Absolute Bioavailability of Vemurafenib in Patients With BRAF


Journal

Clinical pharmacology in drug development
ISSN: 2160-7648
Titre abrégé: Clin Pharmacol Drug Dev
Pays: United States
ID NLM: 101572899

Informations de publication

Date de publication:
05 2020
Historique:
received: 14 06 2019
accepted: 16 12 2019
pubmed: 23 2 2020
medline: 6 5 2022
entrez: 22 2 2020
Statut: ppublish

Résumé

Vemurafenib is a BRAF kinase inhibitor indicated for the treatment of patients with BRAF

Identifiants

pubmed: 32083398
doi: 10.1002/cpdd.773
doi:

Substances chimiques

Protein Kinase Inhibitors 0
Vemurafenib 207SMY3FQT
BRAF protein, human EC 2.7.11.1
Proto-Oncogene Proteins B-raf EC 2.7.11.1

Types de publication

Clinical Trial, Phase I Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

496-504

Subventions

Organisme : F. Hoffmann-La Roche, Ltd.

Informations de copyright

© 2020, The American College of Clinical Pharmacology.

Références

Chapman PB, Hauschild A, Robert C, et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med. 2011;364(26):2507-2516.
McArthur GA, Chapman PB, Robert C, et al. Safety and efficacy of vemurafenib in BRAFV600E and BRAFV600K mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study. Lancet Oncol. 2014;15(3):323-332.
Diamond EL, Subbiah V, Lockhart AC, et al. Vemurafenib for BRAF V600-mutant Erdheim-Chester disease and Langerhans cell histiocytosis: analysis of data from the histology-independent, phase 2, open-label VE-BASKET study. JAMA Oncol. 2018;4(3):384-388.
Larkin J, Ascierto PA, Dreno B, et al. Combined vemurafenib and cobimetinib in BRAF-mutated melanoma. N Engl J Med. 2014;371(20):1867-1876.
Ascierto PA, McArthur GA, Dreno B, et al. Cobimetinib combined with vemurafenib in advanced BRAFV600-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial. Lancet Oncol. 2016;17(9):1248-1260.
Zhang W, McIntyre C, Forbes H, et al. Effect of rifampicin on the pharmacokinetics of a single dose of vemurafenib in patients with BRAFV600 mutation-positive metastatic malignancy. Clinical Pharmacol Drug Dev. 2019;8(6):837-843.
Zhang W, McIntyre C, Kuhn M, et al. Effect of vemurafenib on the pharmacokinetics of a single dose of digoxin in patients with BRAFV600 mutation-positive metastatic malignancy. J Clin Pharmacol. 2018;58(8):1067-1073.
Grippo JF, Zhang W, Heinzmann D, et al. A phase I, randomized, open-label study of the multiple-dose pharmacokinetics of vemurafenib in patients with BRAFV600E mutation-positive metastatic melanoma. Cancer Chemother Pharmacol. 2014;73(1):103-111.
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Zhang W, Heinzmann D, Grippo JF. Clinical pharmacokinetics of vemurafenib. Clin Pharmacokinet. 2017;56(9):1033-1043.
Goldinger SM, Rinderknecht J, Dummer R, et al. A single-dose mass balance and metabolite-profiling study of vemurafenib in patients with metastatic melanoma. Pharmacol Res Perspect. 2015;3(2):e00113.
Shah N, Iyer RM, Mair HJ, et al. Improved human bioavailability of vemurafenib, a practically insoluble drug, using an amorphous polymer-stabilized solid dispersion prepared by a solvent-controlled coprecipitation process. J Pharm Sci. 2013;102(3):967-981.
Flaherty KT, Puzanov I, Kim KB, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med. 2010;363(9):809-819.
Boulton DW, Kasichayanula S, Keung CFA, et al. Simultaneous oral therapeutic and intravenous 14C-microdoses to determine the absolute oral bioavailability of saxagliptin and dapagliflozin. Br J Clin Pharmacol. 2013;75(3):763-768.
Williams HD, Trevaskis NL, Charman SA, et al. Strategies to address low drug solubility in discovery and development. Pharmacol Rev. 2013;65(1):315-499.
Sarapa N, Hsyu PH, Lappin G, Garner RC. The application of accelerator mass spectrometry to absolute bioavailability studies in humans: simultaneous administration of an intravenous microdose of 14C-nelfinavir mesylate solution and oral nelfinavir to healthy volunteers. J Clin Pharmacol. 2005;45(10):1198-1205.
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Auteurs

Weijiang Zhang (W)

Roche Innovation Center New York, New York, New York, USA.

Dawn Colburn (D)

Genentech, Inc, South San Francisco, California, USA.

Brian Simmons (B)

Genentech, Inc, South San Francisco, California, USA.

Zsuzsanna Papai (Z)

PRA Magyarország Kft Fázis I-es Klinikai Farmakológiai Vizsgálóhely, Budapest, Hungary.

Enric Bertran (E)

Roche Innovation Center Basel, Basel, Switzerland.

Simone Schadt (S)

Roche Innovation Center Basel, Basel, Switzerland.

Christophe Husser (C)

Roche Innovation Center Basel, Basel, Switzerland.

Harper Forbes (H)

Hoffmann-La Roche Ltd, Mississauga, Ontario, Canada.

Dieter Roethlisberger (D)

Roche Innovation Center Basel, Basel, Switzerland.

Thomas Hartung (T)

Roche Innovation Center Basel, Basel, Switzerland.

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Classifications MeSH