TABLE 1

In vitro input parameters of efavirenz

Physicochemical	Value	Reference	CL_int from HLMs (Pathway)		CL_int from rhCYP (Pathway)
			µl/min/mg protein	µl/min/mg protein	µl/min/pmol P450	µl/min/pmol P450
MW	315.67		CYP2B61/1 (8-OH)^{^a}	14.5	CYP2B6.1 (8-OH)^{^a}	0.39
LogP	4.6	(Siccardi et al., 2012)	CYP2B61/6 (8-OH)^{^a}	6.4	CYP2B6.6 (8-OH)^{^a}	0.19
B/P ratio	0.74	(Balani et al., 1999)	CYP2B66/6 (8-OH)^{^a}	2.4	CYP2A6 (7-OH)^{^b}	0.05
f _u,plasma	0.029	(Shou et al., 2008)	CYP2B61/1 (7-OH)^{^c}	1.1	CYP2A6 (8-OH)^{^b}	0.08
f_umic	0.30	(Rekic et al., 2011)	CYP2B61/6 (7-OH)^{^c}	1.5	CYP3A4 (8-OH)^{^d}	0.007
Plasma binding protein	Albumin		CYP2B66/6 (7-OH)^{^c}	1.3	CYP3A5 (8-OH)^{^d}	0.03
Caco-2 permeability (10⁻⁵ cm/s)	8.92	(Takano et al., 2006)			CYP1A2 (8-OH)^{^d}	0.07

↵^a Data from Xu, et al. (2012).
↵^b Data from Ogburn, et al. (2010).
↵^c Data from the present study.
↵^d Data from Ward, et al. (2003).