PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 24492363-2 2014 Isavuconazole was effective, with MIC and minimal fungicidal concentration (MFC) values ranging between 0.125 and 1.00 mug/ml. isavuconazole 0-13 microphthalmia Japan Mus musculus 34-37 24100500-0 2013 Isavuconazole (BAL4815) pharmacodynamic target determination in an in vivo murine model of invasive pulmonary aspergillosis against wild-type and cyp51 mutant isolates of Aspergillus fumigatus. isavuconazole 0-13 cytochrome P450, family 51 Mus musculus 146-151 34543091-2 2021 isolates to 5 antifungal drugs (amphotericin B, voriconazole, posaconazole, isavuconazole, terbinafine) by EUCAST method. isavuconazole 76-89 calpastatin Homo sapiens 107-113 33008918-0 2020 Domain-Swap Dimerization of Acanthamoeba castellanii CYP51 and a Unique Mechanism of Inactivation by Isavuconazole. isavuconazole 101-114 cytochrome P450 family 51 subfamily A member 1 Homo sapiens 53-58 33963620-2 2021 Isavuconazole is metabolized by CYP3A4 and CYP3A5 and it has been shown that the CYP3A inducer rifampin reduces isavuconazole exposure. isavuconazole 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 33963620-2 2021 Isavuconazole is metabolized by CYP3A4 and CYP3A5 and it has been shown that the CYP3A inducer rifampin reduces isavuconazole exposure. isavuconazole 0-13 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 33963620-2 2021 Isavuconazole is metabolized by CYP3A4 and CYP3A5 and it has been shown that the CYP3A inducer rifampin reduces isavuconazole exposure. isavuconazole 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-37 33963620-5 2021 Moreover, although it is well known that CYP3A enzymes are important for the metabolism of isavuconazole, this induction-effect has never been studied in combination with the patient"s CYP3A genotype. isavuconazole 91-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-46 33963620-6 2021 PATIENTS: We report three patients treated with both isavuconazole and a CYP3A inducer that is less potent compared to rifampin (rifabutin or phenobarbital), in whom we determined isavuconazole concentrations. isavuconazole 180-193 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-78 33963620-7 2021 RESULTS: These cases suggest that the CYP3A4/5 genotype is an important determinant for isavuconazole exposure and that it might also influence the CYP450-induction interaction. isavuconazole 88-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 33963620-8 2021 CONCLUSIONS: CYP3A-inducers that are less potent compared to rifampin, may be combined with isavuconazole in patients with loss of CYP3A5 activity (CYP3A5*3/*3). isavuconazole 92-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 131-137 33963620-8 2021 CONCLUSIONS: CYP3A-inducers that are less potent compared to rifampin, may be combined with isavuconazole in patients with loss of CYP3A5 activity (CYP3A5*3/*3). isavuconazole 92-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 148-154 33963620-10 2021 However, low isavuconazole exposure was observed in the extensive metabolizer with CYP3A4*1/*1 and CYP3A5*1/*3 alleles. isavuconazole 13-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 33963620-10 2021 However, low isavuconazole exposure was observed in the extensive metabolizer with CYP3A4*1/*1 and CYP3A5*1/*3 alleles. isavuconazole 13-26 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 99-105 31119272-9 2019 In multivariate analysis the association between the length of treatment and higher levels of isavuconazole (P < 0.001) and higher serum GGT and lower isavuconazole levels (P = 0.001) was confirmed. isavuconazole 94-107 gamma-glutamyltransferase light chain 5 pseudogene Homo sapiens 140-143 31877348-0 2020 The antifungal isavuconazole inhibits the entry of lassa virus by targeting the stable signal peptide-GP2 subunit interface of lassa virus glycoprotein. isavuconazole 15-28 glycoprotein 2 Homo sapiens 102-105 31877348-4 2020 Fragment replacement mutational study indicated that isavuconazole targets the stable signal peptide (SSP)-membrane fusion subunit (GP2) interface of Lassa glycoprotein. isavuconazole 53-66 