Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine (a CYP1A2 Substrate) in Patients With BRAF V600 Mutation-Positive Malignancies.
Autor: | Zhang W; F. Hoffmann-La Roche Ltd., New York, New York, USA., McIntyre C; pRED Roche Innovation Centre Welwyn, Roche Products Ltd., Welwyn Garden City, UK., Riehl T; Genentech, Inc., South San Francisco, California, USA., Forbes H; F. Hoffmann-La Roche Ltd., Mississauga, Ontario, Canada., Bertran E; pRED Roche Innovation Centre Basel, Roche Products Ltd., Basel, Switzerland., Choi HJ; Severance Hospital, Yonsei University Health System, Seoul, Republic of Korea., Lee DH; Asan Medical Center, Seoul, Republic of Korea., Lee J; Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, Republic of Korea. |
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Jazyk: | angličtina |
Zdroj: | Clinical pharmacology in drug development [Clin Pharmacol Drug Dev] 2020 Jul; Vol. 9 (5), pp. 651-658. Date of Electronic Publication: 2020 Apr 20. |
DOI: | 10.1002/cpdd.788 |
Abstrakt: | This phase 1 open-label, multicenter, 3-period, fixed-sequence study evaluated the effect of multiple doses of vemurafenib on the pharmacokinetics of 1 dose of tizanidine, a probe CYP1A2 substrate, in patients with BRAF V600 mutation-positive metastatic malignancy. Patients received 1 dose of tizanidine 2 mg on day 1 (period A), vemurafenib 960 mg twice daily on days 2-21 (period B), and 1 dose of tizanidine 2 mg and vemurafenib 960 mg twice daily on day 22 (period C). Log-transformed area under the concentration-time curve (AUC) and maximum plasma concentration (C (© 2020, The American College of Clinical Pharmacology.) |
Databáze: | MEDLINE |
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