PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 30545467-3 2018 Cobicistat-boosted darunavir with emtricitabine and tenofovir alafenamide co-formulation (DRV/c/FTC/TAF), with trade name Symtuza , is the first STR based on a protease inhibitor (PI). Cobicistat 0-10 TATA-box binding protein associated factor 8 Homo sapiens 100-103 31034908-4 2019 The present study was aimed to investigate the translation of in vitro MATE1/2K inhibition to clinical creatinine increase (cobicistat) and lack of it (ritonavir) considering their intracellular concentrations in renal proximal tubules. Cobicistat 124-134 solute carrier family 47 member 1 Homo sapiens 71-76 31034908-7 2019 Ritonavir and cobicistat are MATE1 and MATE2K inhibitors with IC50 values of 3.1 and 90 muM (ritonavir), and 4.4 and 3.2 muM (cobicistat), respectively. Cobicistat 14-24 solute carrier family 47 member 1 Homo sapiens 29-34 31034908-7 2019 Ritonavir and cobicistat are MATE1 and MATE2K inhibitors with IC50 values of 3.1 and 90 muM (ritonavir), and 4.4 and 3.2 muM (cobicistat), respectively. Cobicistat 14-24 solute carrier family 47 member 2 Homo sapiens 39-45 31034908-7 2019 Ritonavir and cobicistat are MATE1 and MATE2K inhibitors with IC50 values of 3.1 and 90 muM (ritonavir), and 4.4 and 3.2 muM (cobicistat), respectively. Cobicistat 14-24 latexin Homo sapiens 88-91 31034908-7 2019 Ritonavir and cobicistat are MATE1 and MATE2K inhibitors with IC50 values of 3.1 and 90 muM (ritonavir), and 4.4 and 3.2 muM (cobicistat), respectively. Cobicistat 14-24 latexin Homo sapiens 121-124 31034908-8 2019 However, the unbound cytosolic concentrations (Cu,cytosol) of ritonavir and cobicistat in human renal proximal tubule epithelial cells, 0.065 and 0.10 muM, respectively, after incubation with the clinical maximum total plasma concentrations at pharmacoenhancer doses does not support inhibition in vivo; Cu,cytosol >30 fold lower than IC50s. Cobicistat 76-86 latexin Homo sapiens 151-154 30508308-1 2019 Darunavir/cobicistat/emtricitabine/tenofovir alafenamide (D/C/F/TAF) is an oral once-daily single-tablet regimen for the treatment of human immunodeficiency virus-1 infection. Cobicistat 10-20 TATA-box binding protein associated factor 8 Homo sapiens 64-67 31933482-1 2019 BACKGROUND: Cobicistat (COBI), a CYP3A inhibitor, is a pharmacokinetic enhancer that increases exposures of the HIV protease inhibitors (PIs) atazanavir (ATV) and darunavir (DRV). Cobicistat 12-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-38 31933482-1 2019 BACKGROUND: Cobicistat (COBI), a CYP3A inhibitor, is a pharmacokinetic enhancer that increases exposures of the HIV protease inhibitors (PIs) atazanavir (ATV) and darunavir (DRV). Cobicistat 24-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-38 31933482-11 2019 CONCLUSIONS: Consistent with COBI-mediated CYP3A inhibition, drospirenone exposure increased following coadministration with COBI-containing regimens, with a greater increase with ATV+COBI. Cobicistat 29-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-48 30798679-1 2019 Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide (E/C/F/TAF) is a potent fixed-dose, once-daily regimen for HIV-1 treatment and has rare emergence of drug resistance. Cobicistat 13-23 TATA-box binding protein associated factor 8 Homo sapiens 67-70 30951643-1 2019 INTRODUCTION: Drugs used in HIV treatment; all protease inhibitors, some non-nucleoside reverse transcriptase inhibitors, and pharmacoenhancers ritonavir and cobicistat can inhibit cytochrome P450 (CYP) enzymes. Cobicistat 158-168 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 181-196 30951643-1 2019 INTRODUCTION: Drugs used in HIV treatment; all protease inhibitors, some non-nucleoside reverse transcriptase inhibitors, and pharmacoenhancers ritonavir and cobicistat can inhibit cytochrome P450 (CYP) enzymes. Cobicistat 158-168 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 