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