⇝ Basic Information
Developed by Gilead, Cobicistat was approved by the European Medicines Agency (EMA) on September 19, 2013 under the trade name Tybost®; after September 24, 2014, the US Food and Drug Administration (FDA) Approved for sale, the trade name is Stribild®, which is marketed by Gilead in the US and Europe.
Cobicistat is a cytochrome P4503A inhibitor. Cobicistat is similar in structure to ritonavir (Nove) and inhibits the activity of hepatic enzymes involved in the metabolism of other anti-HIV drugs, especially the inhibition of the metabolism of levigovir (HIV integrase inhibitor) by hepatic enzymes. When used in combination with Cobicistat, entegitide achieves higher blood levels at lower doses, thereby increasing viral inhibition and reducing side effects. Unlike ritonavir, Cobicistat is the only approved cocktail therapy (HAART) drug enhancer that does not itself have anti-HIV activity.
Tybost® is an oral film-coated tablet containing 150 mg of Cobicistat per tablet. The recommended starting dose is: combined with emtricitabine or darunavir, 150mg each time, once a day, with meals.
⇝ Structural formula
⇝ Mechanism
Cobicistat (GS-9350) is a potent CYP3A selective inhibitor with an IC50 of 30 - 285 nM. Cobicistat (GS-9350) is a potent inhibitor of the potent human cytochrome P450 3A (CYP3A) enzyme.
⇝Synthetic route
⇝ Research key data
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