Table 2.
Ongoing clinical trials of TKIs in patients with NETs.
| Therapeutic Regimen | Molecular Target(s) | Clinical Phase | Patient Population | Sample Size | Primary Outcome | Identifier |
|---|---|---|---|---|---|---|
| Cabozantinib | c-MET, VEGFR2, AXL, KIT, TIE2, FLT3, RET | III | Advanced progressive NETs | 395 | PFS | NCT03375320 |
| Axitinib + Octreotide LAR vs. Placebo + Octreotide LAR | VEGFR 1-3 | II/III | Advanced, progressive, G1/G2 NETs of extra-pancreatic origin | 255 | PFS | NCT01744249 |
| Lenvatinib + Everolimus | VEGFR 1-3, FGFR 1-4, IT, RET, PDGFR-alpha | II | Advanced progressive carcinoid tumors | 32 | ORR | NCT03950609 |
| Nintedanib | VEGFR 1-3, PDGFR-α and -β, FGFR 1-3, FLT3, SRC | II | Advanced, G1/G2 NETs of extra-pancreatic origin | 30 | PFS | NCT02399215 |
| Famitinib | c-KIT, VEGFR2-3, PDGFR, FLT1, FLT3 | II | Advanced, G1/G2 GEP-NETs | 53 | ORR | NCT01994213 |
| Regorafenib | VEGFR 1-3, PDGFRβ, KIT, RET, RAF-1 | II | Advanced, progressive carcinoid or panNET | 48 | PFS | NCT02259725 |
| Anlotinib | VEGFR2/3, FGFR1-4, PDGFR-α and -β, c-KIT, RET | II | G3 advanced GEP-NETs | 60 | PFS | NCT03457844 |
| Pazopanib + temozolomide | VEGFR 1-3, PDGFR-α and -β, c-KIT | I/II | Advanced panNETs | 29 | MTD | NCT01465659 |
| Evofosfamide (TH-302) + Sunitinib | DNA + VEGFR-1-3, PDGFR-α and -β, c-KIT, FLT-3, CSF1R | II | Advanced, G1/G2, treatment-naïve panNETs | 43 | ORR | NCT02402062 |
Abbreviations: AXL: AXL receptor tyrosine kinase; c-KIT: V-Kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; c-MET: MET proto-oncogene, receptor tyrosine kinase; CSF1R: colony stimulating factor 1 receptor; GEP: gastroenteropancreatic; FGFR: fibroblast growth factor receptor; FLT3: Fms related tyrosine kinase 3; MTD: maximum tolerated dose; NET: neuroendocrine tumor; ORR: objective response rate; panNET: pancreatic neuroendocrine tumor; PDGFR: platelet-derived growth factor receptor; PFS: progression-free survival; RAF: v-raf murine sarcoma viral oncogene homolog B1; RET: Ret proto-oncogene; SRC: SRC proto-oncogene, non-receptor tyrosine kinase; TIE2: tyrosine kinase with immunoglobulin and epidermal growth factor homology domains 2; VEGFR: vascular endothelial growth factor receptor.