PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 24654690-3 2014 A dual functional hexynylated 17alpha-ethynylestradiol activity-based probe was synthesized for specifically labeling CYP3A4 and then CC-mediated Eu-tagging with an azido-DOTA-Eu complex for CYP3A4 quantification and activity measurement in human liver microsome and serum samples using (153)Eu SUID ICPMS. Ethinyl Estradiol 30-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 27273461-0 2017 Pharmacokinetic Evaluation of CYP3A4-Mediated Drug-Drug Interactions of Isavuconazole With Rifampin, Ketoconazole, Midazolam, and Ethinyl Estradiol/Norethindrone in Healthy Adults. Ethinyl Estradiol 130-147 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 24997757-1 2015 Pharmacokinetic (PK) interactions between the cytochrome P450 3A4 (CYP3A4) pathway and transdermally administered ethinyl estradiol (EE) and gestodene (GSD) were investigated. Ethinyl Estradiol 114-131 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-65 24997757-1 2015 Pharmacokinetic (PK) interactions between the cytochrome P450 3A4 (CYP3A4) pathway and transdermally administered ethinyl estradiol (EE) and gestodene (GSD) were investigated. Ethinyl Estradiol 114-131 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 24654690-3 2014 A dual functional hexynylated 17alpha-ethynylestradiol activity-based probe was synthesized for specifically labeling CYP3A4 and then CC-mediated Eu-tagging with an azido-DOTA-Eu complex for CYP3A4 quantification and activity measurement in human liver microsome and serum samples using (153)Eu SUID ICPMS. Ethinyl Estradiol 30-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 191-197 24161160-4 2014 gov number: NCT00739622) evaluated the interaction between rilpivirine and ethinylestradiol/norethindrone (combination oral contraceptives), which are metabolized by multiple pathways, including CYP3A4. Ethinyl Estradiol 75-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 195-201 19454483-1 2009 17alpha-Ethinyl estradiol (EE) was systematically evaluated as a reversible and time-dependent inhibitor of 11 human drug-metabolizing cytochromes P450 (P450s) (CYP1A1, CYP1A2, CYP1B1, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2J2, CYP3A4, and CYP3A5) in vitro. Ethinyl Estradiol 0-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 234-240 22809252-5 2012 In addition, the 1,2,3-TRZ fragment was incorporated into a well-established CYP3A4 substrate and mechanism-based inactivator, 17-alpha-ethynylestradiol (17EE), via click chemistry. Ethinyl Estradiol 127-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-83 22809252-5 2012 In addition, the 1,2,3-TRZ fragment was incorporated into a well-established CYP3A4 substrate and mechanism-based inactivator, 17-alpha-ethynylestradiol (17EE), via click chemistry. Ethinyl Estradiol 154-158 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-83 18294327-2 2008 * Ethinyl oestradiol and norethindrone, components of the combination oral contraceptive drug Ortho-Novum 1/35, also are substrates of cytochrome P450 CYP2C19 and CYP3A4 isozymes. Ethinyl Estradiol 2-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 163-169 16837568-10 2006 This score was then correlated with decreases in area under the plasma concentration versus time curve values for coadministered CYP3A4 object drugs (midazolam or ethinylestradiol) from previously published clinical DDI studies. Ethinyl Estradiol 163-179 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 17284510-3 2007 Ethinyl estradiol (EE), commonly found in oral contraceptives (OCs), is a known CYP3A4 substrate. Ethinyl Estradiol 0-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 16261523-2 2005 It has been shown to induce the activity of cytochrome P-450 3A4 (CYP3A4) and to increase the clearance of numerous drugs and steroids such as cortisol and ethinyl estradiol. Ethinyl Estradiol 156-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-64 16261523-2 2005 It has been shown to induce the activity of cytochrome P-450 3A4 (CYP3A4) and to increase the clearance of numerous drugs and steroids such as cortisol and ethinyl estradiol. Ethinyl Estradiol 156-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 15764719-7 2005 In vitro interaction studies with CYP3A4 substrates and possible concomitant medication demonstrated that laquinimod inhibits the metabolism of ethinyl estradiol with an IC50 value of about 150 microM, which is high above the plasma level of laquinimod after clinically relevant doses. Ethinyl Estradiol 144-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 15304426-0 2004 The involvement of CYP3A4 and CYP2C9 in the metabolism of 17 alpha-ethinylestradiol. Ethinyl Estradiol 58-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 14636322-12 2003 CONCLUSIONS: The observed induction of CYP3A4 by TPM, especially at the higher concentrations, provides a potential mechanistic explanation of the reported increase in the ethinyl estradiol clearance by TPM. Ethinyl Estradiol 172-189 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 15554232-8 2004 It was realized that the cytochrome P450 isoenzyme 3A4 (CYP3A4) is the major CYP isozyme in the human liver metabolizing a variety of xenobiotics and endobiotics, being also responsible for the 2-hydroxylation of ethinylestradiol. Ethinyl Estradiol 213-229 