Cobicistat - CAS 1004316-88-4
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Cytochrome P450
Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate.
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B0084-456314 25 mg $298 In stock
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Cobicistat, GS-9350
1.Population pharmacokinetic analysis of elvitegravir and cobicistat in HIV-1-infected individuals.
Barceló C1, Gaspar F2, Aouri M1, Panchaud A2, Rotger M3, Guidi M4, Cavassini M5, Buclin T1, Decosterd LA6, Csajka C7; Swiss HIV Cohort Study. J Antimicrob Chemother. 2016 Mar 29. pii: dkw050. [Epub ahead of print]
OBJECTIVES: Co-formulated elvitegravir, cobicistat, tenofovir disoproxil fumarate and emtricitabine is among the preferred regimens for first-line ART. A population approach was used to characterize the pharmacokinetics of elvitegravir and cobicistat and identify individual factors and co-medications influencing their disposition, taking into consideration the interaction between the two compounds.
2.Evaluating the role of atazanavir/cobicistat and darunavir/cobicistat fixed-dose combinations for the treatment of HIV-1 infection.
Crutchley RD1, Guduru RC2, Cheng AM1. HIV AIDS (Auckl). 2016 Mar 9;8:47-65. doi: 10.2147/HIV.S99063. eCollection 2016.
Atazanavir/cobicistat (ATV/c) and darunavir/cobicistat (DRV/c) are newly approved once daily fixed-dose protease inhibitor combinations for the treatment of HIV-1 infection. Studies in healthy volunteers have established bioequivalence between cobicistat and ritonavir as pharmacoenhancers of both atazanavir (ATV) and darunavir (DRV). In addition, two randomized clinical trials (one Phase II and one Phase III noninferiority trial with a 144-week followup period) demonstrated that cobicistat had sustainable and comparable efficacy and safety to ritonavir as a pharmacoenhancer of ATV through 144 weeks of treatment in HIV-1-infected patients. Furthermore, one Phase III, open-label, single-arm, clinical trial reflected virologic and immunologic responses and safety outcomes consistent with prior published data for DRV/ritonavir 800/100 mg once daily, supporting the use of DRV/c 800/150 mg once daily for future treatment of treatment-naïve and -experienced HIV-1-infected patients with no DRV resistance-associated mutations.
3.Cobicistat Significantly Increases Tacrolimus Serum Concentrations in a Renal Transplant Recipient with Human Immunodeficiency Virus Infection.
Han Z1, Kane BM1, Petty LA2, Josephson MA3, Sutor J4, Pursell KJ2. Pharmacotherapy. 2016 Apr 3. doi: 10.1002/phar.1752. [Epub ahead of print]
Cobicistat is a pharmacokinetic booster in several fixed-dose combination products for treatment of human immunodeficiency virus (HIV) infection. As a potent inhibitor of cytochrome P450 (CYP) 3A enzymes, significant drug-drug interactions are expected between cobicistat and medications that are metabolized primarily through the CYP3A pathway, including calcineurin inhibitors (e.g., tacrolimus and cyclosporine). We describe a case of tacrolimus toxicity due to supratherapeutic tacrolimus concentrations when Stribild® (elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate) was initiated for newly diagnosed HIV infection in a 50-year-old renal transplant recipient who was previously receiving a stable tacrolimus regimen. Drug-drug interaction via CYP3A inhibition was acknowledged and weekly labs were ordered to allow for close monitoring of renal function and tacrolimus serum concentrations as recommended by Stribild® prescribing information.
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CAS 1004316-88-4 Cobicistat

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