Synonyms: GS-9350
cobicistat is an approved drug (FDA (2012), EMA (2013))
Compound class:
Synthetic organic
Comment: This compound is approved as a component of the so-called 'Quad pill' (Stribild®), an anti-HIV therapy which contains cobicistat, elvitegravir, emtricitabine, and tenofovir.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
Used as a pharmacokinetic booster, to enhance systemic exposure to anti-HIV drugs. |
Mechanism Of Action and Pharmacodynamic Effects |
Cobicistat inhibits metabolic liver enzymes, in particular the cytochrome P450 3A subtype, CYP3A4 [3]. The CYP3A enzymes are known to breakdown and inactivate antiviral drugs such as elvitegravir (an HIV integrase inhibitor), although cobicistat has no intrinsic antiviral activity [2]. Additionally, cobicistat appears to inhibit intestinal transport proteins, thus increasing absorption of other anti-HIV drugs such as atazanavir, darunavir and tenofovir alafenamide fumarate [1]. |