antibioticsbooks

Serine Protease
Inhibitors
37
Agents: boceprevir, telaprevir
The serine protease inhibitors, introduced in late
2011, are the first new class of drugs to treat
HCV infection in 13 years. They have been studied
for the treatment of HCV genotype 1 infection,
which is the most prevalent genotype in the
United States. Infections caused by HCV genotype
1 have considerably worse rates of sustained virologic
response (SVR) to pegylated interferon and
ribavirin therapy than genotypes 2 and 3, but the
addition of the serine protease inhibitors to this
combination has boosted SVR rates considerably.
However, they have additional adverse effects and
also increase the pill burden of HCV treatment.
Several future HCV therapies are being studied in
late-phase clinical trials.
Mechanism of Action
Serine protease inhibitors are the first directacting
antivirals (DAAs) for HCV infection available.
They inhibit serine protease enzymes from
cleaving the polyprotein produced by translation
of HCV RNA into its component proteins, similar
to the action of the HIV protease inhibitors.