Table 1.
Inhibitors of PI3K/AKT/mTOR signaling pathway as radiosensitizers for the treatment of HNSCC.
| Drug | Inhibitor | Mechanisms | Phase Ref. |
|---|---|---|---|
| Everolimus (RAD001) |
mTORC1 | Everolimus (RAD001) increased the radiosensitivity in SCC4 cells. | Phase I/II [13,35,45,46,47] (Afinitor®, Stein, Switzerland) |
| Vistusertib (AZD2014) |
mTORC1/m TORC2 inhibitor |
AZD2014 increased the irradiation-repressed cell viability of OSCC patient-derived cells and OSCS cell lines. |
Phase II (Vistusertib®, Netherlands) [39,48,49,50] |
| Buparlisib (BKM120) |
pan-PI3K inhibitor | BKM120 potently exhibited synergistic radiosensitization in OSCC cells. | Phase II [44,51,52,53] |
| Alpelisib (BYL719) |
PI3Kp110𝛼 inhibitor | The combination of BYL719 with irradiation significantly enhanced irradiation-induced regression in OSCC cells. |
Phase I [44,54,55,56,57] |
| Dactolisib (BEZ235) |
PI3K/mTOR dual inhibitor | BEZ235 exhibited statistically antitumor activity with irradiation against OML1-R xenografts. |
Phase I [33,58,59,60] |
| Ribociclib (LEE011) |
CDK4/6 inhibitor | LEE011 enhanced the cytotoxic effects of radiation therapy in HNSCC cells. | Phase II [43,61,62,63] |