Tyrosine kinase inhibitor
They are also called tyrphostins, the short name for "tyrosine phosphorylation inhibitor", originally coined in a 1988 publication,[1] which was the first description of compounds inhibiting the catalytic activity of the epidermal growth factor receptor (EGFR).[4][5] Based on this work imatinib was developed against chronic myelogenous leukemia (CML)[6] and later gefitinib and erlotinib aiming at the EGF receptor.[8] Adavosertib is a Wee1 kinase inhibitor that is undergoing numerous clinical trials in the treatment of refractory solid tumors.[11] Imatinib, sunitinib, sorafenib, and pazopanib have been studied in the treatment of aggressive fibromatosis (desmoid tumor).[14] Recently TKIs have been shown to deprive tyrosine kinases of access to the Cdc37-Hsp90 molecular chaperone system on which they depend for their cellular stability, leading to their ubiquitylation and degradation.
Bcr-Abl tyrosine-kinase inhibitornilotinibchronic myelogenous leukemiahematological malignancypharmaceutical druginhibitstyrosine kinasesenzymessignal transductionphosphatephosphorylationidiopathic pulmonary fibrosistyrosineinhibitorcatalytic activityepidermal growth factor receptorprotein kinasesserinethreonineinsulin receptorleukemicimatinibgefitiniberlotinibDasatinibsenolyticSunitinibVEGF receptorsAdavosertibmyelosuppressiondiarrheaLapatinibsorafenibpazopanibaggressive fibromatosisadenosine triphosphatesubstrateallostericconformational changeubiquitylationnintedanibProtein kinase inhibitorBibcodeFrontiers in PharmacologyCancersEuropean Medicines AgencyTargeted cancer therapyantineoplastic agentsmonoclonal antibodiesReceptor tyrosine kinaseHER1/EGFRCetuximabPanitumumabHER2/neuPertuzumabTrastuzumab+hyaluronidaseTrastuzumab emtansineTrastuzumab deruxtecanZanidatamabCatumaxomabEdrecolomabVEGF-ABevacizumabLeukemialymphomalymphoidGlofitamabElranatamabMosunetuzumabIbritumomabObinutuzumabOfatumumabRituximabTositumomabBrentuximabAlemtuzumabmyeloidGemtuzumab ozogamicinAmivantamabAtezolizumabAvelumabAxatilimabBelantamab mafodotinBermekimabBlinatumomabCemiplimabCosibelimabDaratumumabDinutuximab betaDostarlimabDurvalumabElotuzumabEnfortumab vedotinEpcoritamabInotuzumab ozogamicinIpilimumabIsatuximabLoncastuximab tesirineMirvetuximab soravtansineMogamulizumabMoxetumomab pasudotoxNaxitamabNecitumumabNivolumab+relatlimabOlaratumabOportuzumab monatoxPembrolizumabPolatuzumab vedotinRamucirumabRetifanlimabSacituzumab govitecanSerplulimabSugemalimabTafasitamabTalquetamabTarlatamabTeclistamabTislelizumabTisotumab vedotinToripalimabTremelimumabZenocutuzumabZolbetuximabAfatinib