TABLE 2

Kinetic parameters (E_max – E₀, IC₅₀) derived for inhibition of CGamF (1 μM) accumulation in SCRH by the HIV PIs APV, ATV, SQV, RTV, and DRV Literature values for maximum unbound plasma concentrations (C_{max, unbound}) as observed in patients dosed with these PIs are also given.

Inhibitors	E_max – E_o^a	E_max – E_o	IC₅₀	Plasma Protein Binding^*	C_max Corrected for Plasma Protein Binding^**
	pmol/mg protein/10 min	% of E_max	μM	%	μM
APV	188 ± 16	64 ± 6	43 ± 12	90	1.01–3.16
DRV	238 ± 45	81 ± 16	29 ± 7	93	0.28–1.06
ATV	196 ± 23	67 ± 7	13 ± 4	86	0.62–1.27
SQV	203 ± 24	69 ± 8	6 ± 2	98	0.11–0.30
RTV	158 ± 27	52 ± 10	0.25 ± 0.07	99	0.16

↵* From Swainston Harrison and Scott, 2005; Rittweger and Arasteh, 2007
↵** From Williams and Sinko, 1999; Hoetelmans et al., 2003; Swainston Harrison and Scott, 2005; Marin-Niebla et al., 2007; Ruane et al., 2007
↵a E_max – E₀ represents the difference between calculated maximum uptake rate (at very low inhibitor concentration) and calculated uptake at maximum extent of inhibition by the specific PI