• Alpelisib is an oral inhibitor that selectively targets
the α-isoform of class I PI3K
1,2
• PI3Kα inhibitors may be effective in cancers that
signal heavily through the α-isoform,
3,4
such as:
– Tumors with
PIK3CA
mutations
– HER2-overexpressing tumors
• Compared to pan-PI3K inhibitors,
alpelisib may:
– Have an improved safety profile
1,5
– Have a greater impact on angiogenesis
6
Alpelisib: A PI3K
Selective Inhibitor
CNS, central nervous system; HER2, human epidermal growth factor receptor 2; mTORC,
mammalian target of rapamycin complex;
PI3K, phosphatidylinositol 3-kinase; PIP
2
, phosphatidylinositol 4,5-bisphosphate; PIP
3
,
phosphatidylinositol (3,4,5)-trisphosphate;
PTEN, phosphatase and tensin homolog; RTK, receptor tyrosine kinase.
1. Fritsch C, et al. Cancer Research 2012;72:abstr 3748; 2. Juric D, et al. Cancer Research
2012;72:abstr CT–01;
3. Huang A, et al. Cancer Research 2012;72:abstr 3749; 4. Brana I and Siu LL. BMC Med
2012;10:161;
5. Jia S, et al. Curr Opin Cell Biol 2009;21:199–208; 6. Schnell CR, et al. Cancer Res 2012;72:abstr
3743.
PI3K
RTK
PIP
2
PIP
3
AKT
PTEN
mTORC1
mTORC2
Alpelisib
PI3Kα
