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