Table 3.
CSC-targeting approaches in HNSCC (selected).
| Therapeutic Target | Compound | Model System | Results | Reference |
|---|---|---|---|---|
| 5T4 (oncofetal antigen) | MEDI0641 | tissue microarray, HNSCC cells (UM-SCC-11B, UM-SCC-22B), patient-derived xenograft (PDX) model | Reduction of CSC fraction, tumor regression | [186] |
| Bmi1/AP-1 | PTC-209 | BmiCreER; RosatdTomato mice | cisplatin plus PTC-209 potently eradicates Bmi1+ CSCs and inhibits tumor progression | [80] |
| FGF | BGJ398 | HNSCC cell lines | decreased ALDHhighCD44high, sensitization to cisplatin | [189] |
| Porcupine (PORCN) (Wnt signaling) | LGK974 | HNSCC HN30 cell line | High response in HNSCC with Notch loss of function mutation | [190] |
| ALDH1 | Alda-89, Aldi-6 | HNSCC cells, xenograft model | Combination with cisplatin enhanced tumor cell death and reduced tumor growth | [188] |
| CD44 | Radionuclide 186Re-cmAb (U36) | Patients with Squamous Cell Carcinoma of the Head and Neck | Dose-limiting myelotoxicity, reduction in tumor size | [191] |
| CD44v6 | Anti-CD44v6 antibody BIWA- IRDye800CW and -Indium-111 | Fluorescence-guided surgery, locally invasive xenograft model | Detection of tumor regions and invasive zones | [192] |
| cMET/FZD8 | PF-2341066 | HNSCC patient-derived xenograft (PDX) | Reduced sphere formation, tumor initiation and metastatic spread | [187] |