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-54 15554232-8 2004 It was realized that the cytochrome P450 isoenzyme 3A4 (CYP3A4) is the major CYP isozyme in the human liver metabolizing a variety of xenobiotics and endobiotics, being also responsible for the 2-hydroxylation of ethinylestradiol. Ethinyl Estradiol 213-229 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 15554232-9 2004 The inducibility of CYP3A4 by barbiturates and rifampicin explains the effects of inducers to enhance the clearance of ethynylestradiol and thereby to reduce the effectiveness of oral contraceptives, rifampicin being one of the most potent inducers of human CYP3A4 gene expression. Ethinyl Estradiol 119-135 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 15554232-9 2004 The inducibility of CYP3A4 by barbiturates and rifampicin explains the effects of inducers to enhance the clearance of ethynylestradiol and thereby to reduce the effectiveness of oral contraceptives, rifampicin being one of the most potent inducers of human CYP3A4 gene expression. Ethinyl Estradiol 119-135 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 258-264 10898107-10 2000 The point estimates of rGC for composite (hepatic + intestinal) CYP3A4 activity measured after oral administration of cyclosporine, ethinylestradiol, ethylmorphine, nifedipine and nitrendipine, ranged from 0.66-0.98 (median: 0.83) (P < 0.05). Ethinyl Estradiol 132-148 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-70 12537513-14 2003 The only substantive interactions observed were with ethinylestradiol and triazolam, apparently through induction of CYP3A4, primarily in the gastrointestinal system. Ethinyl Estradiol 53-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-123 11907170-0 2002 Mechanism-based inactivation of cytochrome P450 3A4 by 17 alpha-ethynylestradiol: evidence for heme destruction and covalent binding to protein. Ethinyl Estradiol 55-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-51 11012556-1 2000 AIMS: To characterize the effect of an oral contraceptive (OC) containing ethinylestradiol and gestodene on the activity of CYP3A4 in vivo as measured by the 1"-hydroxylation of midazolam. Ethinyl Estradiol 74-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-130 11012556-8 2000 This study suggests that, at the doses used, ethinylestradiol and gestodene have a relatively small effect on CYP3A4 activity in vivo. Ethinyl Estradiol 45-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 12817528-6 2003 Concomitant treatment with CYP3A4 substrates altered mean AUC0-5 h and mean Cmax for repaglinide by 1% and 17% (ethinyloestradiol/levonorgestrel), 2% and 27% (simvastatin), or 11% and 3% (nifedipine). Ethinyl Estradiol 112-129 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 11849197-0 2002 The effects of an oral contraceptive containing ethinyloestradiol and norgestrel on CYP3A activity. Ethinyl Estradiol 48-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-89 11849197-1 2002 AIMS: To examine the effects of an oral contraceptive containing ethinyloestradiol and norgestrel on intestinal and hepatic CYP3A activity using midazolam as a probe substrate. Ethinyl Estradiol 65-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-129 11012556-0 2000 Effect of an oral contraceptive preparation containing ethinylestradiol and gestodene on CYP3A4 activity as measured by midazolam 1"-hydroxylation. Ethinyl Estradiol 55-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 7628296-9 1995 Therefore, compounds interacting with CYP3A proteins are expected to cause drug-drug interactions (i.e. the antimycotics ketoconazole and clotrimazole, the steroids ethinylestradiol and testosterone, the ergots, the calcium channel blocker nifedipine, and the immunosuppressants FK-506 and rapamycin). Ethinyl Estradiol 165-181 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 8765473-4 1996 The CYP3A inhibitors gestodene, triacetyloleandomycin, and 17 alpha-ethynylestradiol inhibited mifepristone demethylation and hydroxylation by 70-80%; antibodies to CYP3A4 inhibited these reactions by approximately 82 and 65%, respectively. Ethinyl Estradiol 59-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-9 8765473-4 1996 The CYP3A inhibitors gestodene, triacetyloleandomycin, and 17 alpha-ethynylestradiol inhibited mifepristone demethylation and hydroxylation by 70-80%; antibodies to CYP3A4 inhibited these reactions by approximately 82 and 65%, respectively. Ethinyl Estradiol 59-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 165-171 8613951-5 1996 Ritonavir was found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation, IC50) = 0.07 microM; 17alpha-ethynylestradiol 2-hydroxylation, IC50 = 2 microM; terfenadine hydroxylation, IC50 = 0.14 microM). Ethinyl Estradiol 126-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-53 32275771-1 2020 It is known that coadministration of CYP3A inducers may decrease the effectiveness of oral contraceptives containing progestins as mono-preparations or combined with ethinylestradiol. Ethinyl Estradiol 166-182 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-42 32275771-2 2020 In a randomized clinical drug-drug interaction study, we investigated the effects of CYP3A induction on the pharmacokinetics of commonly used progestins and ethinylestradiol. Ethinyl Estradiol 157-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-90