Effect of itraconazole, food, and ethnic origin on the pharmacokinetics of ivosidenib in healthy subjects.

Purpose: To assess the effect of ethnicity, food, and itraconazole (strong CYP3A4 inhibitor) on the pharmacokinetics of ivosidenib after single oral doses in healthy subjects. Methods: Three phase 1 open-label studies were performed. Study 1: Japanese and Caucasian subjects received single doses of...

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Publicado en:European Journal of Clinical Pharmacology Vol. 75; no. 8; pp. 1099 - 1109
Autores principales: Dai, David, Yang, Hua, Nabhan, Salah, Liu, Hua, Hickman, Denice, Liu, Guowen, Zacher, Jeffrey, Vutikullird, Apinya, Prakash, Chandra, Agresta, Samuel, Bowden, Chris, Fan, Bin
Formato: research tables/charts randomized controlled trial Journal Article
Publicado: Springer Nature Aug2019
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Aug2019
      vid: 75
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      pub: Springer Nature
      place: New York, New York
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        137507147
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        10.1007/s00228-019-02673-6
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        atl: Effect of itraconazole, food, and ethnic origin on the pharmacokinetics of ivosidenib in healthy subjects.
      aug:
        au:
          Dai, David
          Yang, Hua
          Nabhan, Salah
          Liu, Hua
          Hickman, Denice
          Liu, Guowen
          Zacher, Jeffrey
          Vutikullird, Apinya
          Prakash, Chandra
          Agresta, Samuel
          Bowden, Chris
          Fan, Bin
        affil: Agios Pharmaceuticals, Inc., 88 Sidney Street, 02139, Cambridge, MA, USA
      sug:
        subj:
          Itraconazole Pharmacodynamics
          Meals Japan
          Ethnic Groups Japan
          Enzyme Inhibitors Pharmacokinetics
          Enzyme Inhibitors Administration and Dosage
          Itraconazole Administration and Dosage
          Drug Interactions
          Human
          Randomized Controlled Trials
          Crossover Design
          Fasting
          Fats
          Administration, Oral
          Japan
          White Persons
          Confidence Intervals
      ab: Purpose: To assess the effect of ethnicity, food, and itraconazole (strong CYP3A4 inhibitor) on the pharmacokinetics of ivosidenib after single oral doses in healthy subjects. Methods: Three phase 1 open-label studies were performed. Study 1: Japanese and Caucasian subjects received single doses of 250, 500, or 1000 mg ivosidenib (NCT03071770). Part 1 of study 2 (a two-period crossover study): subjects received 500 mg ivosidenib after either an overnight fast or a high-fat meal. Subjects received 1000 mg ivosidenib after an overnight fast in the single period of part 2 (NCT02579707). Study 3: in period 1, subjects received 250 mg ivosidenib; then, in period 2, subjects received oral itraconazole (200 mg once daily) on days 1–18, plus 250 mg ivosidenib on day 5 (NCT02831972). Results: Ivosidenib was well tolerated in all three studies. Study 1: pharmacokinetic profiles were generally comparable, although AUC and Cmax were slightly lower in Japanese subjects than in Caucasian subjects, by ~ 30 and 17%, respectively. Study 2: AUC increased by ~ 25% and Cmax by ~ 98%, when ivosidenib was administered with a high-fat meal compared with a fasted state. Study 3: co-administration of itraconazole increased ivosidenib AUC by 169% (90% CI 145–195) but had no effect on ivosidenib Cmax. Conclusions: No ivosidenib dose adjustment is deemed necessary for Japanese subjects. High-fat meals should be avoided when ivosidenib is taken with food. When co-administered with strong CYP3A4 inhibitors, monitoring for QT interval prolongation (a previously defined adverse event of interest) is recommended and an ivosidenib dose interruption or reduction may be considered. ClinicalTrials.gov NCT03071770, NCT02579707, and NCT02831972.
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        randomized controlled trial
        Journal Article
      ougenre: Article
    language: English
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