Pharm

Cobicistat

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Cobicistat, Tybost, COBI

  • See Also
  1. Protease Inhibitor
  2. Anti-Retroviral Therapy
  • Indications
  1. "Boosting" of Protease Inhibitors for HIV Infection (as part of combination therapy)
  • Mechanism
  1. Cobicistat is a strong CYP3A4 inhibitor, NOT a Protease Inhibitor
    1. Cobicistat also inhibits CYP2D6, P-Glycoprotein, BCRP and OATP transporters
    2. Cobicistat is a Carbamate and thiazole derivative
  2. Cobicistat, when added to Protease Inhibitors, "boosts" their serum levels for better efficacy
    1. Examples of boosted Protease Inhibitors include Atazanavir and Darunavir
  • Dosing
  1. Cobicistat 150 mg orally daily with food AND
  2. Protease Inhibitor (one of the following)
    1. Atazanavir 300 mg orally daily (400 mg when combined with Efavirenz) OR
    2. Darunavir 800 mg orally daily
  • Pharmacokinetics
  1. Cobicistat decreases Creatinine Clearance (roughly 10 ml/min when GFR>50 ml/min)
    1. However, Cobicistat does NOT affect GFR
  • Drug Interactions
  1. Many Drug Interactions!
    1. Review Drug Interactions carefully with a formal application when prescribing
    2. Cobicistat strongly inhibits CYP3A4
    3. Cobicistat also inhibits CYP2D6, P-Glycoprotein, BCRP and OATP transporters
    4. Cobicistat differs in its Drug Interactions from Ritonavir (the interaction lists are NOT interchangeable)
  • Safety
  1. Avoid in Lactation
  2. Unknown safety in pregnancy
    1. Avoid starting Cobicistat in pregnancy
  • Resources
  1. Cobicistat (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3784c35c-e87f-410c-900b-8fd6313c6010
  2. Cobicistat (DrugBankOnline)
    1. https://go.drugbank.com/drugs/DB09065