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Table 3 Current status of PI3K inhibitors in clinical trials (data from

From: Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development

Classification Drug name Tumor(s) Clinical trials
Pan-PI3K inhibitors Pictilisib (GDC-0941) Breast cancer, NSCLC, NHL, GBM Phase I/II
Taselisib (GDC-0032) Breast, ovarian, uterus and squamous cell lung cancers, NSCLC, NHL, lymphoma Phase I-III
Buparlisib (BKM120) Breast, prostate, endometrial, cervical, esophageal, ovarian, colorectal, and H&N cancers, GBM, NSCLC, GIST, RCC, melanoma, lymphoma, leukemia, Phase I-III
Pilaralisib (XL147, SAR245408) Breast, endometrial, and ovarian cancers, GBM, NSCLC, lymphoma Phase I/II
Copanlisib (BAY 80–6946) Endometrial, and H&N cancers, cholangiocarcinoma, lymphoma, NHL Phase I-III
Sonolisib (PX-866) Prostate, colorectal, and H&N cancers, melanoma, NSCLC, GBM Phase I/II
ZSTK474 Solid tumors Phase I
Isoform-selective inhibitors Alpelisib (BYL719) Breast, ovarian, gastric, pancreatic, colorectal, H&N, and rectal cancers, melanoma, ESCC, NSCLC, RCC, GIST, MM Phase I/II
Idelalisib (CAL-101, GS-1101) CLL, AML, NHL, MM, and other hematologic malignancies Phase I-IV
AMG319 H&N cancer, CLL, lymphoma Phase I/II
CH5132799 Solid tumors Phase I
MLN1117 (INK1117) RCC, solid tumors Phase I/II
Dual PI3K/mTOR inhibitors Dactolisib (NVP-BEZ235) Breast, prostate, and endometrial cancer, pancreatic neuroendocrine tumor, RCC, GBM, leukemia Phase I/II
NVP-BGT226 Breast cancer, solid tumors Phase I/II
Omipalisib (GSK2126458, GSK458) Solid tumors Phase I
GSK1059615 Lymphoma, solid tumors Phase I
Voxtalisib (XL765, SAR245409) Breast, and ovarian cancers, NSCLC, lymphoma, GBM Phase I/II
Apitolisib (GDC-0980) Breast, prostate, and endometrial cancers, RCC, NHL Phase I/II
GDC-0084 (RG7666) High-grade gliomas Phase I
VS-5584 (SB2343) Malignant mesothelioma, lymphoma, advanced non-hematologic malignancies Phase I
PF-04691502 Breast, and endometrial cancers Phase I/II
Gedatolisib (PF-05212384, PKI-587) Breast, endometrial, colorectal, ovarian, and H&N cancers, NSCLC, SCLC, AML Phase I/II
PQR309 Breast cancer, GBM, lymphoma Phase I/II
  1. NHL Non-Hodgkin’s lymphoma, CLL chronic lymphocytic leukemia, AML acute myeloid leukemia, MM multiple myeloma, NSCLC non-small cell lung cancer, SCLC small cell lung cancer, GBM glioblastoma, GIST gastrointestinal stromal tumor, H&N head and neck cancer, RCC renal cell cancer, ESCC esophageal squamous cell carcinoma