198-201 27843352-10 2016 Therefore, isoenzyms different from CYP3A4 are supposed to be less affected by cobicistat, and thus fewer drug-drug interactions are expected. Cobicistat 79-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-42 30252923-0 2018 Glomerular filtration rate estimated by cystatin C formulas in HIV-1 patients treated with dolutegravir, rilpivirine or cobicistat. Cobicistat 120-130 cystatin C Homo sapiens 40-50 28961682-0 2018 Effect of Cobicistat on Tenofovir Disoproxil Fumarate (TDF): What Is True for TAF May Also Be True for TDF. Cobicistat 10-20 TATA-box binding protein associated factor 8 Homo sapiens 78-81 28895486-8 2017 The EVG/c/TDF/FTC contains cobicistat, a strong cytochrome P450 3A4 (CYP3A4) inhibitor, which can potentiate drug interactions involving metabolizing of medications via this pathway. Cobicistat 27-37 sex determining region Y Homo sapiens 10-13 28895486-8 2017 The EVG/c/TDF/FTC contains cobicistat, a strong cytochrome P450 3A4 (CYP3A4) inhibitor, which can potentiate drug interactions involving metabolizing of medications via this pathway. Cobicistat 27-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-67 28895486-8 2017 The EVG/c/TDF/FTC contains cobicistat, a strong cytochrome P450 3A4 (CYP3A4) inhibitor, which can potentiate drug interactions involving metabolizing of medications via this pathway. Cobicistat 27-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 28848011-0 2017 Differential Influence of the Antiretroviral Pharmacokinetic Enhancers Ritonavir and Cobicistat on Intestinal P-Glycoprotein Transport and the Pharmacokinetic/Pharmacodynamic Disposition of Dabigatran. Cobicistat 85-95 ATP binding cassette subfamily B member 1 Homo sapiens 110-124 27809711-9 2016 Renal AEs were more frequent when TDF was taken with protease inhibitor (PI)- or cobicistat-containing ART. Cobicistat 81-91 sex determining region Y Homo sapiens 34-37 29649076-9 2018 Coadministration with P-gp/BCRP inhibitors such as cobicistat or PI-based regimens (ATV + RTV, LPV/r, or DRV + RTV) resulted in a range of 6%-183% increases in TAF and 105%-316% increases in TFV exposure, whereas coadministration with a P-gp inducer, efavirenz, resulted in a 15%-24% decrease in TAF and TFV exposure. Cobicistat 51-61 ATP binding cassette subfamily B member 1 Homo sapiens 22-26 29649076-9 2018 Coadministration with P-gp/BCRP inhibitors such as cobicistat or PI-based regimens (ATV + RTV, LPV/r, or DRV + RTV) resulted in a range of 6%-183% increases in TAF and 105%-316% increases in TFV exposure, whereas coadministration with a P-gp inducer, efavirenz, resulted in a 15%-24% decrease in TAF and TFV exposure. Cobicistat 51-61 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 27-31 29649076-9 2018 Coadministration with P-gp/BCRP inhibitors such as cobicistat or PI-based regimens (ATV + RTV, LPV/r, or DRV + RTV) resulted in a range of 6%-183% increases in TAF and 105%-316% increases in TFV exposure, whereas coadministration with a P-gp inducer, efavirenz, resulted in a 15%-24% decrease in TAF and TFV exposure. Cobicistat 51-61 ATP binding cassette subfamily B member 1 Homo sapiens 237-241 28891378-0 2018 In vitro inhibition of human UGT isoforms by ritonavir and cobicistat. Cobicistat 59-69 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 29-32 28891378-3 2018 The manufacturer"s data suggests that cobicistat is a more selective CYP3A4 inhibitor than ritonavir. Cobicistat 38-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 28891378-4 2018 However, the inhibitory effect of ritonavir and cobicistat on human UDP glucuronosyltransferase (UGT) enzymes in Phase II metabolism is not established. Cobicistat 48-58 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 68-95 28891378-4 2018 However, the inhibitory effect of ritonavir and cobicistat on human UDP glucuronosyltransferase (UGT) enzymes in Phase II metabolism is not established. Cobicistat 