Table 1.
Inhibitors of the PI3K/AKT/mTOR pathway in clinical development
| Inhibitors | Target(s) | Tumor | Study phase | References |
|---|---|---|---|---|
| Alpelisib | PI3Kα | Advanced Solid Tumor | II | NCT01387321 |
| Duvelisib | PI3K | lymphoma or leukemia | II | NCT04707079 |
| Novartis (BYL719 ) | PI3Kα | SCC of the head and neck | II | NCT01602315 |
| breast cancer | II | NCT02506556 | ||
| Serabelisib (INK1117, TAK117, MLN1117) | PI3Kα | Metastatic Solid Tumors | I | NCT01449370 |
| Flupentixol | ATP binding area of PI3Kα | lung cancer | Preclinical | 70 |
| Capivasertib (AZD5363) | AKT | B-NHL | II | NCT05008055 |
| Afuresertib (GSK2110183) | AKT | Solid tumors, Hematologic malignancies | II | NCT01531894 |
| Uprosertib (GSK2141795) | AKT | Solid Tumors, Lymphoma | I | NCT01266954 |
| Ipatasertib (GDC-0068, RG7440) | AKT | Solid tumor | I | NCT04341259 |
| Perifosine | AKT | Neuroblastoma tumor, RCC, NSCLC | II | NCT00399789, NCT00399789 |
| Everolimus (RAD001) | mTORC1 | advanced NET, breast cancer, MM, non-functioning GI, pulmonary NENs | II (lung, MM) | NCT00401778, NCT00770120 |
| Temsirolimus | mTORC1 | RCC, LAM, lung cancer | II (lung, HL) | NCT00093782, NCT00838955 |
| Torin1 | ATP binding site of mTORC1 and mTORC2 | not mentioned | Preclinical | 86 |
| PI-103 | ATP binding sites of mTOR and PI3K | AML, glioblastoma, melanoma | Preclinical | 87 |
Abbreviations: NCT, ClinicalTrials.gov. No.; SCC, squamous cell carcinoma; B-NHL, B-cell Non-Hodgkin lymphoma; NSCLC, non-small cell lung cancer; GI, gastrointestinal; NENs, pulmonary neuroendocrine neoplasms; MM, malignant mesothelioma; NET, neuroendocrine tumor; LAM, lymphangioleiomyomatosis; AML, acute myeloid leukemia; RCC, renal cell carcinoma; HL, Hodgkin's lymphoma.