Vemurafenib is the only active oral inhibitor of mutated BRAF serine-threonine kinase. It is active against the BRAF V600E mutated form.
It is used in the treatment of metastatic melanoma.
Key Insights from Swiss ADME:
GI absorption: low
Blood Brain Barrier Permeation: absent
Lipinski Rule of 5: indicating good oral bioavailability
Metabolism: metabolised by CYP3A4 enzyme
Volume of distribution: 106L
Plasma protein binding: albumin and alpha-1 acid glycoprotein
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