Table 1
Approved protein kinase inhibitors (adapted from http://www.brimr.org/PKI/PKIs.htm)
Drug
Company
Known targets
Class Disease
Year
approved
Abemaciclib
Lilly
CDK4/6
S/T
Breast cancer
2017
Acalabrutinib Acerta Pharma BTK
NRY Mantle cell lymphoma
2017
Afatinib
Boehringer
Ingelheim
EGFR, ErbB2, ErbB4
RY
NSCLC
2013
Alectinib
Hoffmann-La
Roche
ALK, RET
RY
NSCLC (ALK
+
)
2015
Axitinib
Pfizer
VEGFR1/2/3, PDGFRβ
RY
RCC
2012
Baricitinib
Lilly
JAK1/2
NRY Rheumatoid arthritis
2018
Binimetinib
Array
MEK1/2
S/T
Melanoma
2018
Bosutinib
Pfizer
BCR-Abl, SRC, LYN, and HCK
NRY CML
2012
Brigatinib
Ariad
ALK, ROS1, IGF-1R, Flt3, EGFR
RY
NSCLC (ALK
+
)
2017
Cabozantinib Exelixis
RET, MET, VEGFR1/2/3, KIT, TrkB, FLT3,
AXL, TIE2
RY
RCC, HCC, medullary thyroid cancer
2012
Ceritinib
Novartis
ALK, IGF-1R, InsR, ROS1
RY
NSCLC, ALK
+
after crizotinib resistance
2014
Cobimetinib
Genentech
MEK1/2
T/Y
Melanoma with BRAF mutations together with
vemurafenib
2015
Crizotinib
Pfizer
ALK, MET (HGFR), ROS1, MST1R
RY
NSCLC (ALK
+
or ROS1
+
)
2011
Dabrafenib
GSK
BRAF, BRAF
V600E
, CRAF
S/T
Melanoma, NSCLC (BRAF
V600+
)
2013
Dacomitinib
Pfizer
EGFR family
RY
EGFR-mutant NSCLC
2018
Dasatinib
Bristol-Myers
Squibb
BCR-ABL, EGFR, SRC, LCK, YES, FYN, KIT,
EphA2, PDGFRβ
NRY CML
2006
Encorafenib
Array
BRAF
S/T
Melanoma
2018
Erlotinib
Genentech
EGFR
RY
NSCLC, pancreatic cancer
2004
Everolimus
Novartis
FKBP12/mTOR
S/T
Breast cancer (HER2
À
), PNET, RCC,
angiomyolipoma, SEGA
2009
Fostamatinib Rigel
SYK, spleen tyrosine kinase
RY
Thrombocytopenia
2018
128
A. Moschopoulou et al.