Table 1: Some mTOR inhibitors used clinically and in research.

Chemical ClassClinical uses/trialsReferences

Rapamycin
Sirolimus
Rapamune
RapalogueFDA 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
RapalogueFDA 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
RapalogueFDA approved for advanced stage renal cell carcinoma. Multiple active, recruiting, and completed trials.[62, 63]
Ridaforolimus
AP23573
MK-8669
Deforolimus
RapalogueMultiple active, recruiting, and completed trials for various cancers.[64]
Zotarolimus
ABT-578
RapalogueFDA approved for use in cardiac stents to prevent restenosis following angioplasty. Multiple active and completed trials.[65, 66]
AZD8055ATP-competitive mTOR inhibitorIn clinical trials for gliomas, liver cancer, and solid tumors.[6770]
AZD2014ATP-competitive mTOR inhibitorClinical trials recruiting for metastatic breast and renal cancers.[67]
OSI-027ATP-competitive mTOR inhibitorCompleted phase 1 clinical trial in patients with advanced solid tumors or lymphoma. [71, 72]
MLN0128ATP-competitive mTOR inhibitorCompleted and recruiting phase 1 trials for multiple myeloma and advanced malignancies.[72]
WYE-132ATP-competitive mTOR inhibitorNone.[73]
Torin1ATP-competitive mTOR inhibitorNone.[74]
PI-103 PI3K/mTOR inhibitorNone.[75]
P7170PI3K/mTOR inhibitorPhase 1 clinical trial recruiting for advanced refractory solid tumors.[76]
PF-04691502PI3K/mTOR inhibitorPhase 1 trials completed and recruiting; phase 2 trial for recurrent endometrial cancer recruiting.[77]
PF-05212384
PKI-587
PI3K/mTOR inhibitorPhase 1 clinical trials recruiting for advanced cancers; phase 2 trial for recurrent endometrial cancer recruiting.[78, 79]
GNE477PI3K/mTOR inhibitorNone.
PKI-179PI3K/mTOR inhibitorPhase 1 clinical trial terminated.[80]
WJD008PI3K/mTOR inhibitorNone.
XL765
SAR245409
PI3K/mTOR inhibitorSeveral phase 1 trials completed for solid tumors, breast cancer, malignant gliomas, and recurrent glioblastomas.[81]
NVP-BEZ235PI3K/mTOR inhibitorMultiple phase 1 trials completed. Phase 1/2 trials active, ongoing, or recruiting for various cancers. [82, 83]
BGT226Phase 1 and phase 1/2 trials completed for solid tumors and breast cancer.[84, 85]
SF1126Phase 1 trial completed for solid tumors.[86]
GSK2126458PI3K/mTOR inhibitorActive 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.