Drug information of Telaprevir


Drug group:

Telaprevir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV).

Mechanism of effect

Telaprevir is a NS3/4a protease inhibitor used to inhibit viral HCV replication. NS3/4a protease is an integral part of viral replication and mediates the cleavage the virally encoded polyprotein to mature proteins (NS4A, NS4B, NS5A and NS5B). Telaprevir inhibits NS3/4A with an IC50 of 10nM.


Peak plasma time: 4-5 hr

Peak plasma concentration: 3510 ng/mL

AUC: 22,300 (8650) ng•hr/mL

Food: AUC increased by 237% when administered with a standard fat meal (containing 533 kcal and 21 g fat) compared with fasting conditions

Protein bound: 59-76% (primarily alpha 1-acid glycoprotein and albumin)

Vd: 252 L (72% interindividual variability)


Extensively metabolized in liver by hydrolysis, oxidation, and reduction

Metabolites: R-diastereomer of telaprevir (30-fold less active), pyrazinoic acid, and a metabolite that underwent reduction at the alpha-ketoamide bond of telaprevir (not active) were found to be the predominant metabolites

Metabolized by CYP3A4 is the major CYP isoform; after multiple dosing, nonCYP metabolism is also apparent

Inhibits CYP3A and P-gp

Substrate of CYP3A and P-gp

Half-life: 4-4.7 hr (mean); 9-11 hr (at steady state)

Total body clearance: 32.4 L/h

Excretion: feces (82%); exhaled air (9%); urine (1%)


Among both treatment-naïve and previous treatment failures, subjects of all IL28B genotypes (ie, CT, TT, CC) appeared to have higher SVR rates with telaprevir-containing regimens in clinical trials compared with dual therapy

SVR rates tend to be lower for dual therapy if IL28B CT and TT variants are present compared with IL28B CC



1,125 mg (3 tabs) PO BID (q10-14hr) with food (not low fat)

Administer for 12 weeks in combination with peginterferon alfa and ribavirin (telaprevir must not be used as monotherapy)


Safety and efficacy not established


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 therapy; use two or more forms of contraception, and have monthly pregnancy tests

Serious skin reactions, including drug rash with eosinophilia and systemic symptoms (DRESS), toxic epidermal necrolysis (TEN), and Stevens-Johnson Syndrome (SJS); discontinue immediately and do not reintroduce (see Black Box Warnings)

Anemia: Addition of telaprevir to peginterferon alfa and ribavirin is associated with an additional decrease in hemoglobin concentrations compared with peginterferon alfa and ribavirin alone; obtain baseline Hgb, white cell differential, and platelet count and monitor at weeks 2, 4, 8, and 12 during treatment and as clinically needed

Use sensitive real-time RT-PCR assay for monitoring HCV-RNA levels during treatment at weeks 4 and 12 as clinically indicated

Not recommended for with moderate-to-severe hepatic impairment (Child-Pugh B or C, score 7 or greater) or with decompensated liver disease

Black Box Warnings

Fatal and nonfatal serious skin reactions (including Stevens Johnson syndrome, drug reaction with eosinophilia and systemic symptoms [DRESS], and toxic epidermal necrolysis [TEN]) reported in patients taking telaprevir in combination with peginterferon alfa and ribavirin

Deaths reported when patients continued to receive this treatment regimen after developing a worsening, or progressive rash and systemic symptoms

If serious skin reactions occur, immediately discontinue all 3 drugs of the treatment regimen (ie, telaprevir, peginterferon alfa, ribavirin)

Patients should be promptly referred for urgent medical care

Also consider stopping any other medications that may be associated with serious skin reactions

Points of recommendation

You may bleed more easily. Be careful and avoid injury. Use a soft toothbrush and an electric razor.

  Have blood work checked as you have been told by the doctor. Talk with the doctor.

  Do not take St John's wort with telaprevir. This medicine may not work as well.

  This medicine does not stop the spread of diseases like HIV or hepatitis that are passed through blood or having sex. Do not have any kind of sex without using a latex or polyurethane condom. Do not share needles or other things like toothbrushes or razors. Talk with your doctor.

This medicine may cause harm to the unborn baby if you take it while you are pregnant.

Use 2 kinds of birth control that you can trust while using telaprevir and for 6 months after stopping telaprevir.

  If you are a man and have sex with a female who could get pregnant, protect her from pregnancy during care and for 6 months after care ends. Use birth control that you can trust.

  Do not use a hormone-related kind of birth control.

Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

  • To gain the most benefit, do not miss doses.
  • Take telaprevir at the same time of day.
  • Keep taking telaprevir as you have been told by your doctor or other health care provider, even if you feel well.
  • Take with a high-fat meal.
  • Swallow whole. Do not chew, break, or crush.
  • Drink lots of noncaffeine liquids unless told to drink less liquid by your doctor.
  • If it has been 6 hours or more since the missed dose, skip the missed dose and go back to your normal time.
  • If it has been less than 6 hours since a normal dose, take a missed dose as soon as you think about it and go back to your normal time.
  • Do not use 2 doses or extra doses.

Pregnancy level


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