Cytostatic Agents Licensed or Currently Under Clinical Development
| Agent | Target of action | Clinical phase |
|---|---|---|
| Antiangiogenic agents | ||
| Bevacizumab | VEGF | Licensed |
| Vatalanib | VEGFR-1, VEGFR-2 | Phase III |
| Vandetanib | VEGFR-1, VEGFR-2, VEGFR-3, EGFR | Phase III |
| AGO13736 | VEGFR-1, VEGFR-2 | Phase II |
| Sunitinib | VEGFR, PDGFR, c-KIT, FLT3 | Licensed |
| Marimastat | MMP-1, MMP-2, MMP-3, MMP-7, MMP-9 | Phase III |
| Prinomastat | MMP-2, MMP-9 | Phase III |
| BMS 275291 | MMP-1, MMP-2, MMP-8, MMP-9, MMP-13, MMP-14 | Phase III |
| Endostatin | Capillary endothelial cells | Phase IV |
| EGFR/HER2 targets | ||
| Gefitinib | EGFR | Licensed |
| Erlotinib | EGFR | Licensed |
| Lapatinib | EGFR/HER2 | Licensed |
| Cetuximab | EGFR | Licensed |
| Panitumumab | EGFR | Phase III |
| Trastuzumab | HER2 | Licensed |
| Matuzumab | EGFR | Phase II |
| ABL and SRC targets | ||
| Imatinib mesylate | BCR-ABL, c-KIT | Licensed |
| Dasatinib | BCR-ABL, c-SRC | Phase III |
| Farnesyltransferase inhibitors | ||
| Tipifarnib | CAAX | Phase III |
| Lonafarnib | CAAX | Phase II |
| Proteasome inhibitor | ||
| Bortezomib | 26S proteasome | Licensed |
| ERK inhibitors | ||
| Sorafenib | Raf-1 kinase, BRAF, VEGFR-2, VEGFR-3, c-KIT, PDGFR-β | Licensed |
| PD184352 | MEK1/2 | Phase II |
| CGP69846A | c-RAF | Phase II |
| mTOR inhibitors | ||
| Temsirolimus | mTOR | Phase III |
| Deforolimus | mTOR | Phase III |
| Everolimus | mTOR | Phase III |
| Estrogen blockers | ||
| Tamoxifen | ER | Licensed |
| Fulvestrant | ER | Licensed |
VEGFR = vascular endothelial growth factor receptor; PDGFR = platelet-derived growth factor receptor; FLT3 = Fms-related tyrosine kinase 3; MMP = matrix metalloproteinase; CAAX = carboxy terminal tetrapeptide motif of protein (c = cysteine, A = aliphatic amino acid, X = terminal amino acid); ERK = extracellular regulated kinase; MEK = mitogenic extracellular kinase.