glycoprotein 2 Homo sapiens 132-135 31877348-5 2020 Further mutational study of the SSP-GP2 region of LASV glycoprotein revealed that S27 in the N-terminal transmembrane region of SSP and V431, F434 and V435 in the transmembrane domain of GP2 affect anti-LASV activity of isavuconazole. isavuconazole 220-233 glycoprotein 2 Homo sapiens 36-39 31877348-5 2020 Further mutational study of the SSP-GP2 region of LASV glycoprotein revealed that S27 in the N-terminal transmembrane region of SSP and V431, F434 and V435 in the transmembrane domain of GP2 affect anti-LASV activity of isavuconazole. isavuconazole 220-233 ribosomal protein S27 Homo sapiens 82-85 31877348-5 2020 Further mutational study of the SSP-GP2 region of LASV glycoprotein revealed that S27 in the N-terminal transmembrane region of SSP and V431, F434 and V435 in the transmembrane domain of GP2 affect anti-LASV activity of isavuconazole. isavuconazole 220-233 glycoprotein 2 Homo sapiens 187-190 31791946-3 2020 Here, we described a leading compound, NT-a9, an analogue of isavuconazole, that showed strong antifungal activities in vitro and in vivo NT-a9 showed a wide range of activities against several pathogenic fungi in vitro, including Cryptococcus neoformans, Cryptococcus gattii, Candida albicans, Candida krusei, Candida tropicalis, Candida glabrata, and Candida parapsilosis, with MICs ranging from 0.002 to 1 mug/ml. isavuconazole 61-74 nuclear encoded tRNA alanine 9 (anticodon AGC) Mus musculus 39-44 31791946-3 2020 Here, we described a leading compound, NT-a9, an analogue of isavuconazole, that showed strong antifungal activities in vitro and in vivo NT-a9 showed a wide range of activities against several pathogenic fungi in vitro, including Cryptococcus neoformans, Cryptococcus gattii, Candida albicans, Candida krusei, Candida tropicalis, Candida glabrata, and Candida parapsilosis, with MICs ranging from 0.002 to 1 mug/ml. isavuconazole 61-74 nuclear encoded tRNA alanine 9 (anticodon AGC) Mus musculus 138-143 31791946-9 2020 In the survival study, NT-a9 significantly prolonged the survival times of mice compared with the survival times of the control group or the isavuconazole-, fluconazole-, or amphotericin B-treated groups. isavuconazole 141-154 nuclear encoded tRNA alanine 9 (anticodon AGC) Mus musculus 23-28 31310805-0 2019 Isavuconazole and voriconazole inhibition of sterol 14alpha-demethylases (CYP51) from Aspergillus fumigatus and Homo sapiens. isavuconazole 0-13 sterol 14-demethylase Saccharomyces cerevisiae S288C 74-79 31310805-1 2019 Here we report the first evaluation of isavuconazole inhibition of Aspergillus fumigatus CYP51 and thus sterol biosynthesis in the fungus. isavuconazole 39-52 sterol 14-demethylase Saccharomyces cerevisiae S288C 89-94 31310805-2 2019 Voriconazole and isavuconazole both bound tightly to recombinant A. fumigatus CYP51 isoenzymes A and B (AfCYP51A and AfCYP51B) isolated in Escherichia coli membranes. isavuconazole 17-30 sterol 14-demethylase Saccharomyces cerevisiae S288C 78-83 31310805-8 2019 However, complementation studies in Saccharomyces cerevisiae using strains containing AfCYP51A and AfCYP51B showed isavuconazole to be equally as effective at inhibiting CYP51 activity as voriconazole. isavuconazole 115-128 sterol 14-demethylase Saccharomyces cerevisiae S288C 88-93 31310805-9 2019 These in vitro studies suggest that isavuconazole is an effective alternative to voriconazole as an antifungal agent against the target CYP51 in A. fumigatus. isavuconazole 36-49 sterol 14-demethylase Saccharomyces cerevisiae S288C 136-141 31024507-14 2019 Fusarium keratoplasticum showed high MIC values (8->32 mug mL-1) for itraconazole, voriconazole, posaconazole, and isavuconazole. isavuconazole 118-131 2'-5' oligoadenylate synthetase 1B Mus musculus 62-66 29558838-0 2019 Isavuconazole therapy in an FLT3 mutated acute myeloid leukemia patient receiving midostaurin: A case report. isavuconazole 0-13 fms related receptor tyrosine kinase 3 Homo sapiens 28-32 29558838-6 2019 Isavuconazole, a moderate CYP3A4 inhibitor, was successfully initiated and maintained, while midostaurin therapy was also