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2016 ; 9
(ä): 5495-505
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Sunitinib: the antiangiogenic effects and beyond
#MMPMID27660467
Hao Z
; Sadek I
Onco Targets Ther
2016[]; 9
(ä): 5495-505
PMID27660467
show ga
As a multitargeted kinase inhibitor, sunitinib has carved its way into
demonstrating itself as a most effective tyrosine kinase inhibitor in the
treatment of metastatic renal cell carcinoma. Mechanistically, sunitinib inhibits
multiple receptor tyrosine kinases, especially those involved in angiogenesis,
that is, vascular endothelial growth factor receptor, platelet-derived growth
factor receptor, and proto-oncogene cKIT. Sunitinib has also been implicated in
enhancing cancer invasiveness and metastasis. Mechanisms of resistance are poorly
understood, but both intrinsic and acquired mechanisms are thought to be
involved. While the side effects are manageable, sunitinib, like many other
tyrosine kinase inhibitors, can be associated with serious toxicities that
require careful management including frequent dose reductions. Although still in
the early stage, emerging evidence points to an immunomodulatory role for
sunitinib. It is also likely to contribute to the overall outcomes, especially
those seen in metastatic renal cell carcinoma, and such effects are thought to be
mediated by the proto-oncogene cKIT receptor. Combination with other modalities
such as stereotactic body radiation therapy, therapeutic vaccines, and checkpoint
inhibitors is being pursued for improved efficacy.
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