Skip to main content
. Author manuscript; available in PMC: 2014 Jul 1.
Published in final edited form as: Cancer J. 2013 Jul-Aug;19(4):311–315. doi: 10.1097/PPO.0b013e31829d5cea

Table 1.

PI3-K/Akt/mTOR Inhibitors in Clinical Development

Agent Company Stage of Clinical Development

Pan-Isoform PI3-K Inhibitors
SAR245408 (XL147) Sanofi/Adventis, Exelixis Phase I, II
BKM120 Novartis Phase II, III
GDC-0941 Genentech Phase I, II
BAY 80–6946 Bayer Phase I
GSK1059615 GlaxoSmithKline Phase I
ZSTK474 Zenyaku Phase I

PI3-K/mTOR Inhibitors
SAR254409 (XL765) Sanofi/Adventis, Exelixis Phase I, II
BEZ235 Novartis Phase I, II
GDC-0980 Genentech Phase I, II
GSK1059615 GlaxoSmithKline Phase I
PF-04691502 Pfizer Phase I
PKI-587 Pfizer Phase I
PWT33597 Pathway Therapeutics Phase I

Active Site mTOR Inhibitors
MLN0128 Millenium, Intellikine Phase I
OSI-027 Astellas Phase I
AZD8055 AstraZeneca Phase I

Isoform-Specific PI3-K Inhibitors
BYL719 (alpha specific) Novartis Phase I
INK1117 (alpha specific Intellikine/Millenium Phase I
SAR260301 (beta specific) Sanofi-Adventis Phase I
TGR-1202 (delta specific) TG Therapeutics Phase I
GS-1101 (delta specific) Gilead Phase II-III
AS-252424 (upsilon specific) Merck Serono Pre-clinical

Akt Inhibitors
GDC-0068 Genentech Phase I, II
MK2206 (allosteric inhibitor) Merck Phase I, II
GSK690693 GlaxoSmithKline Phase I, II