Cobicistat

Brands

DEA Class; Rx

Common Brand Names; Tybost

  • CYP450 Inhibitors

A CYP3A inhibitor
Used as a booster to increase exposure of atazanavir or darunavir in adults and pediatric patients with HIV (weight dependent)
Monitor closely for drug interactions

Indicated to increase systemic exposure of atazanavir or darunavir (once-daily dosing regimen) in combination with other antiretroviral agents (ARTs) in the treatment of HIV-1 infection

Coadministration of cobicistat with atazanavir or darunavir and the following drugs is contraindicated owing to potential for serious and/or life-threatening events or loss of therapeutic effect

  • Alfuzosin
  • Amiodarone
  • Carbamazepine, phenobarbital, phenytoin
  • Rifampin
  • Irinotecan (when administered with atazanavir)
  • Lurasidone, pimozide
  • Dihydroergotamine, ergotamine, methylergonovine
  • Cisapride
  • St. John’s wort (Hypericum perforatum)
  • Drospirenone/ethinyl estradiol (when administered with atazanavir)
  • Lomitapide, lovastatin, simvastatin
  • Nevirapine (when administered with atazanavir)
  • Sildenafil when administered for pulmonary arterial hypertension
  • Indinavir (when administered with atazanavir)
  • Triazolam, orally administered midazolam

Note: Adverse effects listed below are for cobicistat coadministered with atazanavir

  • Total bilirubin >2.5x ULN (65%)
  • Ocular icterus, all grades (15%)
  • Jaundice, all grades (13%)
  • Nausea, all grades (12%)
  • Creatine kinase >10x ULN (5%)
  • Jaundice, Grades 2-4 (5%)
  • Rash, Grades 2-4 (5%)
  • Serum amylase >2x ULN (4%)
  • ALT or AST >5x ULN (3%)
  • Glycosuria >1000 mg/dL (3%)
  • Urine RBC >75 RBC/HPF (3%)
  • Ocular icterus Grades 2-4 (3%)
  • GGT >5x ULN (2%)
  • Nausea, Grades 2-4 (2%)

Cobicistat may cause modest increases in serum creatinine and modest declines in CrCl without affecting renal glomerular function; serum creatinine >0.4 mg/dL from baseline should be closely monitored for renal safety; assess CrCl before administering

New-onset or worsening renal impairment reported when used with antiretroviral regimens containing tenofovir; do not use with tenofovir if CrCl <70 mL/min

Assess urine glucose and urine protein at baseline and monitor ClCr, urine glucose, and urine protein when using with tenofovir; monitor serum phosphorus in patients with or at risk for renal impairment

CYP inducers may lower systemic exposure of cobicistat and atazanavir or darunavir, resulting in loss of virologic response

Cobicistat is an inhibitor of CYP3A, CYP2D6, p-glycoprotein (P-gp), BCRP, OATP1B1, and OATP1B3; plasma concentration of drugs that are substrates of the aforementioned isoenzymes or transporters may be increased if coadministered with cobicistat

Antiretrovirals that are not recommended

  • The following are NOT recommended in combination with cobicistat because dosing recommendations for the combinations have not been established
  • Coadministration may result in decreased plasma concentrations of the antiretroviral agents, leading to loss of therapeutic effect and development of resistance
  • More than 1 antiretroviral that requires pharmacokinetic enhancement (ie, 2 protease inhibitors or a protease inhibitor in combination with elvitegravir)
  • Darunavir in combination with efavirenz, nevirapine, or etravirine
  • Atazanavir in combination with etravirine
  • Atazanavir in combination with efavirenz in treatment-experienced patients
  • Darunavir 600 mg BID
  • Other HIV-1 protease inhibitors, including fosamprenavir, saquinavir, or tipranavir
  • Stribild fixed-dose combination tablets (elvitegravir, cobicistat, emtricitabine, tenofovir) are not recommended because cobicistat is a component of Stribild
  • Cobicistat in combination with lopinavir/ritonavir or regimens containing ritonavir are not recommended, owing to similar effects of cobicistat and ritonavir on CYP3A

Coadministration with darunavir or atazanavir is not recommended during pregnancy

In a clinical trial of individuals taking cobicistat coadministered with darunavir, exposures of cobicistat and darunavir were substantially lower during the second and third trimesters of pregnancy

Adults

150 mg/day PO.

Geriatric

150 mg/day PO.

Adolescents

weight 35 kg or more: 150 mg/day PO.
weight less than 35 kg: Safety and efficacy have not been established.

Children

weight 35 kg or more: 150 mg/day PO.
weight less than 35 kg: Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

cobicistat

tablet

  • 150mg
Drugs Generic
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