A single-dose mass balance and metabolite-profiling study of vemurafenib in patients with metastatic melanoma
| Autor: | David J Moore, Felix P. Kuhn, Ruben C Ayala, Simone M. Goldinger, Selby Patricia Gil Bazan, Lucy Lee, Andrew K. Joe, Jeannine D. Rinderknecht, Jagdish Kumar Racha, Kuo-Hsiung Yang, Reinhard Dummer, Joseph F. Grippo, Mei Liu, Wanping Geng |
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| Přispěvatelé: | University of Zurich, Grippo, Joseph F |
| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
BRAF inhibitor
Metabolite 610 Medicine & health Urine Pharmacology 3000 General Pharmacology Toxicology and Pharmaceutics Excretion chemistry.chemical_compound elimination Pharmacokinetics medicine General Pharmacology Toxicology and Pharmaceutics Vemurafenib Feces business.industry 10042 Clinic for Diagnostic and Interventional Radiology Melanoma 10177 Dermatology Clinic Original Articles medicine.disease Renal Elimination Neurology chemistry disposition 2808 Neurology business metabolism mass balance metastatic melanoma medicine.drug |
| Zdroj: | Pharmacology Research & Perspectives |
| Popis: | Vemurafenib, a selective inhibitor of oncogenic BRAF kinase carrying the V600 mutation, is approved for treatment of advanced BRAF mutation-positive melanoma. This study characterized mass balance, metabolism, rates/routes of elimination, and disposition of (14)C-labeled vemurafenib in patients with metastatic melanoma. Seven patients with metastatic BRAF-mutated melanoma received unlabeled vemurafenib 960 mg twice daily for 14 days. On the morning of day 15, patients received (14)C-labeled vemurafenib 960 mg (maximum 2.56 MBq [69.2 μCi]). Thereafter, patients resumed unlabeled vemurafenib (960 mg twice daily). Blood, urine, and feces were collected for metabolism, pharmacokinetic, and dose recovery analysis. Within 18 days after dose, ∽95% of (14)C-vemurafenib-related material was recovered from feces (94.1%) and urine ( |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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