Telaprevir description
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]
Description
INCIVEK (telaprevir) is an inhibitor of the HCV NS3/4A protease.
The IUPAC name for telaprevir is (1S,3aR,6aS)-2-[(2S)-2-({(2S)-2-cyclohexyl-2-[(pyrazin-2-ylcarbonyl)amino]acetyl}amino)-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-1-carboxamide. Its molecular formula is C36H53N7O6 and its molecular weight is 679.85. Telaprevir has the following structural formula:
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Telaprevir drug substance is a white to off-white powder with a solubility in water of 0.0047 mg/mL.
Telaprevir interconverts to an R-diastereomer, VRT-127394, which is the major metabolite in plasma and is approximately 30-fold less potent than telaprevir.
INCIVEK is available as a purple, capsule-shaped, film-coated tablet for oral administration containing 375 mg of telaprevir. Each tablet contains the inactive ingredients colloidal silicon dioxide, croscarmellose sodium, D&C Red No. 40, dibasic calcium phosphate (anhydrous), FD&C Blue No. 2, hypromellose acetate succinate, microcrystalline cellulose, polyethylene glycol, polyvinyl alcohol, sodium lauryl sulfate, sodium stearyl fumarate, talc, and titanium dioxide.[1]
References
- ↑ "INCIVEK (TELAPREVIR) TABLET, FILM COATED [VERTEX PHARMACEUTICALS INCORPORATED]". Retrieved 8 January 2014.
Adapted from the FDA Package Insert.