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. Author manuscript; available in PMC: 2015 Jul 1.
Published in final edited form as: Nat Rev Cancer. 2015 Jan;15(1):7–24. doi: 10.1038/nrc3860

Table 4. Isoform-selective PI3K inhibitors and their clinical applications.

Agent Company Target Trial stage* Tumor types*
BYL719 Novartis p110α I and II

  • SCCHN

  • ESCC

  • Colorectal

  • Breast

  • GIST

  • Kidney

  • Pancreas

  • Gastric

  • Adv. solid tumors
GDC0032 Genentech p110α I

  • Breast

  • Adv. solid tumors
INK1117 Intellikine/Millenium p110α I

  • Adv. solid tumors
AZD8186 Astra-Zeneca p110β I

  • CRPC

  • sqNSCLC

  • TNBC

  • Adv.solid tumors with PTEN deficiency
GSK2636771 GlaxoSmithKline p110β I and II

  • Adv.solid tumors with PTEN deficiency
SAR260301 Sanofi p110β I

  • Adv.solid tumors

  • Lymphoma
IPI145 Infinity p110δ and p110γ I, II, and III

  • CLL

  • SLL

  • ALL

  • INHL

  • Hematologic malignancies
AMG319 Amgen p110δ I Lymphoid malignancies
CAL101 (GS101) Gilead Sciences p110δ I, II, and III

  • INHL

  • CLL

  • MCL

  • SLL

  • Hodgkin lymphoma

  • Non-Hodgkin lymphoma

  • Other lymphomas

  • AML

  • MM

  • Hematologic malignancies
GS9820 Gilead Sciences p110β and p110δ I

  • Lymphoid malignancies
*

Data taken from an April 2014 search of http://www.clinicaltrials.gov.

SCCHN, squamous cell carcinoma of the head and neck; ESCC, esophageal squamous cell carcinoma; GIST, gastrointestinal stromal tumor; CRPC, castration-resistant prostate cancer; sqNSCLC, squamous non-small cell lung cancer; TNBC, triple-negative breast cancer; CLL, chronic lymphocytic leukemia; SLL, small lymphocytic leukemia; ALL, acute lymphoblastic leukemia; INHL, indolent non-Hodgkin lymphoma; MCL, mantle cell lymphoma; AML, acute myeloid leukemia; MM, multiple myeloma