Buparlisib
(BKM120) is an oral
pan-PI3K inhibitor targeting all four
isoforms of class I PI3K (
ɑ
, β, γ, δ)
1
Targeting all class I isoforms may
ensure broad activity in tumors with a
range of molecular drivers
2–5
Alpelisib
(BYL719) is an oral inhibitor
selectively targeting the
α isoform of class I PI3K
6,7
Inhibition of the α isoformmay
reduce off-target toxicity
5,6
Novartis PI3K Inhibitors in Clinical Development
Regulatory
subunit
Catalytic subunit
(4 isoforms: α β γ δ)
p110
p85
PI3K
α
β
γ
δ
α
Buparlisib
Pan-PI3K inhibitor
Alpelisib
PI3Kα inhibitor
IC
50
(nM)
1
52
166
262
116
IC
50
(nM)
6
5
1. Maira SM,
et al
.
Mol Cancer Ther
2012;11:317–328; 2. Liu P,
et al. Nat Rev Drug Disc
2009;8:627–644;
3. Kang S,
et al
.
Proc Natl Acad Sci
USA 2006;103:1289–1294; 4. Hernandez-Aya LF,
et al. Oncologist
2011;16:404–414;
5. Jia S,
et al
.
Curr Opin Cell Biol
2009;21:199–208; 6. Fritsch C,
et al. AACR
2012; Abstr 3748; 7. Juric D,
et al. AACR
2012; Abstr CT-01.
1
6
0
9
0
4
3
6
8
1
BUPARLISIB Y ALPELISIB
