TABLE 1.
Combinatorial effects of phosphatidylinositol 3-kinase (PI3K) + ERBB inhibitors in head and neck squamous cell carcinoma (HNSCC) cell lines
Combinatorial effects of PI3Kα inhibitor HS-173 and reversible or irreversible ERBB-targeting agents in HSC-2 and Detroit 562 HNSCC cell lines. Synergy was assessed using Combenefit software (Di Veroli et al., 2016). Synergy was not observed for PI3Kα inhibitor HS-173 with any reversible inhibitor in either cell line. Four of four and three of four irreversible EGFR inhibitors were synergistic with HS-173 in HSC-2 and Detroit 562 cells, respectively.
| Inhibitor | Target | Reversible/Irreversible | HSC-2 Synergy | Detroit 562 Synergy |
|---|---|---|---|---|
| Gefitinib | EGFR | Reversible | No | No |
| Erlotinib | EGFR | Reversible | No | No |
| BMS-599626 | EGFR/ERBB2 | Reversible | No | No |
| CP-724714 | ERBB2 | Reversible | No | No |
| Afatinib | EGFR/ERBB2 | Irreversible | Yes | Yes |
| TAK-285 | EGFR/ERBB2 | Irreversible | Yes | No |
| CUDC-101 | EGFR/ERBB2/HDAC | Irreversible | Yes | Yes |
| Dacomitinib | EGFR/ERBB2/ERBB4 | Irreversible | Yes | Yes |