PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 32237115-7 2020 Coadministration of laquinimod with CYP3A inhibitors, ketoconazole, fluconazole, and cimetidine increased laquinimod area under the plasma concentration-time curve from time zero to infinity by approximately 3.1-, 2.5-, and 1.1-fold, respectively. laquinimod 20-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-41 21163185-5 2011 Laquinimod is metabolised primarily by the CYP3A4 enzyme in the liver. laquinimod 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 15764719-0 2005 Cytochrome P450 3A4 is the major enzyme responsible for the metabolism of laquinimod, a novel immunomodulator. laquinimod 74-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 15764719-5 2005 Moreover, ketoconazole and troleandomycin, specific inhibitors of CYP3A4 metabolism, demonstrated a significant inhibition of laquinimod metabolism. laquinimod 126-136 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. laquinimod 106-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 15764719-9 2005 In conclusion, the present study demonstrates that laquinimod is a low affinity substrate for CYP3A4 in human liver microsomes. laquinimod 51-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-100 15764719-10 2005 The likelihood for in vivo effects of laquinimod on the metabolism of other CYP3A4 substrates is minor. laquinimod 38-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 15764719-11 2005 However, inhibitory effects on the metabolism of laquinimod by potent and specific inhibitors of CYP3A4, such as ketoconazole, are anticipated and should be considered in the continued clinical program for laquinimod. laquinimod 49-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 15764719-11 2005 However, inhibitory effects on the metabolism of laquinimod by potent and specific inhibitors of CYP3A4, such as ketoconazole, are anticipated and should be considered in the continued clinical program for laquinimod. laquinimod 206-216 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 32237115-7 2020 Coadministration of laquinimod with CYP3A inhibitors, ketoconazole, fluconazole, and cimetidine increased laquinimod area under the plasma concentration-time curve from time zero to infinity by approximately 3.1-, 2.5-, and 1.1-fold, respectively. laquinimod 106-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-41 32237115-9 2020 These results indicate that coadministration of laquinimod with moderate to strong inhibitors of CYP3A or strong inducers of CYP3A may give rise to significant pharmacokinetic drug interactions. laquinimod 48-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-102 32237115-9 2020 These results indicate that coadministration of laquinimod with moderate to strong inhibitors of CYP3A or strong inducers of CYP3A may give rise to significant pharmacokinetic drug interactions. laquinimod 48-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-130 32237115-0 2020 The Effect of CYP3A Induction and Inhibition on the Pharmacokinetics of Laquinimod, a Novel Neuroimmunomodulator. laquinimod 72-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-19 32237115-1 2020 Laquinimod, a neuroimmunomodulator, is extensively metabolized by cytochrome P450 (CYP) 3A4, and modulations of CYP3A4 activity may lead to alterations in the pharmacokinetics and/or clinical effects of laquinimod. laquinimod 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-91 32237115-1 2020 Laquinimod, a neuroimmunomodulator, is extensively metabolized by cytochrome P450 (CYP) 3A4, and modulations of CYP3A4 activity may lead to alterations in the pharmacokinetics and/or clinical effects of laquinimod. laquinimod 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-118 32237115-1 2020 Laquinimod, a neuroimmunomodulator, is extensively metabolized by cytochrome P450 (CYP) 3A4, and modulations of CYP3A4 activity may lead to alterations in the pharmacokinetics and/or clinical effects of laquinimod. laquinimod 203-213 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-118 32237115-2 2020 To determine the drug-drug interaction potential of laquinimod with CYP3A inhibitors and inducers, interaction assessments were conducted in healthy volunteers using single-dose administration of laquinimod before and after multiple dosing of CYP3A inhibitors (ketoconazole, fluconazole, and cimetidine) or a CYP3A4 inducer (rifampin). laquinimod 52-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-73