# Tyrosine kinase inhibitor (TKI)

Source: https://onco.cc/terms/tki-term/  
OnCo record `tki-term` (Term). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

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.

## Summary

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.

## Fields

- Kind: Term
- Last checked: 2026-09-09
- Also known as: 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; kinase inhibitors; multikinase inhibitors; next-generation TKIs; targeted pills

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Tyrosine_kinase_inhibitor
- Wikipedia: https://en.wikipedia.org/wiki/Tyrosine_kinase_inhibitor

## Connected records

- terms: [Anti-VEGF class toxicities (hypertension, proteinuria, bleeding, perforation)](https://onco.cc/terms/antiangiogenic-toxicities/), [BRAF V600E mutation](https://onco.cc/terms/braf-v600-mutation/), [CNS penetration (brain-penetrant drugs)](https://onco.cc/terms/cns-penetration/), [Driver mutation](https://onco.cc/terms/driver-mutation/), [EGFR mutation subtypes (exon 19 deletion, L858R, exon 20 insertion, T790M)](https://onco.cc/terms/egfr-mutation-subtypes/), [Hand-foot syndrome and hand-foot skin reaction](https://onco.cc/terms/hand-foot-syndrome/), [Molecular response (MMR, MR4, treatment-free remission)](https://onco.cc/terms/molecular-response/), [On-target resistance mutations (gatekeeper, solvent-front, compound)](https://onco.cc/terms/gatekeeper-mutation/), [Oncogene addiction](https://onco.cc/terms/oncogene-addiction/), [Philadelphia chromosome (Ph+, BCR::ABL1)](https://onco.cc/terms/philadelphia-chromosome/), [QT prolongation](https://onco.cc/terms/qt-prolongation/), [Rash and skin toxicity (acneiform rash, paronychia)](https://onco.cc/terms/rash-skin-toxicity/)
- fronts: [Targeted Therapy](https://onco.cc/fronts/targeted-therapy/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- drugs: [Cabozantinib](https://onco.cc/drugs/cabozantinib/), [Ibrutinib](https://onco.cc/drugs/ibrutinib/), [Imatinib](https://onco.cc/drugs/imatinib/), [Lenvatinib](https://onco.cc/drugs/lenvatinib/), [Osimertinib](https://onco.cc/drugs/osimertinib/), [Zanubrutinib](https://onco.cc/drugs/zanubrutinib/)
- trials: [ALESIA](https://onco.cc/trials/alesia/), [ALEX](https://onco.cc/trials/alex/), [ARCHER 1050](https://onco.cc/trials/nct01774721/), [ASCEND-4](https://onco.cc/trials/nct01828099/), [AURA3](https://onco.cc/trials/aura3/), [eXalt3](https://onco.cc/trials/nct02767804/), [FLAURA](https://onco.cc/trials/flaura/), [J-ALEX](https://onco.cc/trials/j-alex/), [LUX-Lung 3](https://onco.cc/trials/lux-lung-3/), [PROFILE 1001 ROS1 expansion cohort](https://onco.cc/trials/profile-1001-ros1/), [PROFILE 1014](https://onco.cc/trials/profile-1014/)
- key papers: [Lemmon and Schlessinger 2010: cell signalling by receptor tyrosine kinases](https://onco.cc/key-papers/paper-lemmon-schlessinger-rtk-signalling-cell-2010/)
- institutions: [Chongqing University Cancer Hospital](https://onco.cc/institutions/chongqing-university-cancer-hospital/)
- biomarkers: [ALK fusion (ALK-positive)](https://onco.cc/biomarkers/alk-fusion/), [NTRK1/2/3 gene fusion](https://onco.cc/biomarkers/ntrk-fusion/), [RET fusion and RET mutation](https://onco.cc/biomarkers/ret-fusion/), [ROS1 fusion (ROS1-positive)](https://onco.cc/biomarkers/ros1-fusion/)
- cancers: [ALK-positive non-small-cell lung cancer](https://onco.cc/cancers/alk-positive-nsclc/), [Chronic myeloid leukaemia, accelerated and blast phase](https://onco.cc/cancers/cml-advanced-phase/), [Chronic myeloid leukaemia, chronic phase](https://onco.cc/cancers/cml-chronic-phase/), [EGFR-mutated non-small-cell lung cancer](https://onco.cc/cancers/egfr-mutant-nsclc/), [MET exon 14 and MET-amplified non-small-cell lung cancer](https://onco.cc/cancers/met-altered-nsclc/), [RET fusion-positive non-small-cell lung cancer](https://onco.cc/cancers/ret-fusion-nsclc/), [ROS1-positive non-small-cell lung cancer](https://onco.cc/cancers/ros1-positive-nsclc/)

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