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Table 1 Enzymatic in vitro drug resistance data for telaprevir (VX-950)

From: Molecular basis of telaprevir resistance due to V36 and T54 mutations in the NS3-4A protease of the hepatitis C virus

 

IC50 mean (nM)

IC50 range (nM)

IC50 (fold changes)

HCV genotype 1a

70

-

-

V36A/G/L/M

226

110-444

1.7-6.9

T54S

120

-

1.9

T54A

749

-

11.7

R155G/I/K/L/M/S/T

538

275-1,050

4.3-16.4

A156I/T/V

29,800

12,500-50,000

195-781

A156S

1,400

-

21.9

  1. Enzymatic in vitro resistance data for VX-950 (mean IC50 values, IC50 range and IC50 fold changes) are compared to the reference strain HCV-H, genotype 1a (UniProtKB accession number P27958) and are shown for VX-950 inhibition of wild-type and mutant NS3-4A proteases (V36, T54, R155 and A156) [19,26,28].