Telaprevir Mechanism of Action

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.

http://hepatitis.emedtv.com/telaprevir/telaprevir-mechanism-of-action.html

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.

thank you for your efforts in your replys .But actually I wanted if anyone has info about the mechanism of action whether it is hapten or P-I       

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.

Dear Zaid,

I believe that the telaprevir mediated hypersensitivity reactions (usually presenting as pruritic eczematous dermatitis) occur through p-i, though the mechanism has not been as well characterized as others (namely, abacavir). In the case report cited below (Federico et al), the authors describe an in vitro experiment in which telaprevir was able to induce T-cell activation. However, because it is known that telaprevir is a delayed-type hypersensitivity, the authors speculate that the reaction may be actually mediated by telaprevir's intracellular metabolites, metabolized not within the liver, but within the skin/immune cells themselves.

To my knowledge, no one has crystalized telaprevir with a human leukocyte antigen or T cell receptor. I've included the article (Purcell et al) that first demonstrated this for abacavir.

I hope that helps!

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