20-F-20-C-Methyl Nucleosides and Nucleotides for the Treatment of Hepatitis C Virus: from Discovery to the Clinic - Accounts in Drug Discovery Case Studies in Medicinal Chemistry - page 254

Table 11.5 INFORM-1 antiviral activity for cohorts B-G

HCV RNA median
change from base-
line (log 10 IU
mL 1 ) (range)

Median baseline
HCV RNA
(log 10 IUmL 1 )

HCV RNA
o LLOQ a ( o 43
IUmL 1 ) N (%)

HCV RNA
o LLOD b ( o 15
IUmL 1 ) N (%)

Regimen (RG7128mg/
RG7227mg) N Patient population

B 500 BID/100 TID c 6.5 8 naive -3.9 (-5.0 to -2.9) 1/8 (13) 1/8 (13)

C 1 500 BID/200 TID 6.9 8 naive -5.2 (-5.5 to -3.1) 5/8 (63) 2/8 (25)

C 2 1000 BID/100 TID 6.4 7 naive -4.8 (-5.7 to -4.5) 5/7 (71) 2/7 (29)

D 1000 BID/200 TID 6.3 8 naive -4.8 (-5.5 to -2.7) 5/8 (63) 2/8 (25)

TF d (non-null) E 1000 BID/600 BID 6.2 8 -4.0 (-6.0 to -2.5) 4/8 (50) 1/8 (13)

F 1000 BID/900 BID 6.5 8 TF (null) -4.9 (-5.3 to -3.5) 4/8 (50) 2/8 (25)

G 1000 BID/900 BID 6.5 8 naive -5.1 (-5.9 to -3.0) 7/8 (88) 5/8 (63)

a LLOQ ¼ lower limit of quantification by Roche TaqMan Assay ( o 43 IUmL 1 ).
b LLOD ¼ lower limit of detection by Roche TaqMan Assay ( o 15 IUmL 1 ).
c TID ¼ three times daily.
d TF ¼ treatment failures.