Medical Pharmacology Practice Questions: Inhibitor of RAF Kinase Vemurafenib (Zelboraf)
Click on the correct answer.
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BRAF:
Is a human gene.
Codes for the B-raf protein
B-Raf belongs to the RAF kinase family of growth signal transduction protein kinases.
The B-raf protein in mutated form is found mutated in certain cancers.
A & B
B & C
A, B, C, D (all of the answers are correct)
Melanoma:
Exhibits constitutive activation either by changes in membrane receptors or by Ras or BRAF.
BRAF mutations activate kinase pathways Independent of Ras activation.
BRAF mutations occur in about half of melanomas.
A & B
B & C
A & C
A, B, C
Vemurafenib (Zelboraf) is a BRAF inhibitor more effective compared to typical chemotherapy in treating patients with mutant BRAF melanoma.
True
False
Vemurafenib is effective in treating which one/ons of the following BRAF mutant cancers
BRAF mutant lung cancer
BRAF mutant colon cancer
Both
Neither
Vemurafenib:
An orally bioavailable mutated BRAF (V600E I.e. valine to glutamic acid substitution) inhibitor
An orally bioavailable mutated BRAF (V600K I.e. valine to lysine substitution) inhibitor
Both
Neither
Vemurafenib pharmacokinetics/pharmacodynamics:
Volume of distribution is about 100 leaders
Significant protein binding (>99%)
Both
Neither
Vemurafenib pharmacokinetics:
Vemurafenib is metabolized by the liver microsomal cytochrome P450 drug metabolizing system given that is a substrate for CYP3A4.
Vemurafenib administration can increase the concentration of other drugs which are substrates for CYP1A2 such as Tizanidine.
Both
Neither
Main excretion pathway(s) for vemurafenib:
Feces
Urine
Both about equal
Vemurafenib is clinically-indicated not only for treating melanoma exhibiting BRAF mutations and for treating melanoma exhibiting wild-type (normally occurring) BRAF.
True
False
Most common adverse effects associated with vemurafenib administration are cutaneous in nature.
