PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 28053220-8 2017 In this study, in vitro inhibition assays using rivaroxaban as the probe substrate demonstrated that both dronedarone and NDBD produced reversible inhibition as well as irreversible mechanism-based inactivation of CYP3A4- and CYP2J2-mediated metabolism of rivaroxaban. N-desbutyldronedarone 122-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 214-220 26490246-0 2016 Inactivation of Human Cytochrome P450 3A4 and 3A5 by Dronedarone and N-Desbutyl Dronedarone. N-desbutyldronedarone 69-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-41 26490246-4 2016 We demonstrated for the first time that both dronedarone and its main metabolite N-desbutyl dronedarone (NDBD) inactivate CYP3A4 and CYP3A5 in a time-, concentration-, and NADPH-dependent manner. N-desbutyldronedarone 81-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 26490246-4 2016 We demonstrated for the first time that both dronedarone and its main metabolite N-desbutyl dronedarone (NDBD) inactivate CYP3A4 and CYP3A5 in a time-, concentration-, and NADPH-dependent manner. N-desbutyldronedarone 105-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 26490246-5 2016 For the inactivation of CYP3A4, the inactivator concentration at the half-maximum rate of inactivation and inactivation rate constant at an infinite inactivator concentration are 0.87 microM and 0.039 minute(-1), respectively, for dronedarone, and 6.24 microM and 0.099 minute(-1), respectively, for NDBD. N-desbutyldronedarone 300-304 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 26490246-7 2016 The partition ratios for the inactivation of CYP3A4 and CYP3A5 by dronedarone are 51.1 and 32.2, and the partition ratios for the inactivation of CYP3A4 and CYP3A5 by NDBD are 35.3 and 36.6. N-desbutyldronedarone 167-171 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 26490246-7 2016 The partition ratios for the inactivation of CYP3A4 and CYP3A5 by dronedarone are 51.1 and 32.2, and the partition ratios for the inactivation of CYP3A4 and CYP3A5 by NDBD are 35.3 and 36.6. N-desbutyldronedarone 167-171 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 26490246-8 2016 Testosterone protected both CYP3A4 and CYP3A5 from inactivation by dronedarone and NDBD. N-desbutyldronedarone 83-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 28053220-4 2017 Amiodarone, dronedarone, and their major metabolites, N-desethylamiodarone (NDEA) and N-desbutyldronedarone (NDBD), demonstrate inhibitory effects on CYP3A4 and CYP2J2 with U.S. Food and Drug Administration-recommended probe substrates. N-desbutyldronedarone 86-107 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 28053220-4 2017 Amiodarone, dronedarone, and their major metabolites, N-desethylamiodarone (NDEA) and N-desbutyldronedarone (NDBD), demonstrate inhibitory effects on CYP3A4 and CYP2J2 with U.S. Food and Drug Administration-recommended probe substrates. N-desbutyldronedarone 109-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 26490246-10 2016 MBI of CYP3A4 and CYP3A5 was further supported by the discovery of glutathione adducts derived from the quinone oxime intermediates of dronedarone and NDBD. N-desbutyldronedarone 151-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 7-13 26490246-11 2016 In conclusion, dronedarone and NDBD inactivate CYP3A4 and CYP3A5 via unique dual mechanisms of MBI and formation of the metabolite-intermediate complex. N-desbutyldronedarone 31-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53