Table 3.

List of Drugs and Drug Metabolites with C_max,u/K_i Values ≥ 0.1.

Compound	Cmax (μM)	Unbound Fraction 100, %	Cmax,u (μM)	Ki(OAT1) (μM)	Cmax,u/Ki(OAT1)	Ki(OAT3) (μM)	Cmax,u/Ki(OAT3)
Sulindac	32.0a	6.78%a	2.24	56.8	0.039	1.65	1.36
Sulindac sulfide	22.6a	6.01%a, 4.6%b	0.14e1.5b	3.68	0.038e0.408	0.66	0.212e2.27
Sulindac sulfone	4.48a	2.1%b	0.1e0.4b	23.0	0.004e0.017	0.60	0.167e0.667
Losartan	0.814e1.44c	1.4%d	0.011e0.02	11.4	0.00096e0.0018	0.36	0.03e0.056
Losartan carboxylic acid	0.554e1.13c	1%d,e	0.005e0.011	0.69	0.007e0.016	0.10	0.05e0.11
Abiraterone	0.37f	<1%e	0.0037	>20	NA	>20	NA
Abiraterone sulfate	25f	<0.15%e	0.25	38.2	0.0065	1.83	0.137
Abiraterone N-oxide sulfate	9.2f	0.22%e	0.092	>100	NA	1.36	0.068

Values ≥ 0.1 are highlighted in bold.

NA: Not available.

^ahttps://doi.org/10.1002/j.1552–4604.1993.tb04699.x.

^bhttps://doi.org/10.1124/jpet.110.165852.

^chttps://doi.org/10.1111/j.1365–2710.2011.01279.x.

^dDrugbank (https://www.drugbank.ca/drugs/DB00678).

^eAccording to FDA guidance (https://www.fda.gov/media/108130/download), the unbound fraction should be set to 1% if experimentally determined to be less than 1%.

^fhttps://doi.org/10.1002/cpdd.132.