Available by prescription only, telaprevir (INCIVEK®) is a protease inhibitor used in adults who have chronic hepatitis C infections. It comes as a tablet that is taken 3 times daily for 12 weeks.
The mechanism of action by which telaprevir works is by inhibiting the activity of protease enzymes in the body. These enzymes are used by the hepatitis C virus to clip long protein strands into shorter, usable strands. The virus then uses these shorter strands to replicate itself (reproduce). By blocking protease enzymes, telaprevir prevents the hepatitis C virus from multiplying.
Telaprevir is a NS3-4A protease inhibitor that competes with the substrate, NS5A/5B, and targets the substrate-binding site, the serine residue of the protease’s catalytic triangle. Upon binding to the protease, the ∂-ketomide (ketone and amide group of telaprevir) forms a reversible covalent linkage with Ser-139. Because of this mechanism, telaprevir is often referred to as an ∂-ketomide-based “serine trap” inhibitor.
Telaprevir is a HCV NS3-4A protease inhibitor indicated in the treatment of genotype 1chronic hepatitis C in adult and must only be used in combination with peginterferon alfa and ribavirin.