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. 2009 Dec 15;102(1):8–18. doi: 10.1038/sj.bjc.6605483

Table 2b. VEGF RTKi and soluble biomarkers.

References Drug, disease and trial Biomarkers N Drug-induced changes Prognostic and predictive values
Rini et al (2008a) Sunitinib Bevacizumab refractory RCC Phase 2 VEGF-A, VEGF-C, sVEGFR-3 PlGF 61 ↑VEGF-A and PlGF ↓VEGF-C and sVEGFR-3 Low baseline VEGF-C (P=0.0006) and VEGF–R-3 (P=0.006) associated with longer PFS and ORR
Burstein et al (2008) Sunitinib Metastatic breast cancer VEGF, sVEGFR-2, sVEGFR-3, sKIT 64 ↑VEGF, ↓VEGFR-2, VEGFR-3 ↓VEGFR-3 and ↑OS (P=0.07) ↓sKIT and ↑TTP and ↑OS (P=0.0194)
Bello et al (2006) Sunitinib Neuroendocrine tumour VEGF, IL-8, sVEGFR-2, sVEGFR-3 109 ↑VEGF ↓VEGFR-2, ↓sVEGFR-3 ↓VEGFR-3 with PR (n=11) ↑Il-8 with decreased tumour size
Norden-Zfoni et al (2007) Sunitinib (SU11248) Imatinib-resistant GIST Phase1/2 VEGF, sVEGFR-2 73 ↑VEGF ↓sVEGFR-2 NS
Azad et al (2008) Sorafenib+Bevacizumab Advanced cancer Phase 1 VEGF IL-6 IL-8 28 ↑VEGF No change: IL-6, IL-8 NS
Batchelor et al (2007) Cediranib (AZD2171) Glioblastoma Phase 2 VEGF, PlGF, sVEGFR-1, sVEGFR-2, FGF-2, SDF-1α, 16 ↑VEGF, ↑PlGF ↓sVEGFR-2 PD-associated variables: ↓PlGF, ↑sVEGFR2, ↑bFGF, ↑SDF-1α
Drevs et al (2007) Cediranib (AZD2171) Advanced cancer Phase 1 sVEGFR-1 sVEGFR-2 FGF-2, PlGF,Tie-2, E-selectin, IL- 8 83 ↓sVEGFR-2 ↑VEGF, ↑PlGF NS
Rosen et al (2007) AMG 706 Advanced cancer Phase 1 PlGF, VEGF, FGF-2, sVEGFR-1 71 ↑PlGF ↓sVEGFR-2 ↑PlGF (P=0.003) and ↓VEGFR-2 (P=0.001) associated with change in tumour size
Jonker et al (2007) Brivanib (BMS-582664) Advanced cancer; