Table 1:
Competitive environment table of the major tyrosine kinase inhibitors currently under development for HNSCC treatment.
| Drug | Target(s) | Developmental stage in HNSCC | FDA approved treatment | |
|---|---|---|---|---|
| EGFR targeting | Erlotinib* | EGFR (HER 1) | Phase III | EGFR-mutated NSCLC |
| Gefitinib* | EGFR (HER 1) | Phase III | EGFR-mutated NSCLC | |
| Lapatinib | EGFR and HER2 | Phase III | HER2-positve breast cancer | |
| Afatinib | EGFR, HER2 and HER4 | Phase III | EGFR-mutated NSCLC | |
| Poziotinib | EGFR, HER2 and HER4 | Phase II | NSCLC w/ S768 mutations | |
| Neratinib | EGFR, HER2 and HER4 | Preclinical | HER2-positive breast cancer | |
| Vandetanib | EGFR, VEGFR, and RET | Phase II | Medullary thyroid cancer | |
| VEGFR targeting | Sunitinib | VEGFR 1–3, PDGFR ⍺/β, FLT-3, c-KIT, RET and BRAF | Phase II | RCC |
| Sorafenib | VEGFR 1–3, PDGFRβ, FLT-3, c-KIT, RET and BRAF | Phase II | HCC, RCC, thyroid cancer | |
| Cediranib | VEGFR 1–3, PDGFR ⍺/β and c-KIT | Phase II | None | |
| Pazopanib | VEGFR 1–3, PDGFR ⍺/β and c-KIT | Phase II | RCC | |
| Nintedanib | VEGFR1–3, PDGFR and FGFR1–2 | Phase II | Idiopathic pulmonary fibrosis, NSCLC | |
| Axitinib | VEGFR 1–3, PDGFRβ and c-KIT | Phase II | RCC | |
| Lenvatinib | VEGFR 1–3, FGFR 1–4, PDGFR ⍺, c-KIT and RET | Phase I | HCC, thyroid cancer | |
| Motesanib | VEGFR 1–3 and c-KIT | Preclinical | None | |
| Fostamatinib | VEGFR, SYK, FLT3, aurora A kinase and RET | Phase II | Chronic immune thrombocytopenia | |
| Foretinib | VEGFR2 and c-MET | Phase II | None | |
| Bcr-Abl targeting | Imatinib | BCR-ABL, DDR, c-KIT, PDGFR and CSF-1R | Phase II | CML, Ph+ ALL, GIST and MDS |
| Dasatinib | BCR-ABL and SRC family | Phase II | CML and Ph+ ALL | |
| Nilotinib | BCR-ABL, PDGFRα and c-KIT | Phase I | Ph+ CML | |
| Ponatinib | BCR-ABL, VEGFR, PDGFR | Phase II | Ph+ ALL, CML |
: denotes single-target tyrosine kinase inhibitor; BCR-ABL: Breakpoint cluster region protein-Abelson murine leukemia viral oncogene homolog 1, BRAF: B-rapidly accelerated fibrosarcoma kinase, CML: Chronic myeloid leukemia, CSF-1R: Colony stimulating factor 1 receptor, DDR: Discoidin domain receptor, EGFR: Epidermal growth factor receptor, FGFR: Fibroblast growth factor receptor, FLT3: FMS-like tyrosine kinase 3, GIST: Gastrointestinal stromal tumors, HCC: Hepatocellular carcinoma, HER: Human epidermal growth factor receptor, KIT: Also called c-KIT tyrosine kinase, MDS: Myelodysplatic syndrome, NSCLC: Non-small cell lung cancer, PDGFR: Platelet derived growth factor receptor, Ph+ ALL: Philadelphia chromosome-positive acute lymphoblastic leukemia, Ph+ CML: Philadelphia chromosome-positive chronic myelogenous leukemia, RCC: Renal cell carcinoma, RET: Rearranged during transfection, SRC: Sarcoma-family kinase, SYK: Spleen tyrosine kinase, VEGFR: Vascular endothelial growth factor receptor