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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.
Showing the molecule this term concerns: Imatinib.
The glossary entry explains the word; the readout page carries the scoring rule, the thresholds approvals use, the companion diagnostics and the tests.
Shares ALESIA, J-ALEX, PROFILE 1001 ROS1 expansion cohort, eXalt3.
Shares CNS penetration (brain-penetrant drugs), ALESIA, J-ALEX, eXalt3.
Shares Molecular response (MMR, MR4, treatment-free remission), Philadelphia chromosome (Ph+, BCR::ABL1), On-target resistance mutations (gatekeeper, solvent-front, compound), Chronic myeloid leukaemia, chronic phase.
Shares PROFILE 1001 ROS1 expansion cohort, ROS1 fusion (ROS1-positive), Philadelphia chromosome (Ph+, BCR::ABL1), PROFILE 1014.
Shares Molecular response (MMR, MR4, treatment-free remission), Philadelphia chromosome (Ph+, BCR::ABL1), Chronic myeloid leukaemia, chronic phase, Chronic myeloid leukaemia, accelerated and blast phase.
Shares LUX-Lung 3, ARCHER 1050, FLAURA, Osimertinib.
Shares ALESIA, J-ALEX, PROFILE 1014, ALEX.
Shares Lemmon and Schlessinger 2010: cell signalling by receptor tyrosine kinases, ALESIA, J-ALEX, eXalt3.