administered. isavuconazole 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 29022838-6 2017 Expert opinion: Currently studies demonstrating the pharmacogenomic influences on itraconazole, posaconazole and isavuconazole are minimal and limited to their inhibitory effects on CYP3A4 in expressors of CYP3A5 variants. isavuconazole 113-126 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 206-212 30295407-1 2019 INTRODUCTION: Isavuconazole, a triazole antifungal, is an inhibitor of cytochrome P450 3A4, which also metabolizes tacrolimus and sirolimus. isavuconazole 14-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-90 30477963-5 2018 In addition, isavuconazole may inhibit CYP3A4. isavuconazole 13-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 28355467-4 2017 Isavuconazole, the newest triazole agent, offers the advantages of once-daily dosing, a wider spectrum of antifungal activity than voriconazole, predictable pharmacokinetics and fewer CYP enzyme-mediated drug interactions. isavuconazole 0-13 peptidylprolyl isomerase G Homo sapiens 184-187 26482310-7 2016 Relative increases of azole MICs (from 4- to 32-fold) were observed for fluconazole, voriconazole, and isavuconazole when at least two mutations were present in the same ERG11 allele. isavuconazole 103-116 sterol 14-demethylase Saccharomyces cerevisiae S288C 170-175 27273149-0 2017 Pharmacokinetic Effects of Isavuconazole Coadministration With the Cytochrome P450 Enzyme Substrates Bupropion, Repaglinide, Caffeine, Dextromethorphan, and Methadone in Healthy Subjects. isavuconazole 27-40 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 67-82 27273149-4 2017 Thus, isavuconazole is a mild inducer of CYP2B6 but does not appear to affect CYP1A2-, CYP2C8-, or CYP2D6-mediated metabolism. isavuconazole 6-19 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 41-47 27273461-0 2017 Pharmacokinetic Evaluation of CYP3A4-Mediated Drug-Drug Interactions of Isavuconazole With Rifampin, Ketoconazole, Midazolam, and Ethinyl Estradiol/Norethindrone in Healthy Adults. isavuconazole 72-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 27273461-1 2017 This report describes the phase 1 trials that evaluated the metabolism of the novel triazole antifungal isavuconazole by cytochrome P450 3A4 (CYP3A4) and isavuconazole"s effects on CYP3A4-mediated metabolism in healthy adults. isavuconazole 104-117 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-140 27273461-1 2017 This report describes the phase 1 trials that evaluated the metabolism of the novel triazole antifungal isavuconazole by cytochrome P450 3A4 (CYP3A4) and isavuconazole"s effects on CYP3A4-mediated metabolism in healthy adults. isavuconazole 104-117 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 142-148 27273461-1 2017 This report describes the phase 1 trials that evaluated the metabolism of the novel triazole antifungal isavuconazole by cytochrome P450 3A4 (CYP3A4) and isavuconazole"s effects on CYP3A4-mediated metabolism in healthy adults. isavuconazole 104-117 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 181-187 27273461-1 2017 This report describes the phase 1 trials that evaluated the metabolism of the novel triazole antifungal isavuconazole by cytochrome P450 3A4 (CYP3A4) and isavuconazole"s effects on CYP3A4-mediated metabolism in healthy adults. isavuconazole 154-167 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 181-187 27273461-2 2017 Coadministration of oral isavuconazole (100 mg once daily) with oral rifampin (600 mg once daily; CYP3A4 inducer) decreased isavuconazole area under the concentration-time curve (AUCtau ) during a dosing interval by 90% and maximum concentration (Cmax ) by 75%. isavuconazole 25-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 27273461-2 2017 Coadministration of oral isavuconazole (100 mg once daily) with oral rifampin (600 mg once daily; CYP3A4 inducer) decreased isavuconazole area under the concentration-time curve (AUCtau ) during a dosing interval by 90% and maximum concentration (Cmax ) by 75%. isavuconazole 124-137 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 27273461-3 