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eISSN 2508-786X

Table. 1.

Table. 1.

Approved kinase inhibitors for cancer

Kinase inhibitorFDA approval yearKFDA approval yearBrand name (U.S)IndicationBlack box warning
Primary target: ALKCrizotinib20112011Xalkori  
Ceritinib20142015Zykadia
Alectinib20152016AlecensaALK-positive NSCLC 
Brigatinib20172018Alunbrig 
Lorlatinib2018-Lorbrena 

BCR-ABLImatinib20012006GleevecPh+ ALL or CML, aggressive systemic mastocytosis, dermatofibrosarcoma protuberans, Kit (CD117)-positive GIST, et al 
Dasatinib20062007SprycelPh+ ALL or CML 
Nilotinib20072007TasignaPh+ CMLQT prolongation and Sudden Deaths
Bosutinib2012-BosulifPh+ CML 
Ponatinib20122017IclusigPh+ ALL or CMLHepatotoxicity, Arterial occlusion, Heart failure, Venous thromboembolism

BRAFVemurafenib20112012ZelborafBRAF-mutant melanoma 
Dabrafenib20132014TafinlarBRAF-mutant melanoma, NSCLC, anaplastic thyroid cancer 
Encorafenib2018-BraftoviBRAF-mutant melanoma 

BTKIbrutinib20132014ImbruvicaChronic lymphocytic leukemia, mantle cell lymphoma, et al 
Acalabrutinib2017-CalquenceMantle cell lymphoma 

CDK4&6Palbociclib20152016IbranceHR-positive, HER2-negative breast cancer   
Ribociclib2017-Kisqali
Abemaciclib20172019Verzenio

CSF1RPexidartinib2019-TuralioTenosynovial giant cell tumorHepatotoxicity

EGFRGefitinib20032003Iressa 
Erlotinib20042005Tarceva 
Afatinib20132014GilotrifEGFR-mutant NSCLC 
Osimertinib20152016Tagrisso 
Dacomitinib2018-Vizimpro 

HER2Lapatinib20072007TykerbHER2-positive breast cancerHepatotoxicity  
Neratinib2017-Nerlynx

FGFRErdafitinib2019-BalversaUrothelial carcinoma, locally advanced or metastatic 

FLT3Midostaurin20172019RydaptFLT3-positive acute myeloid leukemia (AML), mast cell leukemia, et al 
Gilteritinib2018-XospataFLT3-positive AMLDifferentiation syndrome

MEKTrametinib20132015MekinistBRAF-mutant melanoma, NSCLC, anaplastic thyroid cancer  
Cobimetinib20152015CotellicBRAF-mutant melanoma
Binimetinib2018-MektoviBRAF-mutant melanoma 

PI3KIdelalisib20142015ZydeligChronic lymphocytic leukemia, follicular B-cell non-Hodgkin lymphoma, et alHepatotoxicity, Severe diarrhea/ colitis, Pneumonitis, Infection, Intestinal perforation
Alpelisib2019-PiqrayHR-positive, HER2-negative, PIK3CAmutant breast cancer 

TRKLarotrectinib2018-VitrakviSolid tumors with NTRK fusion proteins 

VEGFRSorafenib20052008NexavarHCC, RCC, differentiated thyroid cancer 
Sunitinib20062006SutentGIST, pancreatic neuroendocrine tumors, RCCHepatotoxicity
Pazopanib20092010VotrientRCC, soft tissue sarcomasHepatotoxicity
Vandetanib20112013CaprelsaMedullary thyroid cancerQT prolongation, torsades de pointes, and sudden death
Axitinib20122012InlytaRCC
Cabozantinib20122017CabometyxMedullary thyroid cancer, HCC, RCC,Hemorrhage, Perforations and fistulas
Regorafenib20122013StivargaMetastatic colorectal cancer, GIST, HCCHepatotoxicity
Lenvatinib20152015LenvimaHCC, RCC, differentiated thyroid cancer 

ALK, anaplastic lymphoma kinase; ALL, acute lymphoblastic leukemia; BRAF, v-raf murine sarcoma viral oncogene homolog B1; BTK, bruton’s tyrosine kinase; CDK, cyclin-dependent kinase; CML, chronic myeloid leukemia; CSF, colony stimulation factor; EGFR, epidermal growth factor receptor; FGFR, fibroblast growth factor receptor; FLT3, fms related tyrosine kinase 3; GIST, gastrointestinal stromal tumor; HCC, hepatocellular carcinoma; HER2, human epidermal growth factor receptor 2; HR, hormone receptor; MEK, mitogen-activated protein kinase kinase; NSCLC, non-small cell lung cancer; PI3K, phosphatidylinositol 3-kinase; PIK3CA, phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha; Ph+, philadelphia chromosome-positive; RCC, renal cell carcinoma; TRK, tropomyosin receptor kinase; NTRK, neurotrophic receptor tyrosine kinase; VEGFR, vascular endothelial growth factor receptor.

Korean J Clin Pharm 2019;29:223-30 https://doi.org/10.24304/kjcp.2019.29.4.223
© 2019 Korean J Clin Pharm