Academic Journal
Itraconazole Increases Ibrutinib Exposure 10‐Fold and Reduces Interindividual Variation—A Potentially Beneficial Drug‐Drug Interaction
| Title: | Itraconazole Increases Ibrutinib Exposure 10‐Fold and Reduces Interindividual Variation—A Potentially Beneficial Drug‐Drug Interaction |
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| Authors: | Tuija Tapaninen, Aleksi M. Olkkola, Aleksi Tornio, Mikko Neuvonen, Erkki Elonen, Pertti J. Neuvonen, Mikko Niemi, Janne T. Backman |
| Source: | Clinical and Translational Science, Vol 13, Iss 2, Pp 345-351 (2020) |
| Publisher Information: | Wiley, 2020. |
| Publication Year: | 2020 |
| Collection: | LCC:Therapeutics. Pharmacology LCC:Public aspects of medicine |
| Subject Terms: | Therapeutics. Pharmacology, RM1-950, Public aspects of medicine, RA1-1270 |
| More Details: | The oral bioavailability of ibrutinib is low and variable, mainly due to extensive first‐pass metabolism by cytochrome P450 (CYP) 3A4. The unpredictable exposure can compromise its safe and effective dosing. We examined the impact of itraconazole on ibrutinib pharmacokinetics. In a randomized crossover study, 11 healthy subjects were administered itraconazole 200 mg or placebo twice on day 1, and once on days 2–4. On day 3, 1 hour after itraconazole (placebo) and breakfast, ibrutinib (140 mg during placebo; 15 mg during itraconazole) was administered. Itraconazole increased the dose‐adjusted geometric mean area under the concentration‐time curve from zero to infinity (AUC0–∞) of ibrutinib 10.0‐fold (90% confidence interval (CI) 7.2–13.9; P |
| Document Type: | article |
| File Description: | electronic resource |
| Language: | English |
| ISSN: | 1752-8062 1752-8054 |
| Relation: | https://doaj.org/toc/1752-8054; https://doaj.org/toc/1752-8062 |
| DOI: | 10.1111/cts.12716 |
| Access URL: | https://doaj.org/article/701e1cf86da34400937cd534eb0f5ba8 |
| Accession Number: | edsdoj.701e1cf86da34400937cd534eb0f5ba8 |
| Database: | Directory of Open Access Journals |
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| ISSN: | 17528062 17528054 |
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| DOI: | 10.1111/cts.12716 |
| Published in: | Clinical and Translational Science |
| Language: | English |