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|NEW DRUG - INDEX PAGE|
INCIVEK (telaprevir) is an inhibitor of the HCV NS3/4A protease.
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.
Mechanism of Action
Telaprevir is a direct-acting antiviral agent (DAA) against the hepatitis C virus.
Telaprevir is an inhibitor of the HCV NS3/4A serine protease, necessary for the proteolytic cleavage of the HCV encoded polyprotein into mature forms of the NS4A, NS4B, NS5A and NS5B proteins and essential for viral replication. In a biochemical assay, telaprevir inhibited the proteolytic activity of the recombinant HCV NS3 protease domain with an IC50 value of 10 nM.
INDICATIONS AND USAGE
INCIVEK is a hepatitis C virus (HCV) NS3/4A protease inhibitor indicated, in combination with peginterferon alfa and ribavirin, for the treatment of genotype 1 chronic hepatitis C (CHC) in adult patients with compensated liver disease, including cirrhosis, who are treatment-naïve or who have been previously treated with interferon-based treatment, including prior null responders, partial responders, and relapsers.
INCIVEK must not be used as monotherapy and must only be used in combination with peginterferon alfa and ribavirin.
A high proportion of previous null responders (particularly those with cirrhosis) did not achieve Sustained Virologic Response (SVR) and had telaprevir resistance-associated substitutions emerge on treatment with INCIVEK.
INCIVEK efficacy has not been established for patients who have previously failed therapy with a treatment regimen that includes INCIVEK or other HCV NS3/4A protease inhibitors.
All contraindications to peginterferon alfa and ribavirin also
apply since INCIVEK must be administered with peginterferon alfa
Pregnant women and men whose female partners are pregnant: Because ribavirin may cause birth defects and fetal death, telaprevir in combination with peginterferon alfa and ribavirin is contraindicated in pregnant women and in men whose female partners are pregnant.
Co-administration with drugs that:
are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events.
strongly induce CYP3A which may lead to lower exposure and loss of efficacy of INCIVEK.
WARNINGS AND PRECAUTIONS
Pregnancy: Use with Ribavirin and Peginterferon alfa: Ribavirin may cause birth defects and fetal death; avoid pregnancy in female patients and female partners of male patients. Patients must have a negative pregnancy test prior to initiating therapy, use at least 2 effective methods of contraception, and undergo monthly pregnancy tests.
Serious Skin Reactions: Serious skin reactions including Drug Rash with Eosinophilia and Systemic Symptoms and Stevens-Johnson Syndrome have been reported. For serious skin reactions, all components of INCIVEK combination treatment should be discontinued immediately.
Rash: Patients with mild to moderate rash should be monitored for progression. If rash progresses and becomes severe, INCIVEK should be discontinued.
Anemia: Monitor hemoglobin prior to and at regular intervals during INCIVEK combination treatment. Follow dose modifications for ribavirin; discontinue INCIVEK if required.
Co-administration of INCIVEK combination treatment with other drugs can alter the concentration of other drugs and other drugs may alter the concentrations of telaprevir. Consult the full prescribing information prior to and during treatment for potential drug-drug interactions.
USE IN SPECIFIC POPULATIONS
Hepatic Impairment: Safety and efficacy have not been established in patients with Child-Pugh score greater than or equal to 7 (class B and C).
Co-infection: Safety and efficacy have not been established in HCV/HIV and HCV/HBV co-infected patients.
Pediatrics: Safety and efficacy have not been established in pediatric patients.
Solid Organ Transplant: Safety and efficacy have not been established in patients undergoing solid organ transplants.
Ribavirin Pregnancy Registry available.
The most common adverse drug reactions to INCIVEK (incidence at
least 5% higher with INCIVEK than in controls) were rash,
pruritus, anemia, nausea, hemorrhoids, diarrhea, anorectal
discomfort, dysgeusia, fatigue, vomiting, and anal pruritus.
To report SUSPECTED ADVERSE REACTIONS, contact Vertex Pharmaceuticals Incorporated at 877-824-4281 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
750 mg taken 3 times a day (7-9 hours apart) with food (not low
INCIVEK must be administered with both peginterferon alfa and ribavirin for all patients for 12 weeks, followed by a response-guided regimen of either 12 or 36 additional weeks of peginterferon alfa and ribavirin depending on viral response and prior response status.
For specific dosage instructions for peginterferon alfa and ribavirin, refer to their respective prescribing information.
See PACKAGE INSERT for additional information.
|375 mg tablets|
Package Insert data:
Vertex Pharmaceuticals Incorporated
Cambridge, MA 02139
Issued May 2011
©2011 Vertex Pharmaceuticals Incorporated
All rights reserved.