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Pharmacology · Chemotherapy: CDK4/6 inhibitors
Sample itemA postmenopausal woman with hormone receptor positive, HER2 negative metastatic breast cancer is given palbociclib with letrozole. What is the target of palbociclib?
Original practice item, not a recalled exam question. Nothing here is recorded.
The answer and the reasoning
B. CDK4 and CDK6, blocking progression from G1 to S
Palbociclib inhibits cyclin-dependent kinases 4 and 6, preventing phosphorylation of Rb and holding the cell in G1. Combined with endocrine therapy it prolongs progression-free survival, and the main toxicity is neutropenia.
Option by option
A. HER2 tyrosine kinase
HER2 tyrosine kinase is targeted by lapatinib, and the tumour here is HER2 negative.
B. CDK4 and CDK6, blocking progression from G1 to S (correct)
Correct. Palbociclib inhibits CDK4 and CDK6, causing G1 arrest.
C. The aromatase enzyme
Aromatase is inhibited by letrozole, the partner drug, not by palbociclib.
D. mTOR kinase
mTOR kinase is inhibited by everolimus, a different add-on agent.
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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