TABLE 1

Summary of structure and disposition pathways of the four probe compounds

CompoundsStructureIndicationRoutes of Clearance in Human
APGraphicNot applicableCytochrome P450–mediated oxidative metabolism by 1A2, 2B6, 2C8, 2C9, 2C18, and 3A4 (Balani et al., 2002)
RTGGraphicAnti-HIVPhase II glucuronidation by UGT1A1 (Kassahun et al., 2007; Liu et al., 2019)
3TCGraphicAnti-HIVActive transport and renal clearance by MDR1, MRP1, MRP2, MRP3, MRP4, and BCRP (Johnson et al., 1999)
ICGGraphicMedical diagnosticsTransported by OATP1B3 and NTCP (de Graaf et al., 2011). Clearance route for ICG is unclear (Huang and Vore, 2001; Hwang et al., 2017).
  • BCRP, breast cancer resistance protein; HIV, human immunodeficiency virus; MDR1, multidrug resistance mutation 1; MRP, multidrug resistance-associated protein; NTCP, sodium taurocholate cotransporting polypeptide; OATP1B3, organic anion transporter family 1 member B3; UGT1A1, UDP (uridine diphosphate) glucuronosyltransferase family 1 member A1.