48-58 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 97-100 29767543-3 2018 Cobicistat-boosted darunavir along with emtricitabine and tenofovir alafenamide co-formulation (DRV/c/FTC/TAF or the trade name Symtuza ) is the first marketed protease inhibitor-based fixed-dose combination regimen for the treatment of HIV infection. Cobicistat 0-10 TATA-box binding protein associated factor 8 Homo sapiens 106-109 28960344-1 2017 OBJECTIVES: Ritonavir and cobicistat are strong inhibitors of human cytochrome P450-3A (CYP3A) isoforms, and are used clinically as pharmacokinetic boosting agents for other antiretroviral drugs. Cobicistat 26-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-86 28960344-1 2017 OBJECTIVES: Ritonavir and cobicistat are strong inhibitors of human cytochrome P450-3A (CYP3A) isoforms, and are used clinically as pharmacokinetic boosting agents for other antiretroviral drugs. Cobicistat 26-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-93 28960344-2 2017 Data reported by the manufacturer suggest that cobicistat is a more selective inhibitor of CYP3A than ritonavir. Cobicistat 47-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-96 28960344-6 2017 KEY FINDINGS: Ritonavir and cobicistat both were strong inhibitors of CYP3A4, with IC50 values of 0.014 and 0.032 mum, respectively. Cobicistat 28-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 70-76 28960344-10 2017 CONCLUSIONS: Consistent with previous reports, both ritonavir and cobicistat were highly potent inhibitors of CYP3A. Cobicistat 66-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-115 28443391-3 2017 Areas covered: Atazanavir sulfate + cobicistat (ATV/c) was recently approved for the treatment of HIV-1 infection. Cobicistat 36-46 nibrin Homo sapiens 48-53 28443391-4 2017 Bioequivalence between cobicistat (COBI) and ritonavir (RTV) as a pharmacoenhancer of ATV was established. Cobicistat 23-33 nibrin Homo sapiens 86-89 28443391-4 2017 Bioequivalence between cobicistat (COBI) and ritonavir (RTV) as a pharmacoenhancer of ATV was established. Cobicistat 35-39 nibrin Homo sapiens 86-89 27171740-1 2016 Coformulated elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide (E/C/F/TAF) has high efficacy and improved renal and bone safety in multiple phase 3 trials; TAF single agent is being studied in 2 phase 3 trials in patients with chronic hepatitis B. Cobicistat 27-37 TATA-box binding protein associated factor 8 Homo sapiens 173-176 27697800-1 2016 Ritonavir and cobicistat, used as pharmacokinetic enhancers in combination with some antiretrovirals (ARVs) for the treatment of HIV, are potent inhibitors of the CYP3A4 isoenzyme. Cobicistat 14-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 163-169 27697800-2 2016 Most glucocorticoids are metabolised via the CYP3A4 pathway and iatrogenic Cushing"s syndrome (ICS), with possible secondary adrenal insufficiency (SAI), is a recognised complication following co-administration with ritonavir or cobicistat. Cobicistat 229-239 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 25164142-6 2014 Both agents inhibit CYP3A4, with cobicistat being a more specific CYP inhibitor than ritonavir. Cobicistat 33-43 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 26945713-3 2016 Cobicistat and ritonavir are equally strong inhibitors of cytochrome P450 (CYP) 3A4 and consequently were shown to be equivalent pharmacokinetic enhancers for elvitegravir and for the PIs atazanavir and darunavir. Cobicistat 0-10 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 58-73 26945713-3 2016 Cobicistat and ritonavir are equally strong inhibitors of cytochrome P450 (CYP) 3A4 and consequently were shown to be equivalent pharmacokinetic enhancers for elvitegravir and for the PIs atazanavir and darunavir. Cobicistat 0-10 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 75-78 26945713-4 2016 Since cobicistat is a more selective CYP inhibitor than ritonavir and is devoid of enzyme-inducing properties, differences are expected in their interaction profiles with some co-medications. Cobicistat 6-16 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 37-40 27196356-1 2016 Cobicistat and ritonavir are structurally distinct compounds that both potently inhibit cytochrome P450 (CYP) 3A, the metabolizing enzyme primarily responsible for the elimination of several antiretroviral medications, and, as such, are pharmacokinetic boosters for antiretroviral agents that require longer dosing intervals. