Table 1.

Phosphoinositide 3-kinase inhibitors in development

DiscoveryPreclinicalPhase IPhase II
Eli LillyaXL-499 (Exelixis)fIPI-145 (Intellikine/Infinity)jCAL-101/GS-
Merck Serono S.A.bKAR-4141 (Karus)gCAL-263 (Calistoga/Gilead)k1101 (Calistoga/Gilead)
Incyte CorporationcUCB PharmahAMG-319 (Amgen)l 
Respivert LimiteddIncozen TherapeuticsiGlaxoSmithKlinem 
Cellzomee   
Pathway Therapeutics   
Genentech   
Intellikine/Infinity   
  • a Eli Lilly patent applications: WO2009064802; WO2008064018.

  • b Merck Serono patent application: WO2011058149.

  • c Incyte patent applications: WO2011075630; WO2011008487.

  • d Respivert patent applications: WO2011048111.

  • e The company has phosphoinositide 3-kinase program. Status and patent information are not available.

  • f The structure of XL-499 (Exelixis) is not disclosed. The patent information is not available.

  • g The structure of KAR-4141 (Karus) is not disclosed. The patent information is not available.

  • h The development candidate ID and structure are not disclosed. UCB Pharma Patent applications: WO2011058113; WO2011058112; WO2011058111; WO2011058110; WO2011058109; WO2011058108.

  • i The development candidate ID and structure are not disclosed. Incozen Patent application: WO2011055215.

  • j IPI-145 is a dual PI3Kδ/γ inhibitor. The structure is not disclosed. Intellikine/Infinity patent applications: WO2011008302; WO2010129816; WO2010036380; WO2009088986; WO2009088990.

  • k The structure of CAL-263 is not disclosed. Calistoga/Gilead patent application: WO2010123931.

  • l The structure of AMG-319 is not disclosed. Amgen patent applications: WO2011075628; WO2010151740; WO2010151737; WO2010151735; WO2010151791; WO2008118468; WO2008118455; WO2008118454.

  • m The clinical candidate ID and structure are not disclosed. The patent information is not available.