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Pharmacology · Chemotherapy: imatinib
Sample itemA 45-year-old man with massive splenomegaly and a leucocyte count of 2.4 lakh per microlitre has the Philadelphia chromosome t(9;22). Imatinib is started. Which statement about the drug is correct?
Original practice item, not a recalled exam question. Nothing here is recorded.
The answer and the reasoning
A. It inhibits the BCR-ABL tyrosine kinase and is also effective in gastrointestinal stromal tumour through c-KIT inhibition
Imatinib inhibits the constitutively active BCR-ABL kinase produced by the Philadelphia chromosome, and also c-KIT and PDGFR, so it is used for gastrointestinal stromal tumours that carry c-KIT mutations. Adverse effects include fluid retention, nausea, myalgia and cytopenias. Resistance is commonly due to ABL kinase domain mutations.
Option by option
A. It inhibits the BCR-ABL tyrosine kinase and is also effective in gastrointestinal stromal tumour through c-KIT inhibition (correct)
Correct. Targeting the kinase addresses the driver in both diseases.
B. It inhibits EGFR and is also effective in lung adenocarcinoma
EGFR inhibition describes gefitinib, erlotinib and osimertinib.
C. It inhibits the proteasome and is also effective in myeloma
Proteasome inhibition describes bortezomib.
D. It binds CD20 and is also effective in follicular lymphoma
Binding CD20 is the action of rituximab, a monoclonal antibody.
Source note: Original NextPrep sample item — pending expert review. This item is original practice material awaiting independent expert review, so confirm important facts in a standard textbook.
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