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• W2038595087 abstract "Abstract 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 μ Ci]). 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 (<1%). The parent compound was the predominant component (95%) in plasma. The mean plasma elimination half‐life of 14 C‐vemurafenib–related material was 71.1 h. Each metabolite accounted for <0.5% and ≤6% of the total administered dose in urine and feces, respectively (0–96 h postdose). No new metabolites were detected. Vemurafenib was well‐tolerated. Excretion of vemurafenib via bile into feces is considered the predominant elimination route from plasma with minor renal elimination (<1%)." @default.
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• W2038595087 date "2015-02-02" @default.
• W2038595087 modified "2023-10-03" @default.
• W2038595087 title "A single‐dose mass balance and metabolite‐profiling study of vemurafenib in patients with metastatic melanoma" @default.
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• W2038595087 doi "https://doi.org/10.1002/prp2.113" @default.
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