In advanced, progressive, well-differentiated nonfunctional GI and lung NET, and advanced, progressive pNET
AFINITOR delivers a triple antitumor effect both in vitro and in vivo1,2
mTOR pathway activation is common across the NET spectrum, including GI and lung NET, and pNET
- >70% of clinical specimens of ileal GI NET and lung NET3,4
- mTOR pathway activation is most common in well-differentiated (G1/G2) lung NET
- 52% to 67% of pNET5,6
- Insulin-driven activation of the PI3K/Akt/mTOR pathway is thought to play a key role in normal pancreatic cell proliferation2
The high rate of mTOR pathway activation in NET
makes mTOR inhibition with AFINITOR
a rational approach to targeted therapy.
As an mTOR inhibitor, AFINITOR delivers a triple antitumor effect in vitro and in vivo by directly inhibiting1:
Triple antitumor effect:
Target advanced, progressive, well-differentiated nonfunctional GI and lung NET, and advanced, progressive pNET, with the triple antitumor effect of AFINITOR.
GI, gastrointestinal; MOA, mechanism of action; mTOR, mammalian target of rapamycin; NET, neuroendocrine tumor(s); pNET; pancreatic neuroendocrine tumor(s).
- AFINITOR [summary of product characteristics]. Basel, Switzerland: Novartis Pharma AG; May 2016.
- Yuan R, Kay A, Berg WJ, Lebwohl D. Targeting tumorigenesis: development and use of mTOR inhibitors in cancer therapy. J Hematol Oncol. 2009;2:45.
- Geis C, Fendrich V, Rexin P, et al. Ileal neuroendocrine tumors show elevated activation of mammalian target of rapamycin complex. J Surg Res. 2015;194(2):388-393.
- Bago-Horvath Z, Sieghart W, Grusch M, et al. Synergistic effects of erlotinib and everolimus on bronchial carcinoids and large-cell neuroendocrine carcinomas with activated EGFR/AKT/mTOR pathway. Neuroendocrinology. 2012;96(3):228-237.
- Komori Y, Yada K, Ohta M, et al. Mammalian target of rapamycin signaling activation patterns in pancreatic neuroendocrine tumors. J Hepatobiliary Pancreat Sci. 2014;21(4):288-295.
- Kasajima A, Pavel M, Darb-Esfahani S, et al. mTOR expression and activity patterns in gastroenteropancreatic neuroendocrine tumours. Endocr Relat Cancer. 2011;18(1):181-192.