TABLE 5.

Sensitivities of NS5B mutants and NS3 mutant A156V to polymerase inhibitors and BILN-2061, as well as IFN

Inhibitor	IC50 (μM) ± SD (IC50 change)a
	WT-1b-N	D55E	H95Q	V138I	N411S	M414L	M414T	Y448H	A156Vb
A-782759 Abbott, 1	0.004 ± 0.003 (1)	0.013 ± 0.005 (3.3)	0.81 ± 0.034 (20)	0.013 ± 0.004 (3)	1.33 ± 0.08 (333)	0.41 ± 0.08 (103)	8.9 ± 1.39 (>800)	1.22 ± 0.15 (305)	0.003 ± 0.001 (0.8)
Shire, 2	0.35 ± 0.08 (1)	0.29 ± 0.10 (0.7)	0.143 ± 0.01 (0.4)	0.26 ± 0.06 (0.7)	0.24 ± 0.11 (1)	0.17 ± 0.08 (0.5)	0.35 ± 0.08 (1)	0.29 ± 0.11 (1)	0.44 ± 0.004 (1.3)
Merck, 3	0.27 ± 0.05 (1)	0.52 ± 0.14 (1.9)	ND	0.38 ± 0.13 (1.4)	0.14 ± 0.7 (0.5)	0.24 ± 0.08 (1)	0.17 ± 0.08 (0.5)	0.35 ± 0.08 (1)	0.29 ± 0.11 (1)
Boehringer Ingelheim, 4	1.97 ± 0.23 (1)	3.77 ± 1.2 (1.9)	1.24 ± 0.1 (0.7)	5.35 ± 0.35 (3)	0.6 ± 0.33 (1)	1.9 ± 0.23 (1)	0.64 ± 0.03 (0.3)	1.32 ± 0.11 (1)	5 ± 0.6 (2.5)
BILN-2061 Boehringer Ingelheim, 5	0.001 ± 0.0004 (1)	0.0020 ± 0.0014 (2)	0.001 ± 0.0005 (1)	0.0013 ± 0.0002 (1)	0.001 ± 0.0001 (1)	0.001 ± 0.0002 (1)	0.0019 ± 0.001 (1.9)	0.002 ± 0.0001 (1)	0.61 ± 0.16 (610)
IFN (μg/ml)	0.06 ± 0.03 (1)	ND	0.05 ± 0.03 (0.8)	0.08 ± 0.001 (1)	0.15 ± 0.001 (1)	0.09 ± 0.001 (1.5)	0.19 ± 0.02 (3)	0.2 ± 0.02 (3)	0.04 ± 0.02 (0.7)

^aND, not done due to unavailability of Merck, 3, or the same lot of IFN used for this study. Data are averages of at least two separate experiments done in triplicate. Change in IC₅₀ (n-fold) = IC₅₀ of mutant tested/IC₅₀ of wild-type replicon.

^bNS3 mutant.