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Table 2 Phosphatidylinositol 3-kinase pathway inhibitors in clinical development

From: Mutations in the phosphatidylinositol 3-kinase pathway: role in tumor progression and therapeutic implications in breast cancer

Kinase target Drug Manufacturer Mechanism of action
Pan-PI3K BKM120 Novartis ATP-competitive
  XL-147 Exelixis ATP-competitive
  PX-866 Oncothyreon ATP-competitive
  GDC-0941 Genentech/Roche ATP-competitive
  CH5132799 Chugai Pharma ATP-competitive
p110δ-specific CAL-101 Calistoga ATP-competitive
p110α-specific BYL719 Novartis ATP-competitive
  GDC-0032 Genentech/Roche ATP-competitive
  INK-1117 Intellikine ATP-competitive
PI3K/mTOR PKI-587 Pfizer ATP-competitive
  BEZ235 Novartis ATP-competitive
  BGT226 Novartis ATP-competitive
  PF-4691502 Pfizer ATP-competitive
  GDC-0980 Genentech/Roche ATP-competitive
  XL-765 Exelixis ATP-competitive
  SF1126 Semafor ATP-competitive/peptide-conjugate
  GSK1059615 GSK ATP-competitive
TORC1 Everolimus (RAD001) Novartis Indirect, FKBP12-mediated
  Temsirolimus (CCI-779) Wyeth/Pfizer Indirect, FKBP12-mediated
  Ridaferolimus (AP-23573) Merck/Ariad Indirect, FKBP12-mediated
TORC1/TORC2 INK-128 Intellikine ATP-competitive
  OSI-027 OSI Pharm. ATP-competitive
  AZD-8055 Astrazeneca ATP-competitive
AKT AZD5363 Astrazeneca ATP-competitive
  GDC-0068 Genentech/Roche ATP-competitive
  GSK690693 GSK ATP-competitive
  MK-2206 Merck Allosteric
  VQD002 Vioquest ATP-competitive
  1. mTOR, mammalian target of rapamycin; PI3K, phosphatidylinositol 3-kinase.