Cobicistat

Cobicistat Uses, Dosage, Side Effects, Food Interaction and all others data.

Cobicistat, marketed under the name Tybost (formerly GS-9350), indicated for treating infection with human immunodeficiency virus (HIV). Although it does not have any anti-HIV activity, cobicistat acts as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A isoforms (CYP3A) and therefore increases the systemic exposure of coadministered agents that are metabolized by CYP3A enzymes. More specifically, cobicistat is indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. Increasing systemic exposure of anti-retrovirals (ARVs) without increasing dosage allows for better treatment outcomes and a decreased side effect profile.

Trade Name Cobicistat
Availability Prescription only
Generic Cobicistat
Cobicistat Other Names Cobicistat
Related Drugs Biktarvy, Truvada, tenofovir, ritonavir, Complera, Atripla, Stribild
Weight 150mg, 150mg + 800mg + 200mg + 10mg, 150mg + 150mg + 200mg + 10mg, 150mg + 150mg + 200mg + 300mg,
Type Oral Tablet, Oral
Formula C40H53N7O5S2
Weight Average: 776.03
Monoisotopic: 775.354960183
Protein binding

97-98% bound to human plasma proteins.

Groups Approved
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Cobicistat
Cobicistat

Uses

Cobicistat is a CYP3A inhibitor used to increase the systemic exposure of atazanavir or darunavir in combination with other antiretroviral agents in the treatment of HIV-1 infection.

Cobicistat is a CYP3A inhibitor indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. It is not interchangeable with ritonavir to increase systemic exposure of darunavir 600 mg twice daily, fosamprenavir, saquinavir, or tipranavir due to lack of exposure data. The use of cobicistat is not recommended with darunavir 600 mg twice daily, fosamprenavir, saquinavir or tipranavir. Complex or unknown mechanisms of drug interactions preclude extrapolation of ritonavir drug interactions to certain cobicistat interactions. Cobicistat and ritonavir when administered with either atazanavir or darunavir may result in different drug interactions when used with concomitant medications.

Cobicistat is also used to associated treatment for these conditions: Human Immunodeficiency Virus (HIV) Infections, Human Immunodeficiency Virus Type 1 (HIV-1) Infection

How Cobicistat works

Cobicistat is a mechanism-based inhibitor of cytochrome P450 3A (CYP3A) isoforms. Inhibition of CYP3A-mediated metabolism by cobicistat increases the systemic exposure of CYP3A substrates atazanavir and darunavir and therefore enables increased anti-viral activity at a lower dosage. Cobicistat does not have any anti-HIV activity on its own.

Toxicity

The most common adverse reactions reported during clinical trials were jaundice (13%), ocular icterus (15%), and nausea (12%).

Food Interaction

  • Avoid St. John's Wort. St. John's Wort is contraindicated as it induces the CYP3A metabolism of cobicistat and may reduce its serum concentration.
  • Take at the same time every day.
  • Take with food.

Cobicistat Disease Interaction

Moderate: creatinine clearance

Elimination Route

Median peak plasma concentrations were observed at 3.5 hours post-dose.

Half Life

The terminal plasma half-life of cobicistat is approximately 3 to 4 hours.

Elimination Route

With single dose administration of [14C] cobicistat after multiple dosing of cobicistat for six days, the mean percent of the administered dose excreted in feces and urine was 86.2% and 8.2%, respectively.

Innovators Monograph

You find simplified version here Cobicistat

*** Taking medicines without doctor's advice can cause long-term problems.
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