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-112 26935921-8 2016 Consistent with the previous report, CYP3A4 and CYP2D6 were determined as the major enzymes that contribute to COBI metabolism. Cobicistat 111-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 26935921-8 2016 Consistent with the previous report, CYP3A4 and CYP2D6 were determined as the major enzymes that contribute to COBI metabolism. Cobicistat 111-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 48-54 25331712-9 2015 However, the INI elvitegravir, which is given in combination with cobicistat, requires a dose of estrogen of at least 30 microg. Cobicistat 66-76 PHD finger protein 5A Homo sapiens 13-16 26872388-0 2016 Effect of Ethanol on the Metabolic Characteristics of HIV-1 Integrase Inhibitor Elvitegravir and Elvitegravir/Cobicistat with CYP3A: An Analysis Using a Newly Developed LC-MS/MS Method. Cobicistat 110-120 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-131 26872388-12 2016 However, in the presence of COBI we were unable to determine these parameters effectively because COBI, being a strong inhibitor of CYP3A4, blocked the EVG/ethanol-CYP3A4 interactions. Cobicistat 98-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 132-138 26872388-12 2016 However, in the presence of COBI we were unable to determine these parameters effectively because COBI, being a strong inhibitor of CYP3A4, blocked the EVG/ethanol-CYP3A4 interactions. Cobicistat 98-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 164-170 26872388-13 2016 Docking studies predicted a shift of EVG or COBI binding to the active site of CYP3A4 in the presence of ethanol. Cobicistat 44-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 79-85 26566368-3 2015 The rationale behind COBI development was to provide an alternative to ritonavir (RTV) as a protease inhibitor pharmacoenhancer, due to associated adverse events with short- and long-term RTV use, such as gastrointestinal intolerability, drug-drug interactions, insulin resistance, lipodystrophy, and hyperlipidemia. Cobicistat 21-25 insulin Homo sapiens 262-269 26347243-1 2015 INTRODUCTION: We present what we believe to be the first case in the literature of rhabdomyolysis-induced renal failure caused by a probable drug interaction between elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate (EVG/COBI/FTC/TDF) and pravastatin/fenofibrate. Cobicistat 179-189 sex determining region Y Homo sapiens 248-251 26319088-11 2015 Moreover, as cobicistat is metabolized predominantly by CYP3A, plasma concentrations may increase or decrease on coadministration with CYP3A inhibitors or inducers, respectively. Cobicistat 13-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-61 26319088-11 2015 Moreover, as cobicistat is metabolized predominantly by CYP3A, plasma concentrations may increase or decrease on coadministration with CYP3A inhibitors or inducers, respectively. Cobicistat 13-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-140 26035169-0 2015 Rezolsta (Darunavir/Cobicistat): First Boosted Protease Inhibitor Co-formulated with Cobicistat. Cobicistat 21-31 serpin family A member 13, pseudogene Homo sapiens 48-66 26035169-1 2015 Rezolsta (darunavir/cobicistat) is the first boosted protease inhibitor in a fixed-dose combination to be approved for the treatment of HIV infection. Cobicistat 21-31 