Table 1.
Clinical development of both conventional and novel mTOR inhibitors
| Target | Compound (company) | Malignancy | Phase of development |
|---|---|---|---|
| mTORC1 | Everolimus (Novartis) |
Renal cell carcinoma, subependymal giant cell astrocytoma, pancreatic neuroendocrine tumors, ER + breast cancer (in combination with exemestane) | Approved |
| Temsirolimus (Pfizer) | Renal cell carcinoma | Phase II | |
| PI3K/mTOR | BEZ235 (Novartis) | Advanced solid tumors, breast cancer, castration-resistant prostate cancer, renal cell carcinoma, leukemias, pancreatic neuroendocrine tumors, urothelial transitional cell carcinoma | Phase II |
| GDC-0980 (Genentech) | Solid cancers, non-Hodgkin lymphoma, breast cancer, prostate cancer | Phase II | |
| PF-05212384 (Pfizer) | Advanced solid tumors, colorectal cancer, endometrial neoplasms | Phase II | |
| SAR245409 (XL-765; Sanofi/Exelixis) | Advanced solid tumors, CLL, indolent non-Hodgkin lymphoma, mantle cell lymphoma, ovarian cancer | Phase I | |
| VS-5584 (Verastem, Inc) | Advanced solid tumours, Relapsed mesothelioma, | Preclinical | |
| PI-103 | Xenograft and in-vivo models | Phase II | |
| mTORC1/2 | AZD2014 (AstraZeneca) | Advanced solid tumors, breast cancer, renal cell carcinoma | Phase I/II |
| CC-223 (Celgene) | Breast cancer, glioblastoma, hematologic malignancies, liver cancer, NSCLC, neuroendocrine tumors | Phase I | |
| AZD8055 (AstraZeneca) | Hepatocellular carcinoma, Glioblastoma Mutiforme | Phase I | |
| INK128 (National Cancer Institute) (NCI) | Recurrent Glioblastoma, Metastatic Anaplastic Thyroid Cancer | Phase I | |
| MLN0128 (INK128; Intellikine) | Advanced solid tumors, hematologic malignancies | Phase II | |
| Temsirolimus (Pfizer) | Advanced solid tumors, breast cancer, castration-resistant prostate cancer,[53] renal cell carcinoma, leukemias, pancreatic neuroendocrine tumors, urothelial transitional cell carcinoma |
Phase II | |
| BEZ235 (Novartis) | Solid cancers, non-Hodgkin lymphoma, breast cancer, prostate cancer | Phase II |