TABLE 3

Scaled and observed CL of clinical acrylamide covalent inhibitors in human and rat

Drug	Species	CLh int	CLb int, u	Scaled CLb	Observed CLb
		µl/min/10⁶cells	µl/min/g	ml/min/kg
Canertinib (CI-1033)	Human	12	733	14	8.4^{^a}
	Rat	49	822	84	29^b
Ethacrynic acid	Human	13	925	27	21^c
Ibrutinib (PCI-32765)	Human	130	142	21	20^d
	Rat	147	56	35	47^e

↵^a Canertinib mean human CLp: CL = 15 ml/min/kg (Simon et al., 2006); fup = 0.01; fu mic = 0.14; BPR = 1.8.
↵^b Canertinib mean rat CLp = 40 ml/min/kg (Gonzales et al., 2008); fup = 0.01; fu mic = 0.29; BPR = 1.4.
↵^c Ethacrynic acid mean human CLp = 8.7 ml/min/kg (Lacreta et al., 1994); fup = 0.006; fu mic = 0.75; BPR = 0.41.
↵^d Ibrutinib mean human CLp = 14.6 ml/min/kg (de Vries et al., 2016); fup = 0.024; fu mic = 0.31; BPR = 0.75.
↵^e Ibrutinib mean rat CLp = 34 ml/min/kg (Shibata and Chiba, 2015); fup = 0.016; fu mic = 0.53; BPR = 0.72; n = 2 for CL hint, u and CLb int, u assessments.