Olysio (simeprevir) - Hepatitis C Drug Information

Olysio (simeprevir) 150mg capsule. Photo courtesy Janssen Pharmaceutical

Classification

Olysio (simeprevir) is a protease inhibitor-class drug used in combination antiviral therapy for the treatment of hepatitis C (HCV). Olysio works by binding to the active site of a nonstructural protein essential to HCV replication.

Olysio was approved in November 2013 by the U.S. Food and Drug Administration (FDA) for use in adults 18 years or over with HCV genotype 1 infection, either with or without compensated liver disease (i.e., where the liver is still functional).

Olysio is approved for use in previously untreated (treatment-naïve) patients, as well as those with either partial or no response to prior HCV therapy.

Clinical research has indicated that the cure rate for treatment-naïve patients on an Olysio-based regimen is between 80% and 85%.

Olysio may be challenging to use in co-infected HIV patients as it is contraindicated for use with all non-nucleoside reverse transcriptase inhibitors and ritonavir-boosted protease inhibitors (see below).

Dosage

One 150 mg capsule taken daily with food. Olysio capsules are white with "TMC145" printed on one side and "150" printed on the other side in black ink.

Prescribing Recommendations

Olysio is prescribed for use in combination with pegylated interferon (peg-interferon) + ribavirin. Olysio must never be used as monotherapy.

The duration of therapy is as follows:

  • Treatment-naïve patients: 24 weeks in total, with Olysio + peg-interferon + ribavirin prescribed for 12 weeks, followed by 12 weeks on peg-interferon + ribavirin alone.
     
  • Patients with previous failed HCV therapy (including those with cirrhosis): 48 weeks in the total, with Olysio + peg-interferon + ribavirin prescribed for 12 weeks, followed by 36 weeks on peg-interferon + ribavirin alone.

Before initiation of therapy, it is recommended that patients be screened for the Q80K polymorphism.

("Polymorphisms" occur when two or more genetic variants exist within a species population—in this case HCV.)

Studies have shown that the efficacy of an Olysio-based regimen is significantly diminished for HCV-1 strains containing the Q80K polymorphism. If the Q80K polymorphism is confirmed, an alternative therapy is strongly recommended.

Common Side Effects

The most common side effects associated with Olysio + peg-interferon +ribavirin are:

  • Rash
  • Pruritus (itching)
  • Nausea
  • Myalgia (muscle pain)
  • Dyspnea (shortness of breath)

In clinical research, 2% of patients on an Olysio-based regimen terminated therapy prematurely due to intolerable side effects.  

Drug Interactions

The following should also be avoided when using Olysio:

  • HIV boosters used in combination in combination antiretroviral therapy (cART): Norvir (ritonavir),  cobicistat (used in the fixed dose combination drug, Stribild)
     
  • Antibiotics: clarithromycin, Ketek
     
  • Anticonvulsants: Tegretol, Dilantin, Trileptal, phenobarbital
     
  • Antifungals: fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole
     
  • Gastroprokinetic medication: Prepulsid, Propulsid
     
  • Dexamethasone (a potent steroid drug)
     
  • St. John's Wort, milk thistle

Contraindications

Olysio is contraindicated for use in patients with decompensated liver disease (i.e., when the liver is no longer functioning).

Additionally, Olysio is contraindicated for use during pregnancy or in men whose partners are pregnant as animal studies have suggested a potential risk for birth defects or fetal death.

It is recommended that all women of child-bearing age be monitored monthly for pregnancy during the course of therapy.  It is also recommended that the patient and her male partner be provided at least two non-hormonal methods of contraception, and that they be used during the course of therapy and for six months afterwards.

Source:

U.S. Food and Drug Administration (FDA). "FDA approves new treatment for hepatitis C virus." Silver Springs, Maryland; November 22, 2013; Press Release.

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