TABLE 3.

Human PK studies considered for model establishment and validation

Routea	Dose	Genotypeb	Measured biomarker(s)	Sample	Reference	Usec
i.v.	8.38, 9.87 mg · kg−1	FF, SS	INH, AcINH, INA, INAG	Blood, urine	30	E/V
i.v.	5 mg · kg−1	FF, FS, SS	INH, AcINH, INA, INAG	Blood, urine	31	E
i.v.	10 mg · kg−1	SS	INH, AcINH, AcHz, DiAcHz	Blood	32	E
p.o.	300 mg	FF, FS, SS	INH, AcINH	Blood	33	E/V
p.o.	300, 600, 900 mg	FF, FS	INH	Blood	34	V
p.o.	4.75, 4.68 mg · kg−1	FF, SS	INH, Hz	Blood	35	V
p.o.	300 mg	FF, SS	INH, AcHz	Blood	36	V
p.o.	300 mg	FF, SS	AcHz, DiAcHz	Blood	37	V
p.o.	300 mg	FF, SS	INH, AcINH, AzHz, DiAcHz	Blood	38	V
p.o.	5 mg · kg−1	FF, SS	INH, AcINH, INA, INAG	Urine	39	V
p.o.	20 mg · kg−1	FF, SS	INH, AcINH, INA, INAG, AcINH, DiAcHz	Urine	29	V

^ai.v., intravenous; p.o., oral.

^bFF, fast acetylator; FS, intermediate acetylator; SS, slow acetylator.

^cE, establishment; V, validation.