serpin family A member 13, pseudogene Homo sapiens 54-72 24375014-8 2014 Elvitegravir and cobicistat inhibited BCRP and OATP in vitro, emtricitabine and TDF did not. Cobicistat 17-27 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 38-42 24646860-7 2014 Similar to cimetidine and ritonavir, cobicistat had the greatest effect on MATE1 with a 50% inhibition constant of 0.99 muM for creatinine transport. Cobicistat 37-47 solute carrier family 47 member 1 Homo sapiens 75-80 24798279-3 2014 Since ritonavir-boosted regimens are associated with long-term adverse events, cobicistat, a CYP3A4 inhibitor without antiviral activity, has been developed. Cobicistat 79-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 25350960-1 2014 OBJECTIVE: To describe baseline and emergent HIV-1 resistance to elvitegravir/ cobicistat/emtricitabine/tenofovir DF (EVG/COBI/FTC/TDF) and ritonavir-boosted atazanavir/emtricitabine/tenofovir DF (ATV+RTV+FTC/TDF) in HIV-1-infected, treatment-naive subjects through 144 weeks. Cobicistat 79-89 sex determining region Y Homo sapiens 131-134 24375014-8 2014 Elvitegravir and cobicistat inhibited BCRP and OATP in vitro, emtricitabine and TDF did not. Cobicistat 17-27 solute carrier organic anion transporter family member 1A2 Homo sapiens 47-51 24900196-1 2010 Cobicistat (3, GS-9350) is a newly discovered, potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-106 24412072-6 2014 Through these efforts, a potent and selective inhibitor of CYP3A, GS-9350 (cobicistat) with improved physiochemical properties was discovered. Cobicistat 75-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-64 24805065-3 2014 Currently, the CYP3A4 inhibitor ritonavir and its derivative cobicistat are prescribed to HIV patients as pharmacoenhancers. Cobicistat 61-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 25030944-1 2014 Elvitegravir/cobicistat/emtricitabine/tenofovirDF (EVG/COBI/FTC/TDF) is the new single-tablet, fixed-dose formulation containing an integrase strand transfer inhibitor recently approved as antiretroviral treatment. Cobicistat 13-23 sex determining region Y Homo sapiens 64-67 23746300-1 2013 Cytochrome P450 3A4 (CYP3A4) inhibitors ritonavir and cobicistat, currently administered to HIV patients as pharmacoenhancers, were designed on the basis of the chemical structure/activity relationships rather than the CYP3A4 crystal structure. Cobicistat 54-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 23746300-1 2013 Cytochrome P450 3A4 (CYP3A4) inhibitors ritonavir and cobicistat, currently administered to HIV patients as pharmacoenhancers, were designed on the basis of the chemical structure/activity relationships rather than the CYP3A4 crystal structure. Cobicistat 54-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 23746300-1 2013 Cytochrome P450 3A4 (CYP3A4) inhibitors ritonavir and cobicistat, currently administered to HIV patients as pharmacoenhancers, were designed on the basis of the chemical structure/activity relationships rather than the CYP3A4 crystal structure. Cobicistat 54-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 219-225 23616950-1 2013 Cobicistat is a novel cytochrome P450 3A4 (CYP3A4) inhibitor in advanced clinical evaluation for use as a pharmacoenhancer of antiretroviral drugs. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-41 23616950-1 2013 Cobicistat is a novel cytochrome P450 3A4 (CYP3A4) inhibitor in advanced clinical evaluation for use as a pharmacoenhancer of antiretroviral drugs. