Telaprevir Film-Coated Tablets

Name: Telaprevir Film-Coated Tablets

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:

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.

Indications

Chronic Hepatitis C

INCIVEK® (telaprevir), in combination with peginterferon alfa and ribavirin, is indicated for the treatment of genotype 1 chronic hepatitis C in adult patients with compensated liver disease, including cirrhosis, who are treatment-naïve or who have previously been treated with interferon-based treatment, including prior null responders, partial responders, and relapsers [see Clinical Studies, including definitions of these terms].

The following points should be considered when initiating treatment with INCIVEK:

  • INCIVEK must not be administered as monotherapy and must only be prescribed with both peginterferon alfa and ribavirin [see WARNINGS AND PRECAUTIONS].
  • A high proportion of previous null responders (particularly those with cirrhosis) did not achieve a Sustained Virologic Response (SVR) and had telaprevir resistance-associated substitutions emerge on treatment with INCIVEK combination treatment [see Microbiology and Clinical Studies].
  • 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 [see Microbiology].

What is telaprevir (incivek)?

Telaprevir is an antiviral medication that prevents certain virus cells from multiplying in your body. Telaprevir is used in combination with peginterferon alfa (Pegasys, PegIntron) and ribavirin (Copegus, Rebetol, Ribasphere, RibaTab) to treat hepatitis C in adults.

Read the medication guide or patient instructions provided with each medication in your combination therapy. Do not change your doses or medication schedule without your doctor's advice. Every person with hepatitis C should remain under the care of a doctor.

Telaprevir is usually given to people who have never been treated for hepatitis C, or after interferon and ribavirin have been tried without successful treatment of symptoms.

Telaprevir may also be used for purposes not listed in this medication guide.

What is the most important information i should know about telaprevir (incivek)?

Do not take telaprevir as your only medication to treat hepatitis C. Telaprevir must be used in combination with peginterferon alfa (Pegasys, PegIntron) and ribavirin (Copegus, Rebetol, Ribasphere, RibaTab).

Read the medication guide or patient instructions provided with each medication in your combination therapy. Do not change your doses or medication schedule without your doctor's advice.

Telaprevir is given together with interferon alfa and ribavirin. Ribavirin can cause birth defects or death in an unborn baby. Do not use this combination of drugs if you are pregnant, or if you are a man and your sexual partner is pregnant. Use at least 2 effective forms of birth control while either sexual partner is using interferon alfa and ribavirin, and for at least 6 months after treatment ends.

Telaprevir may cause a severe skin reaction. Call your doctor right away if you have a fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

The following drugs should not be used while you are taking telaprevir: alfuzosin (Uroxatral), cisapride (Propulsid), pimozide (Orap), atorvastatin (Lipitor, Caduet), lovastatin (Mevacor, Altoprev, Advicor) or simvastatin (Zocor, Simcor, Vytorin, Juvisync), midazolam (Versed), triazolam (Halcion), sildenafil (Revatio) or tadalafil (Adcirca) when used to treat pulmonary arterial hypertension, St. John's wort, rifampin (Rifadin, Rifater, Rifamate), ergonovine, ergotamine (Ergomar, Cafergot, Migergot), dihydroergotamine (D.H.E. 45, Migranal), or methylergonovine (Methergine).

There are many other drugs that can interact with telaprevir. Tell your doctor about all medications you use.

What should i discuss with my healthcare provider before taking telaprevir (incivek)?

You should not use telaprevir if you are allergic to it.

To make sure you can safely take telaprevir, tell your doctor if you have any of these other conditions:

  • hepatitis B or liver problems other than hepatitis C;
  • kidney disease (or if you are on dialysis);
  • anemia (lack of red blood cells);
  • if you have had an organ transplant;
  • HIV or AIDS;
  • a history of gout; or
  • if you have ever used medicine to treat hepatitis in the past and it did not work.

There are many other drugs that can cause serious or life threatening medical problems if you take them together with telaprevir. The following drugs should not be used while you are taking telaprevir:

  • alfuzosin (Uroxatral);
  • atorvastatin (Lipitor, Caduet), lovastatin (Mevacor, Altoprev, Advicor), or simvastatin (Zocor, Simcor, Vytorin, Juvisync);
  • cisapride (Propulsid);
  • pimozide (Orap);
  • midazolam (Versed) or triazolam (Halcion);
  • sildenafil (Revatio) or tadalafil (Adcirca) when used to treat pulmonary arterial hypertension;
  • St. John's wort;
  • rifampin (Rifadin, Rifater, Rifamate); or
  • ergonovine, ergotamine (Ergomar, Cafergot, Migergot), dihydroergotamine (D.H.E. 45, Migranal), or methylergonovine (Methergine).

FDA pregnancy category X. Telaprevir is given together with interferon alfa and ribavirin. Although telaprevir is not expected to harm an unborn baby, ribavirin is known to cause birth defects or death in an unborn baby. Do not use this combination of drugs if you are pregnant, or if you are a man and your sexual partner is pregnant. If you are a woman, you may need to have a negative pregnancy test before using these medications and every month during your treatment.

  • Use at least 2 non-hormonal forms of birth control while either sexual partner is using telaprevir with interferon alfa and ribavirin. Keep using 2 forms of birth control for at least 6 months after treatment ends.
  • If you are a woman, do not use telaprevir with interferon alfa and ribavirin if you are pregnant.
  • If you are a man, do not use telaprevir with interferon alfa and ribavirin if your sexual partner is pregnant. An unborn baby could also be harmed if a man fathers the child while he is taking ribavirin.
  • Hormonal contraception (such as birth control pills, injections, implants, skin patches, and vaginal rings) may not be effective enough to prevent pregnancy during your treatment. Ask your doctor about using a non-hormone method of birth control (such as a condom, intrauterine device (IUD), diaphragm with spermicide) to prevent pregnancy while taking telaprevir.
  • Tell your doctor right away if a pregnancy occurs while either the mother or the father is using telaprevir with interferon alfa and ribavirin.

It is not known whether telaprevir passes into breast milk or if it could harm a nursing baby. Do not breast-feed a baby while taking telaprevir.

What happens if i miss a dose (incivek)?

If you are less than 4 hours late in taking your medicine, take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

(web3)