Table 1.
Some mTOR inhibitors used clinically and in research.
| Chemical | Class | Clinical uses/trials | References |
|---|---|---|---|
| Rapamycin Sirolimus Rapamune |
Rapalogue | FDA approved to prevent organ rejection following renal transplant and for use in drug eluting stents to prevent restenosis following angioplasty. Orphan drug status for bone sarcoma, tuberous sclerosis, and uveitis. Multiple active, recruiting, and completed trials. | [35, 62, 63] |
| Everolimus RAD001 Afinitor Zortress |
Rapalogue | FDA approved for subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis, specific forms of breast and pancreatic cancer, advanced renal cell carcinoma, noncancerous kidney tumors, and renal and liver transplants. Multiple active, recruiting, and completed trials. Orphan drug status for lymphoplasmacytic lymphoma and gastric cancer. | [62, 63] |
| Temsirolimus CCI-779 Torisel |
Rapalogue | FDA approved for advanced stage renal cell carcinoma. Multiple active, recruiting, and completed trials. | [62, 63] |
| Ridaforolimus AP23573 MK-8669 Deforolimus |
Rapalogue | Multiple active, recruiting, and completed trials for various cancers. | [64] |
| Zotarolimus ABT-578 |
Rapalogue | FDA approved for use in cardiac stents to prevent restenosis following angioplasty. Multiple active and completed trials. | [65, 66] |
| AZD8055 | ATP-competitive mTOR inhibitor | In clinical trials for gliomas, liver cancer, and solid tumors. | [67–70] |
| AZD2014 | ATP-competitive mTOR inhibitor | Clinical trials recruiting for metastatic breast and renal cancers. | [67] |
| OSI-027 | ATP-competitive mTOR inhibitor | Completed phase 1 clinical trial in patients with advanced solid tumors or lymphoma. | [71, 72] |
| MLN0128 | ATP-competitive mTOR inhibitor | Completed and recruiting phase 1 trials for multiple myeloma and advanced malignancies. | [72] |
| WYE-132 | ATP-competitive mTOR inhibitor | None. | [73] |
| Torin1 | ATP-competitive mTOR inhibitor | None. | [74] |
| PI-103 | PI3K/mTOR inhibitor | None. | [75] |
| P7170 | PI3K/mTOR inhibitor | Phase 1 clinical trial recruiting for advanced refractory solid tumors. | [76] |
| PF-04691502 | PI3K/mTOR inhibitor | Phase 1 trials completed and recruiting; phase 2 trial for recurrent endometrial cancer recruiting. | [77] |
| PF-05212384 PKI-587 |
PI3K/mTOR inhibitor | Phase 1 clinical trials recruiting for advanced cancers; phase 2 trial for recurrent endometrial cancer recruiting. | [78, 79] |
| GNE477 | PI3K/mTOR inhibitor | None. | |
| PKI-179 | PI3K/mTOR inhibitor | Phase 1 clinical trial terminated. | [80] |
| WJD008 | PI3K/mTOR inhibitor | None. | |
| XL765 SAR245409 |
PI3K/mTOR inhibitor | Several phase 1 trials completed for solid tumors, breast cancer, malignant gliomas, and recurrent glioblastomas. | [81] |
| NVP-BEZ235 | PI3K/mTOR inhibitor | Multiple phase 1 trials completed. Phase 1/2 trials active, ongoing, or recruiting for various cancers. | [82, 83] |
| BGT226 | Phase 1 and phase 1/2 trials completed for solid tumors and breast cancer. | [84, 85] | |
| SF1126 | Phase 1 trial completed for solid tumors. | [86] | |
| GSK2126458 | PI3K/mTOR inhibitor | Active and recruiting phase 1 trials for solid tumors. | [72, 83] |
Current clinical trials information from clinical trials.gov on September 12, 2013. 1507 studies returned for “rapamycin,” “everolimus,” “sirolimus,” or “temsirolimus.” “None” means no hits returned.