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 22850510-1 2012 The experimental pharmacoenhancer cobicistat (COBI), a potent mechanism-based inhibitor of cytochrome P450 3A enzymes, was found to inhibit the intestinal efflux transporters P-glycoprotein and breast cancer resistance protein. Cobicistat 34-44 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 194-226 22850510-1 2012 The experimental pharmacoenhancer cobicistat (COBI), a potent mechanism-based inhibitor of cytochrome P450 3A enzymes, was found to inhibit the intestinal efflux transporters P-glycoprotein and breast cancer resistance protein. Cobicistat 46-50 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 194-226 24900196-0 2010 Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 24343782-2 2014 Cobicistat has a lower potential for off-target drug interactions than the standard boosting agent ritonavir, due to its more selective inhibition of CYP3A and lower likelihood for enzymatic induction, and is devoid of anti-HIV activity. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-155 24100879-9 2013 The selective cytochrome P450 3A4 inhibitor cobicistat is a better tolerated alternative to ritonavir for pharmacokinetic "boosting", but may also result in clinically undesirable drug interactions. Cobicistat 44-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-33 23896476-2 2013 COBI and TFV have been reported to interact with distinct transporters in renal proximal tubules; while TFV is renally eliminated by a combination of glomerular filtration and tubular secretion via anion transporters OAT1, OAT3, and MRP4, COBI inhibits renal cation transporters, particularly MATE1, resulting in a measurable decrease in the tubular secretion of creatinine. Cobicistat 0-4 solute carrier family 22 member 6 Homo sapiens 217-221 23896476-2 2013 COBI and TFV have been reported to interact with distinct transporters in renal proximal tubules; while TFV is renally eliminated by a combination of glomerular filtration and tubular secretion via anion transporters OAT1, OAT3, and MRP4, COBI inhibits renal cation transporters, particularly MATE1, resulting in a measurable decrease in the tubular secretion of creatinine. Cobicistat 0-4 solute carrier family 22 member 8 Homo sapiens 223-227 23896476-2 2013 COBI and TFV have been reported to interact with distinct transporters in renal proximal tubules; while TFV is renally eliminated by a combination of glomerular filtration and tubular secretion via anion transporters OAT1, OAT3, and MRP4, COBI inhibits renal cation transporters, particularly MATE1, resulting in a measurable decrease in the tubular secretion of creatinine. Cobicistat 0-4 ATP binding cassette subfamily C member 4 Homo sapiens 233-237 23896476-2 2013 COBI and TFV have been reported to interact with distinct transporters in renal proximal tubules; while TFV is renally eliminated by a combination of glomerular filtration and tubular secretion via anion transporters OAT1, OAT3, and MRP4, COBI inhibits renal cation transporters, particularly MATE1, resulting in a measurable decrease in the tubular secretion of creatinine. Cobicistat 0-4 solute carrier family 47 member 1 Homo sapiens 293-298 23703578-11 2013 Cobicistat is a new potent CYP3A inhibitor that is combined with elvitegravir and will be combined with HIV-PIs in the future. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-32 22321026-7 2012 Trials investigating the efficacy of once-daily co-formulated elvitegravir/cobicistat/emtricitabine/tenofovir (EVG/COBI/FTC/TDF) demonstrate a high rate of virologic suppression with fewer CNS and psychiatric adverse events compared with co-formulated efavirenz/emtricitabine/tenofovir. Cobicistat 75-85 sex determining region Y Homo sapiens 124-127 21348537-6 2011 The presence of a strong CYP3A inhibitor such as ritonavir or cobicistat renders the potential for increase in systemic exposures of CYP3A substrates coadministered with boosted elvitegravir. Cobicistat 62-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-30 21348537-6 2011 The presence of a strong CYP3A inhibitor such as ritonavir or cobicistat renders the potential for increase in systemic exposures of CYP3A substrates coadministered with boosted elvitegravir. Cobicistat 62-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 133-138 24900196-1 