Imatinib: First NIB approved by FDA. The suffix "nib" indicates a small-molecule ❌ ("nib" is verbal shorthand for "inhibit") of kinase enzymes.
- A small molecule ❌ inhibitor of tyrosine kinase
- Treats chronic myeloid leukaemia; as it is selective for ❌ TK fusion protein and competes with ❌ for binding siten inhibiting phosphorylation (and ❌).
Other NIBs in clinical use: gefitinib, erlotinib, sorafenib, sunitinib, and dasatinib.
- Share ❌ mechanism of action (competitive ATP inhibition at catalytic binding site of TK) BUT difference is the ❌ of targeted kinases
e.g. ❌ inhibits signals from several Rs including VEGF and PDGRF families.
NIBs are well tolerated but frequently cause ❌, arthralgia, & myalgia. Rarely
cumulative cardiotoxicity: ❌ needed.
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intracellular
intracellular
proliferation
proliferation
myelosupression, rash, GI upset, fatigue
myelosupression, rash, GI upset, fatigue