Biomedical Engineering Reference
In-Depth Information
Table 1
FDA-approved targeted tyrosine kinase inhibitors
DCI name
(trade name)
Year of
approval
Target
Indication, cancer
Imatinib (Gleevec
®
,
Glivec
®
)
2001
BCR-ABL, c-KIT,
PDGRF
Philadelphia-positive-chronic myelog-
enous leukemia (CML) and acute
lymphoblastic leukemia (ALL)
Myelodisplasic syndrome-myeloprolifera-
tive disorders (MDS/MPD)
Aggressive systemic mastocytosis (ASM)
Hypereosinophilic syndrome (HES),
chronic eosinophilic leukemia (CEL)
Dermato- fi brosarcoma protuberans
(DFSP)
CD17-positive gastrointestinal stromal
tumors (GIST)
Ge fi tinib (Iressa
®
)
2003
EGFR
Non-small cell lung cancer (NSCLC)
Erlotinib (Tarceva
®
)
2004
EGFR
NSCLC
Pancreatic cancer
Sorafenib
(Nexavar
®
)
2005
VEGFR, PDGRF,
RAF, Mek, Erk
Hepato-cellular carcinoma (HCC)
Renal cell carcinoma (RCC)
Sunitinib (Sutent
®
)
2006
FLT3, PDGFR,
VEGFR, KIT
RCC, GIST
Pancreatic NET
Dasatinib (Sprycel
®
)
2006
Src, ABL
Philadelphia-positive CML, ALL
Lapatinib (Tyverb
®
)
2007
EGFR, HER2
HER2-positive breast cancer
Nilotinib (Tasigna
®
)
2007
BCR, ABL
Philadelphia-positive CML
Pazopanib
(Votrient
®
)
2009
VEGRF 1,2,3
RCC
Vandetanib
(Caprelsa
®
)
2011
VEGFR, EGFR
Thyroid cancer
Vemurafenib
(Zelboraf
®
)
2011
B-RAF
Melanoma with B-RAF V600E mutation
Crizotinib (Xalkori
®
)
2011
ALK, hepatocyte
growth factor
receptor
(HGFR; cMet)
Anaplastic lymphoma kinase
(ALK)-positive NSCLC
These therapeutic agents are about to revolutionize cancer treatment, and some
of them have allowed to transform deadly malignancies into chronically manage-
able conditions. Nevertheless, primary or secondary drug resistance, persistence of
cancer stem cells, and drug adverse effects still limit their ability to stabilize or even
cure malignant diseases in the long term. In addition, poor tolerance and therapeutic
failure are not uncommon, and relapse is a nearly inevitable consequence of treat-
ment interruption. The appropriate management of oncologic patients therefore
requires careful monitoring of these novel treatments [
4
], for which most clinicians
have at present a limited experience.
