Table 2.
Presumed anti-angiogenic agents currently in clinical trialsa
| Category | Drug name | Target/mechanism | Current clinical trialsa |
|
|---|---|---|---|---|
| Phase (no.) |
Cancers in trials | |||
| Target angiogenic factor | Volociximab (M200) |
Anti-α5β1 integrin monoclonal antibody |
II | Melanoma |
| Aflibercept (VEGF TrapR1/R2) |
VEGF decoy receptor | II, III | Ovary, lung | |
| PI-88 | Mimics Heparan Sulfate, inhibits heparanase, binds FGF and VEGF |
II | Prostate | |
| PTC299 | VEGF 5′-UTR mRNA | I | Breast | |
| Ad-hIFN-β (BG00001) |
IFN-β gene, adenovirus vector | II | CNS, CRC, mesothelioma | |
| Target angiogenic signal: tyrosine kinase inhibitors |
Cediranib (AZD2171) |
VEGF | I, II, III |
CRC, solid tumors, lymphoma |
| Nilotinib (AMN107) |
KIT, PDGFR, and Bcr-Abl | III | GIST | |
| Vatalanib (PTK787/ZK 222584) |
VEGF | I, II, III |
CRC, MM, metastatic tumors | |
| AMG 706 | VEGF, PDGF, c-kit, Ret | II, III | Breast, NSCLC | |
| Pazopanib (GW786034) |
VEGFR, c-kit, PDGF-R | II, III | RCC | |
| Axitinib (AG- 013736) |
VEGFR-1, -2, PDGF-βR | I, II | Lung, thyroid, CRC, melanoma, kidney, pancreas |
|
| Semaxanib (SU5416) |
Flk-1/KDR | I, II | Fallopian tube, breast, H & N, sarcoma, melanoma, kidney |
|
| AG-6013736 | VEGFR, PDGFR | II | Thyroid | |
| Brivanib (BMS- 582664) |
VEGFR, FGFR | II | HCC | |
| ABT-869 | VEGFR, PDGFR | II | RCC | |
| Dasatinib (BMS- 354825) |
bcr/abl | I | Solid tumors | |
| Vandetanib (ZD 6474) |
VEGFR, EGFR | I-III | Numerous | |
| RAF265 | Raf, VEGFR-2 | I | Metastatic melanoma | |
| Target endothelial cells | TNP-470 | Fumagillin analogue, binds MetAP2 causing EC arrest in G1 phase |
I, II | Pancreas, Kaposi’s sarcoma |
| Squalamine lactate | Intracellular blockage of numerous pathways |
II | Prostate, ovarian | |
| Recombinant tPA | Induces Angiostatin | II | Solid tumors | |
| Ad-rhEndo (E10A) | Endostatin gene transfer | I | Advanced Solid tumor | |
| ABT-510 | Thrombospondin Analogue: inhibits VEGF, bFGF, HGF, IL-8 |
I | Solid tumors | |
| Col-3 | MMP inhibitor | I | Metastatic cancer | |
| 2-methoxyestradiol (Panzem) |
Estradiol Metabolite | I, II | RCC, carcinoid, solid tumors | |
| Combretastatin A4 Phosphate |
Tubulin | I | Solid tumors | |
| Bavituximab | Aminophospholipids monoclonal antibody |
I | Solid tumors | |
| Other agents with anti- angiogenic properties |
AMG 386 | Angiopoietins | II | Breast |
| Tetrathiomolybdate | Copper Chelator | II | Breast, prostate, CRC, HCC, esophageal |
|
| Celecoxib | COX-2 inhibitor | I-III | MM, head and neck, CRC, leukemia, lymphoma |
|
mCRC Metastatic colorectal cancer, NSCLC non-small cell lung cancer, H & N head and neck cancer, CML chronic myelogenous leukemia, GIST gastrointestinal stromal tumor, RCC renal cell carcinoma, MM multiple myeloma, NHL Non-Hodgkin’s lymphoma