{"entity":{"id":"tki-term","kind":"term","name":"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","kinase inhibitors","multikinase inhibitors","next-generation TKIs","targeted pills"],"tldr":"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.","asOf":"2026-09-09","wikipedia":"https://en.wikipedia.org/wiki/Tyrosine_kinase_inhibitor","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Tyrosine_kinase_inhibitor"}],"tags":[],"related":["gatekeeper-mutation","driver-mutation","oncogene-addiction","rash-skin-toxicity"],"cancers":[],"sections":["targeted-therapy"],"technologies":["kinase-inhibitors"],"targets":[],"drugs":["imatinib","osimertinib","ibrutinib","zanubrutinib","lenvatinib","cabozantinib"],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"category":"Treatment jargon"},"route":"/terms/tki-term/","neighbours":{"term":[{"id":"antiangiogenic-toxicities","kind":"term","name":"Anti-VEGF class toxicities (hypertension, proteinuria, bleeding, perforation)","route":"/terms/antiangiogenic-toxicities/"},{"id":"braf-v600-mutation","kind":"term","name":"BRAF V600E mutation","route":"/terms/braf-v600-mutation/"},{"id":"cns-penetration","kind":"term","name":"CNS penetration (brain-penetrant drugs)","route":"/terms/cns-penetration/"},{"id":"driver-mutation","kind":"term","name":"Driver mutation","route":"/terms/driver-mutation/"},{"id":"egfr-mutation-subtypes","kind":"term","name":"EGFR mutation subtypes (exon 19 deletion, L858R, exon 20 insertion, T790M)","route":"/terms/egfr-mutation-subtypes/"},{"id":"hand-foot-syndrome","kind":"term","name":"Hand-foot syndrome and hand-foot skin reaction","route":"/terms/hand-foot-syndrome/"},{"id":"molecular-response","kind":"term","name":"Molecular response (MMR, MR4, treatment-free remission)","route":"/terms/molecular-response/"},{"id":"gatekeeper-mutation","kind":"term","name":"On-target resistance mutations (gatekeeper, solvent-front, compound)","route":"/terms/gatekeeper-mutation/"},{"id":"oncogene-addiction","kind":"term","name":"Oncogene addiction","route":"/terms/oncogene-addiction/"},{"id":"philadelphia-chromosome","kind":"term","name":"Philadelphia chromosome (Ph+, BCR::ABL1)","route":"/terms/philadelphia-chromosome/"},{"id":"qt-prolongation","kind":"term","name":"QT prolongation","route":"/terms/qt-prolongation/"},{"id":"rash-skin-toxicity","kind":"term","name":"Rash and skin toxicity (acneiform rash, paronychia)","route":"/terms/rash-skin-toxicity/"}],"section":[{"id":"targeted-therapy","kind":"section","name":"Targeted Therapy","route":"/fronts/targeted-therapy/"}],"technology":[{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"drug":[{"id":"cabozantinib","kind":"drug","name":"Cabozantinib","route":"/drugs/cabozantinib/"},{"id":"ibrutinib","kind":"drug","name":"Ibrutinib","route":"/drugs/ibrutinib/"},{"id":"imatinib","kind":"drug","name":"Imatinib","route":"/drugs/imatinib/"},{"id":"lenvatinib","kind":"drug","name":"Lenvatinib","route":"/drugs/lenvatinib/"},{"id":"osimertinib","kind":"drug","name":"Osimertinib","route":"/drugs/osimertinib/"},{"id":"zanubrutinib","kind":"drug","name":"Zanubrutinib","route":"/drugs/zanubrutinib/"}],"trial":[{"id":"alesia","kind":"trial","name":"ALESIA","route":"/trials/alesia/"},{"id":"alex","kind":"trial","name":"ALEX","route":"/trials/alex/"},{"id":"nct01774721","kind":"trial","name":"ARCHER 1050","route":"/trials/nct01774721/"},{"id":"nct01828099","kind":"trial","name":"ASCEND-4","route":"/trials/nct01828099/"},{"id":"aura3","kind":"trial","name":"AURA3","route":"/trials/aura3/"},{"id":"nct02767804","kind":"trial","name":"eXalt3","route":"/trials/nct02767804/"},{"id":"flaura","kind":"trial","name":"FLAURA","route":"/trials/flaura/"},{"id":"j-alex","kind":"trial","name":"J-ALEX","route":"/trials/j-alex/"},{"id":"lux-lung-3","kind":"trial","name":"LUX-Lung 3","route":"/trials/lux-lung-3/"},{"id":"profile-1001-ros1","kind":"trial","name":"PROFILE 1001 ROS1 expansion cohort","route":"/trials/profile-1001-ros1/"},{"id":"profile-1014","kind":"trial","name":"PROFILE 1014","route":"/trials/profile-1014/"}],"paper":[{"id":"paper-lemmon-schlessinger-rtk-signalling-cell-2010","kind":"paper","name":"Lemmon and Schlessinger 2010: cell signalling by receptor tyrosine kinases","route":"/key-papers/paper-lemmon-schlessinger-rtk-signalling-cell-2010/"}],"institution":[{"id":"chongqing-university-cancer-hospital","kind":"institution","name":"Chongqing University Cancer Hospital","route":"/institutions/chongqing-university-cancer-hospital/"}],"biomarker":[{"id":"alk-fusion","kind":"biomarker","name":"ALK fusion (ALK-positive)","route":"/biomarkers/alk-fusion/"},{"id":"ntrk-fusion","kind":"biomarker","name":"NTRK1/2/3 gene fusion","route":"/biomarkers/ntrk-fusion/"},{"id":"ret-fusion","kind":"biomarker","name":"RET fusion and RET mutation","route":"/biomarkers/ret-fusion/"},{"id":"ros1-fusion","kind":"biomarker","name":"ROS1 fusion (ROS1-positive)","route":"/biomarkers/ros1-fusion/"}],"cancer":[{"id":"alk-positive-nsclc","kind":"cancer","name":"ALK-positive non-small-cell lung cancer","route":"/cancers/alk-positive-nsclc/"},{"id":"cml-advanced-phase","kind":"cancer","name":"Chronic myeloid leukaemia, accelerated and blast phase","route":"/cancers/cml-advanced-phase/"},{"id":"cml-chronic-phase","kind":"cancer","name":"Chronic myeloid leukaemia, chronic phase","route":"/cancers/cml-chronic-phase/"},{"id":"egfr-mutant-nsclc","kind":"cancer","name":"EGFR-mutated non-small-cell lung cancer","route":"/cancers/egfr-mutant-nsclc/"},{"id":"met-altered-nsclc","kind":"cancer","name":"MET exon 14 and MET-amplified non-small-cell lung cancer","route":"/cancers/met-altered-nsclc/"},{"id":"ret-fusion-nsclc","kind":"cancer","name":"RET fusion-positive non-small-cell lung cancer","route":"/cancers/ret-fusion-nsclc/"},{"id":"ros1-positive-nsclc","kind":"cancer","name":"ROS1-positive non-small-cell lung cancer","route":"/cancers/ros1-positive-nsclc/"}]}}