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. Author manuscript; available in PMC: 2016 Mar 14.
Published in final edited form as: Oncologist. 2009 Jun 1;14(6):621–636. doi: 10.1634/theoncologist.2008-0272

Table 1.

Selected antiangiogenic agents currently in clinical trials for adult malignant glioma

Agent Target(s) Mechanism Tumor type(s) Phase Combinations
VEGF inhibitors
  Aflibercept VEGF-A, VEGF-B, PlGF Decoy receptor New GBM, recurrent or stable MG I TMZ and RT
Recurrent MG II
  Bevacizumab VEGF-A Monoclonal antibody New GBM, recurrent MG II/III Various combinationsa
VEGF receptor inhibitors
  AEE788 VEGFR-1/VEGFR-2, EGFR Tyrosine kinase inhibitor Recurrent GBM I/II
Recurrent GBM I/II Everolimus
  Cediranib VEGFR-1 to VEGFR-3, PDGFR-β, c-Kit Tyrosine kinase inhibitor New GBM I/II TMZ and RT
Recurrent GBM III Versus lomustine (randomized)
III
  CT-322 VEGFR-1 to VEGFR-3 Fibronectin (adnectin)-based inhibitor Recurrent GBM II Alone and with irinotecan
  Pazopanib (GW786034) VEGFR-1 to VEGFR-3, PDGFR-β, c-Kit Tyrosine kinase inhibitor Recurrent GBM II
Recurrent MG II Lapatinib
  Sorafenib VEGFR-2, VEGFR-3, BRAF, PDGFR-β, c-Kit, Ras, p38α Tyrosine kinase inhibitor New GBM, recurrent GBM I/II Various combinationsb
  Sunitinib VEGFR-2, PDGFR-β, Flt3, c-Kit Tyrosine kinase inhibitor Recurrent MG I Irinotecan
Recurrent MG II
  Vandetanib (ZD6474, Zactima®) VEGFR-2, EGFR, RET Tyrosine kinase inhibitor New GBM I/II TMZ and RT
Recurrent MG I Imatinib and hydroxyurea
Recurrent glioma I/II
  Vatalanib (PTK787) VEGFR-1 to VEGFR-3, PDGFR-β, c-Kit Tyrosine kinase inhibitor New GBM I TMZ and RT in patients taking EIAEDs
New GBM I/II TMZ and RT with or without vatalanib (randomized)
Recurrent MG I Imatinib and hydroxyurea
  XL184 VEGFR-2, Met, RET, c-Kit, Flt3, Tie-2 Tyrosine kinase inhibitor Recurrent GBM II
Alternative angiogenesis pathway inhibitors
  ABT-510 CD36 receptor Thrombospondin-1 mimetic peptide New GBM I TMZ and RT
  AMG102 HGF/SF Monoclonal antibody Recurrent GBM II
  Dasatinib PDGFR-β, Src, BCR-ABL, c-Kit, EphA2 Tyrosine kinase inhibitor Recurrent MG I Erlotinib
Recurrent GBM II
  Imatinib PDGFR-β, BCR-ABL, c-Kit Tyrosine kinase inhibitor Recurrent MG I Everolimus and hydroxyurea
Stable or recurrent MG I TMZ
  Tandutinib (MLN518) PDGFR-β, Flt3, c-Kit Tyrosine kinase inhibitor Recurrent GBM I/II
Recurrent MG II Bevacizumab
  Celecoxib COX-2 Suppress VEGF and FGF GBM following RT II Multiarm study with permutations of celecoxib, thalidomide, and isotretinoin
Recurrent MG II 6-Thioguanine and capecitabine with either TMZ or lomustine
  Panzem® (2ME2) HIF-1α Disrupt tumor microtubules and suppress HIF-1α Recurrent GBM II Protracted TMZ schedule
Recurrent GBM II
  Metronomic TMZ Endothelial cells, EPCs Induce apoptosis, inhibit recruitment of EPCs New GBM II Gliadel® wafer, TMZ, and radiotherapy followed by metronomic TMZ
GBM following RT II With retinoic acid versus standard adjuvant TMZ with retinoic acid
Recurrent MG II Bevacizumab
Endothelial cell migration inhibitors
  ATN-161 Integrin α5β1 Fibronectin-derived PHSRN peptide Recurrent MG I/II Carboplatin
  Cilengitide Integrins ανβ3 and ανβ5 RGD synthetic peptide New GBM I/II TMZ and RT
New GBM III TMZ and RT
Recurrent MG I/II Monotherapy (several trials)
a

Bevacizumab is being combined in various phase II trials with TMZ and radiotherapy as well as TMZ, radiotherapy, and irinotecan for newly diagnosed GBM patients; with TMZ and erlotinib for stable GBM following radiotherapy; and with bortezomib, enzastaurin, erlotinib, etoposide, irinotecan, sorafenib, tandutinib, or metronomic TMZ for recurrent MG or GBM.

b

Sorafenib is being combined in various phase I and II trials with TMZ and radiotherapy for newly diagnosed GBM and with lapatinib, erlotinib, tipifarnib, temsirolimus, bevacizumab, or a protracted schedule of TMZ for recurrent GBM.

Abbreviations: COX-2, cyclo-oxygenase 2; EGFR, epithelial growth factor receptor; EIAEDs, enzyme-inducing antiepileptic drugs; EPC, endothelial progenitor cell; FGF, fibroblast growth factor; GBM, glioblastoma; HGF/SF, hepatocyte growth factor/scatter factor; HIF-1α, hypoxia inducible factor 1α; MG, malignant glioma; PDGFR, platelet-derived growth factor; PlGF, placental growth factor; RA, retinoic acid; RT, radiotherapy; TMZ, temozolomide; VEGF, vascular endothelial growth factor.