Table 1.
Antiangiogenic RTKIs agents under clinical trials investigation in mCRC.
| Drugs | Target | Number of participants | Setting | Treatment | Primary outcome measures | Phase | Identifiers |
|---|---|---|---|---|---|---|---|
| Vatalanib (PTK787/ZK 222584) | VEGFR1-3, FGFR1-3, PDGFRα-β | 1168 | 1st line mCRC | Oxaliplatin/5FU/Leucovorin ± vatalanib | PFS | III | NCT00056459 |
| 855 | 2nd line mCRC | OS | NCT00056446 | ||||
| Nintedanib (BIBF1120) | VEGFR1-3, FGFR1-3, PDGFRα-β | 768 | Refractory mCRC | BSC ± Nintedanib | PFS/OS | III | NCT02149108 |
| 54 | Refractory mCRC | mFOLFOX6 ± Nintedanib | PFS | III | NCT01362361 | ||
| Semaxanib (SU5416) | VEGFR2 | 710 | 1st line mCRC | Leucovorin and Fluorouracil ± Semaxanib | OS | III | NCT00004252 |
| Brivanib | VEGFR2/FGFR1 | 750 | mCRC kRAS wild-type (refractory) | Cetuximab ± Brivanib | OS | III | NCT00640471 |
| Sunitinib | PDGFR-β, VEGFR2, | 768 | 1st line mCRC | FOLFIRI ± Sunitinib | PFS | III | NCT00457691 |
| Fruquintinib | VEGFR1-3 | 416 | 3rd line mCRC | Fruquintinib vs. placebo | OS | III | NCT02314819 |
| Cediranib (AZD2171) | VEGFR1-3 | 1814 | 1st line mCRC | Beva + folfox vs. beva + Cediranib | PFS | II/III | NCT00384176 |
| Sorafenib | VEGFR1-3 PDGFR-β BRAF | 101 | 2nd line mCRC | FOLFOX6/FOLFIRI ± Sorafenib | PFS | II | NCT00889343 |
| Vanucizumab | VEGF-A Angiopoietin-2 | 197 | 1st line mCRC | mFOLFOX6 + beva vs. mFOLFOX6 + Vancizumab | PFS | II | NCT02141295 |
| Famitinib | VEGFR2-3, c-Kit, PDGFR | 154 | 3rd line advanced mCRC | Famitinib vs. placebo | PFS | II | NCT01762293 |
| Axitinib | VEGFR1-3 | 70 | 1st line maintenance therapy | Axitinib alone after FOLFOX/beva in 1st line | PFS | II | NCT01490866 |
| Apatinib | VEGFR2 | 54 | Refractory mCRC progressed after 2nd line | Apatinib alone | PFS | II | NCT03190616 |
mCRC: metastatic colorectal cancer; 5FU: 5-fluorouracil; FOLFOX: oxaliplatin in combination with 5-fluorouracil and folinic acid; FOLFIRI: irinotecan in combination with 5-fluorouracil and folinic acid; BSC: best supportive care; Beva: bevacizumab; PFS: progression-free survival; OS: overall survival; VEGFR: vascular endothelial growth factor receptor; FGFR: fibroblast growth factor receptor; PDGFR: platelet-derived growth factor receptor.