II. Indications
- "Boosting" of Protease Inhibitors for HIV Infection (as part of combination therapy)
III. Mechanism
- Cobicistat is a strong CYP3A4 inhibitor, NOT a Protease Inhibitor
- Cobicistat also inhibits CYP2D6, P-Glycoprotein, BCRP and OATP transporters
- Cobicistat is a Carbamate and thiazole derivative
- Cobicistat, when added to Protease Inhibitors, "boosts" their serum levels for better efficacy
- Examples of boosted Protease Inhibitors include Atazanavir and Darunavir
IV. Dosing
- Cobicistat 150 mg orally daily with food AND
-
Protease Inhibitor (one of the following)
- Atazanavir 300 mg orally daily (400 mg when combined with Efavirenz) OR
- Darunavir 800 mg orally daily
V. Pharmacokinetics
- Cobicistat decreases Creatinine Clearance (roughly 10 ml/min when GFR>50 ml/min)
- However, Cobicistat does NOT affect GFR
VI. Drug Interactions
- Many Drug Interactions!
- Review Drug Interactions carefully with a formal application when prescribing
- Cobicistat strongly inhibits CYP3A4
- Cobicistat also inhibits CYP2D6, P-Glycoprotein, BCRP and OATP transporters
- Cobicistat differs in its Drug Interactions from Ritonavir (the interaction lists are NOT interchangeable)
VII. Safety
- Avoid in Lactation
- Unknown safety in pregnancy
- Avoid starting Cobicistat in pregnancy
VIII. Resources
- Cobicistat (DailyMed)
- Cobicistat (DrugBankOnline)