Skip to main content

Table 3 Current status of PI3K inhibitors in clinical trials (data from http://clinicaltrials.gov)

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