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. 2019 Jan 2;8(1):18. doi: 10.3390/cells8010018

Table 2.

Pharmacological use of different mTOR inhibitor classes. The table displays the characteristics of the corresponding inhibitor family and lists important examples.

First Generation
Target: TORC1 (binding to FKBP1)
Examples:

  • Sirolimus (prophylaxis organ rejection)

  • Temsirolimus (renal cell carcinoma)

  • Everolimus (renal cell carcinoma)

Status:

  • FDA/EMEA approved for certain applications

Second Generation
Targets: TORC1,TORC2,PI3K (bind kinase domain)
Examples:

  • NVP-BEZ235 (PI3K/TORC1/TORC2)

  • PF-04691502 (PI3K/mTOR)

  • OSI-027 (TORC1/TORC2)

Status:

  • Different preclinical and clinical stages

Third Generation
Targets: TORC1,TORC2
(bivalent binding to FRB domain and kinase domain)
Example:

  • RapaLink-1

(rapamycin-FRB-binding compound linked to TORKi)
Status:
Preclinical research