2010 Cobicistat (3, GS-9350) is a newly discovered, potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes. Cobicistat 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-113 35229634-3 2022 Here, we show that cobicistat, which is an FDA-approved drug booster that blocks the activity of the drug-metabolizing proteins cytochrome P450-3As (CYP3As) and P-glycoprotein (P-gp), inhibits SARS-CoV-2 replication. Cobicistat 19-29 ATP binding cassette subfamily B member 1 Homo sapiens 161-175 34934565-4 2021 This report presents a patient who received a femoral artery stent and developed a large retroperitoneal hemorrhage after she was prescribed apixaban in addition to her antiretroviral therapy (AVT) regimen that included cobicistat, a strong CYP3A4 inhibitor. Cobicistat 220-230 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 241-247 35598441-2 2022 We investigated the safety, tolerability, and pharmacokinetics of a multidose SJ733 regimen and a single-dose pharmacoboost approach using cobicistat to inhibit CYP3A4, thereby increasing exposure. Cobicistat 139-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-167 34185564-11 2021 The incremental QALY and cost savings for DTG/3TC compared with DTG/abacavir(ABC)/3TC, cobicistat-boosted darunavir(DRV/c)/tenofovir alafenamide(TAF)/FTC, and bictegravir (BIC)/TAF/FTC, based on NMA results were 0.465, 0.142, and 0.698, and $42,948, $122,846, and $44,962, respectively. Cobicistat 87-97 TATA-box binding protein associated factor 8 Homo sapiens 145-148 35229634-3 2022 Here, we show that cobicistat, which is an FDA-approved drug booster that blocks the activity of the drug-metabolizing proteins cytochrome P450-3As (CYP3As) and P-glycoprotein (P-gp), inhibits SARS-CoV-2 replication. Cobicistat 19-29 ATP binding cassette subfamily B member 1 Homo sapiens 177-181 35229634-4 2022 Two independent cell-to-cell membrane fusion assays showed that the antiviral effect of cobicistat is exerted through inhibition of spike protein-mediated membrane fusion. Cobicistat 88-98 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 132-137 35229634-7 2022 This was consistent with the effects of cobicistat on two of its known targets, CYP3A4 and P-gp, the silencing of which boosted the in vitro antiviral activity of remdesivir in a cobicistat-like manner. Cobicistat 40-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 35229634-7 2022 This was consistent with the effects of cobicistat on two of its known targets, CYP3A4 and P-gp, the silencing of which boosted the in vitro antiviral activity of remdesivir in a cobicistat-like manner. Cobicistat 40-50 phosphoglycolate phosphatase Homo sapiens 91-95 35229634-7 2022 This was consistent with the effects of cobicistat on two of its known targets, CYP3A4 and P-gp, the silencing of which boosted the in vitro antiviral activity of remdesivir in a cobicistat-like manner. Cobicistat 179-189 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 35229634-7 2022 This was consistent with the effects of cobicistat on two of its known targets, CYP3A4 and P-gp, the silencing of which boosted the in vitro antiviral activity of remdesivir in a cobicistat-like manner. Cobicistat 179-189 phosphoglycolate phosphatase Homo sapiens 91-95 33300183-1 2021 In AMBER and EMERALD, darunavir/cobicistat/emtricitabine/tenofovir alafenamide (D/C/F/TAF) 800/150/200/10mg demonstrated high virological response and low virological failure (VF) through week 96. Cobicistat 32-42 TATA-box binding protein associated factor 8 Homo sapiens 86-89 33830489-3 2021 We report three cases of cobicistat-tacrolimus co-administration, two of which also include the co-administration of mTOR inhibitors, in HIV-positive patients undergoing SOT (2 kidney and 1 liver recipient). Cobicistat 25-35 mechanistic target of rapamycin kinase Homo sapiens 117-121 33501995-1 2021 BACKGROUND: Cobicistat, dolutegravir and rilpivirine are all modest