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Characterization of the Effect of Upadacitinib on the Pharmacokinetics of Bupropion, a Sensitive Cytochrome P450 2B6 Probe Substrate.
| Content Provider | Europe PMC |
|---|---|
| Author | Mohamed, Mohamed‐Eslam F. Minocha, Mukul Trueman, Sheryl Feng, Tian Enejosa, Jeffrey Fisniku, Ogert Othman, Ahmed A. |
| Abstract | AbstractThis phase 1 study characterized the effect of multiple doses of upadacitinib, an oral Janus kinase 1 selective inhibitor, on the pharmacokinetics of the cytochrome P450 (CYP) 2B6 substrate bupropion. Healthy subjects (n = 22) received a single oral dose of bupropion 150 mg alone (study period 1) and on day 12 of a 16‐day regimen of upadacitinib 30 mg once daily (study period 2). Serial blood samples for measurement of bupropion and hydroxybupropion plasma concentrations were collected in each study period. The central values (90% confidence intervals) for the ratios of change were 0.87 (0.79‐0.96) for bupropion maximum plasma concentration (Cmax), 0.92 (0.87‐0.98) for bupropion area under the plasma‐concentration time curve from time 0 to infinity (AUCinf), 0.78 (0.72‐0.85) for hydroxybupropion Cmax, and 0.72 (0.67‐0.78) for hydroxybupropion AUCinf when administered with, relative to when administered without, upadacitinib. After multiple‐dose administration of upadacitinib 30 mg once daily, upadacitinib mean ± SD AUC0‐24 was 641 ± 177 ng·h/mL, and Cmax was 83.3 ± 30.7 ng/mL. These results confirm that upadacitinib has no relevant effect on pharmacokinetics of substrates metabolized by CYP2B6. |
| Related Links | https://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC7984436&blobtype=pdf |
| Page Count | 8 |
| ISSN | 2160763X |
| Journal | Clinical Pharmacology in Drug Development [Clin Pharmacol Drug Dev] |
| Volume Number | 10 |
| DOI | 10.1002/cpdd.844 |
| PubMed Central reference number | PMC7984436 |
| Issue Number | 3 |
| PubMed reference number | 32648334 |
| e-ISSN | 21607648 |
| Language | English |
| Publisher | John Wiley and Sons Inc. |
| Publisher Date | 2020-07-09 |
| Publisher Place | Hoboken |
| Access Restriction | Open |
| Rights License | This is an open access article under the terms of the http://creativecommons.org/licenses/by-nc-nd/4.0/ License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non‐commercial and no modifications or adaptations are made. © 2020 AbbVie Inc. Clinical Pharmacology in Drug Development published by Wiley Periodicals LLC on behalf of American College of Clinical Pharmacology |
| Subject Keyword | upadacitinib CYP2B6 bupropion Janus kinase inhibitor pharmacokinetics drug interaction |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology (medical) Pharmaceutical Science |
