
OATP1B3	−	Yes	Yes	−	−	No
OATP2B1	Yes	Yes	Yes	Yes	Yes	−
References:	https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/007073s128lbl.pdf; Kusuhara et al. (2012)	https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-366_Crestor.cfm; Kalliokoski and Niemi (2009)	https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/020872s018,021963s002lbl.pdf; Kalliokoski and Niemi (2009), Lappin et al. (2010)	Trausch et al. (1995), Zschiesche et al. (2002), Shirasaka et al. (2010)	Vaidyanathan et al. (2008), Tapaninen et al. (2011), Rebello et al. (2012)	https://www.accessdata.fda.gov/drugsatfda_docs/nda/98/020942_versed_toc.cfm; Maeda (2015)