inhibitors of proximal tubular creatinine secretion (IPTCrS) and hence a moderate and early non-progressive creatinine estimated glomerular filtration rate (Cr-eGFR) reduction has been observed in clinical trials. Cobicistat 12-22 epidermal growth factor receptor Homo sapiens 228-232 33629115-0 2021 Targeting xenobiotic nuclear receptors PXR and CAR to prevent cobicistat hepatotoxicity. Cobicistat 62-72 nuclear receptor subfamily 1 group I member 2 Homo sapiens 39-42 33629115-0 2021 Targeting xenobiotic nuclear receptors PXR and CAR to prevent cobicistat hepatotoxicity. Cobicistat 62-72 nuclear receptor subfamily 1 group I member 3 Homo sapiens 47-50 33398250-8 2020 We found that cobicistat is the most efficient inhibitor of Mpro both in silico and in vitro. Cobicistat 14-24 NEWENTRY Severe acute respiratory syndrome-related coronavirus 60-64 33222380-0 2021 Pharmacoenhancement of Low Crizotinib Plasma Concentrations in Patients with Anaplastic Lymphoma Kinase-Positive Non-Small Cell Lung Cancer using the CYP3A Inhibitor Cobicistat. Cobicistat 166-176 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-155 33222380-3 2021 We investigated whether the CYP3A inhibitor cobicistat increases Cmin,ss of the CYP3A substrate crizotinib in patients with low exposure. Cobicistat 44-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-33 33222380-3 2021 We investigated whether the CYP3A inhibitor cobicistat increases Cmin,ss of the CYP3A substrate crizotinib in patients with low exposure. Cobicistat 44-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-85 32140912-11 2020 CYP3A4 inhibitors such as ritonavir or cobicistat may increase the chance of this adverse effect. Cobicistat 39-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 31516033-1 2020 Darunavir/cobicistat/emtricitabine/tenofovir alafenamide (D/C/F/TAF) 800/150/200/10 mg is being investigated in two Phase III trials. Cobicistat 10-20 TATA-box binding protein associated factor 8 Homo sapiens 64-67 32741313-6 2021 Our studies have identified six potential inhibitors of Mpro enzyme, out of which four are commercially available FDA approved drugs (Cobicistat, Iopromide, Cangrelor, and Fortovase) and two are from Specs database of natural compounds (Hopeaphenol and Cyclosieversiodide-A). Cobicistat 134-144 NEWENTRY Severe acute respiratory syndrome-related coronavirus 56-60 32479865-2 2020 METHODS: Prezcobix/Rezolsta is a fixed-dose combination of 800 mg of the HIV protease inhibitor darunavir (DRV) and 150 mg cobicistat, a CYP3A4 inhibitor, which is indicated in combination with other antiretroviral agents for the treatment of HIV infection. Cobicistat 123-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 137-143 32684114-4 2021 The results showed that DB02388 and Cobicistat (DB09065) exhibited potential binding affinities towards Mpro over 100 ns MD simulations, with binding energy values of -49.67 and -46.60 kcal/mol, respectively. Cobicistat 36-46 NEWENTRY Severe acute respiratory syndrome-related coronavirus 104-108 32684114-6 2021 The potency of DB02388 and Cobicistat is attributed to their abilities to form several hydrogen bonds with the essential amino acids inside the active site of Mpro. Cobicistat 27-37 NEWENTRY Severe acute respiratory syndrome-related coronavirus 159-163 32984524-2 2020 The prompt recognition of this drug-drug interaction is critical to avoid adverse outcomes when glucocorticoids are used with anti-retroviral treatment containing cobicistat, a potent cytochrome P450 3A (CYP3A4) inhibitor. Cobicistat 163-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 204-210 32984524-12 2020 Conclusion: It is essential to avoid drugs that include cobicistat when administering glucocorticoids that are metabolized via the CYP3A4 pathway due to the risk of developing Cushing syndrome and secondary adrenal insufficiency. Cobicistat 56-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-137