OnCo
termsTerm

Tyrosine kinase inhibitor (TKI)

aka TKI, TKIs, tyrosine kinase inhibitors, kinase inhibitor, multikinase inhibitor, multi-kinase inhibitor, multi-targeted TKI, EGFR-TKI, ALK TKI, BTK inhibitor, BTK inhibitors, BTK inhibition, targeted pill, -nib, TKI-pretreated, TKI-naive, first-generation, second-generation, third-generation, next-generation TKI

Pills that block the on-switch enzyme (a kinase) that a particular cancer depends on: imatinib for CML, osimertinib for EGFR lung cancer, ibrutinib for CLL. Usually taken daily at home and continued as long as they work.

Small molecules that occupy the ATP pocket (or an allosteric site) of a kinase; selectivity ranges from single-target (osimertinib, asciminib) to multikinase (sorafenib, lenvatinib, cabozantinib, which also hit VEGF receptors). Generations improve potency, brain penetration and coverage of resistance mutations. They produce rapid responses in oncogene-addicted cancers, and resistance emerges through on-target mutations or bypass pathways. Class toxicities depend on off-target kinases: rash and diarrhoea (EGFR), hypertension and hand-foot reaction (VEGFR), QT prolongation, and pneumonitis. Not every kinase inhibitor is 'tyrosine' (CDK4/6 and MEK are serine/threonine kinases) but the shorthand is used broadly.

Category
Treatment jargon

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Targeted Therapy

technologies

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Small-molecule kinase inhibitors

drugs

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ApprovedSmall-molecule multi-kinase inhibitor (MET, VEGFR2, AXL, RET)
Cabozantinib · Cabometyx
ApprovedSmall-molecule covalent BTK inhibitor (first generation)
Ibrutinib · Imbruvica
ApprovedSmall-molecule kinase inhibitor (BCR-ABL, KIT, PDGFRA)
Imatinib · Gleevec
ApprovedSmall-molecule multi-kinase inhibitor (VEGFR, FGFR, PDGFR, RET, KIT)
Lenvatinib · Lenvima
ApprovedSmall-molecule kinase inhibitor (EGFR)
Osimertinib · Tagrisso
ApprovedSmall-molecule covalent BTK inhibitor (second generation)
Zanubrutinib · Brukinsa

terms

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Anti-VEGF class toxicities (hypertension, proteinuria, bleeding, perforation)BRAF V600E mutationCNS penetration (brain-penetrant drugs)Driver mutation (actionable / targetable alteration)EGFR mutation subtypes (exon 19 deletion, L858R, exon 20 insertion, T790M)Hand-foot syndrome and hand-foot skin reactionMolecular response (MMR, MR4, treatment-free remission)On-target resistance mutations (gatekeeper, solvent-front, compound)Oncogene addictionPhiladelphia chromosome (Ph+, BCR::ABL1)QT prolongationRash and skin toxicity (acneiform rash, paronychia)