2017 Conversely, coadministration of isavuconazole (200 mg single dose) with oral ketoconazole (200 mg twice daily; CYP3A4 inhibitor) increased isavuconazole AUC from time 0 to infinity (AUC0- ) and Cmax by 422% and 9%, respectively. isavuconazole 32-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 111-117 27273461-3 2017 Conversely, coadministration of isavuconazole (200 mg single dose) with oral ketoconazole (200 mg twice daily; CYP3A4 inhibitor) increased isavuconazole AUC from time 0 to infinity (AUC0- ) and Cmax by 422% and 9%, respectively. isavuconazole 139-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 111-117 27273461-4 2017 Isavuconazole was coadministered (200 mg 3 times daily for 2 days, then 200 mg once daily) with single doses of oral midazolam (3 mg; CYP3A4 substrate) or ethinyl estradiol/norethindrone (35 mug/1 mg; CYP3A4 substrate). isavuconazole 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-140 27273461-4 2017 Isavuconazole was coadministered (200 mg 3 times daily for 2 days, then 200 mg once daily) with single doses of oral midazolam (3 mg; CYP3A4 substrate) or ethinyl estradiol/norethindrone (35 mug/1 mg; CYP3A4 substrate). isavuconazole 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 201-207 27273461-7 2017 These results indicate that isavuconazole is a sensitive substrate and moderate inhibitor of CYP3A4. isavuconazole 28-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 27821435-5 2017 When NMEs were considered as victim drugs, 21 NMEs had at least one positive clinical DDI, with three NMEs shown to be sensitive substrates of CYP3A (AUC ratio >= 5 when coadministered with strong inhibitors): cobimetinib, isavuconazole (the active metabolite of prodrug isavuconazonium sulfate), and ivabradine. isavuconazole 226-239 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 143-148 27821435-5 2017 When NMEs were considered as victim drugs, 21 NMEs had at least one positive clinical DDI, with three NMEs shown to be sensitive substrates of CYP3A (AUC ratio >= 5 when coadministered with strong inhibitors): cobimetinib, isavuconazole (the active metabolite of prodrug isavuconazonium sulfate), and ivabradine. isavuconazole 274-297 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 143-148 27273004-6 2017 These findings indicate that isavuconazole is a weak inhibitor of P-gp, as well as OCT1, OCT2, MATE1, or a combination thereof but not of BCRP, OATP1B1, OAT1, or OAT3. isavuconazole 29-42 ATP binding cassette subfamily B member 1 Homo sapiens 66-70 27273004-6 2017 These findings indicate that isavuconazole is a weak inhibitor of P-gp, as well as OCT1, OCT2, MATE1, or a combination thereof but not of BCRP, OATP1B1, OAT1, or OAT3. isavuconazole 29-42 solute carrier family 22 member 1 Homo sapiens 83-87 27273004-6 2017 These findings indicate that isavuconazole is a weak inhibitor of P-gp, as well as OCT1, OCT2, MATE1, or a combination thereof but not of BCRP, OATP1B1, OAT1, or OAT3. isavuconazole 29-42 solute carrier family 22 member 2 Homo sapiens 89-93 27273004-6 2017 These findings indicate that isavuconazole is a weak inhibitor of P-gp, as well as OCT1, OCT2, MATE1, or a combination thereof but not of BCRP, OATP1B1, OAT1, or OAT3. isavuconazole 29-42 solute carrier family 47 member 1 Homo sapiens 95-100 27001813-4 2016 Fifty percent inhibitory concentrations (IC50s) for P-gp and BCRP were both 2 muM for itraconazole, 5 and 12 muM for hydroxyitraconazole, 3 and 6 muM for posaconazole, and 3 and 11 muM for isavuconazole, respectively. isavuconazole 189-202 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 27001813-4 2016 Fifty percent inhibitory concentrations (IC50s) for P-gp and BCRP were both 2 muM for itraconazole, 5 and 12 muM for hydroxyitraconazole, 3 and 6 muM for posaconazole, and 3 and 11 muM for isavuconazole, respectively. isavuconazole 189-202 BCR pseudogene 1 Homo sapiens 61-65 26482310-10 2016 Resistance mechanisms in yeasts involving ABC transporters and ERG11 decreased the activity of isavuconazole, while MDR1 had limited effect. isavuconazole 95-108 sterol 14-demethylase Saccharomyces cerevisiae S288C 63-68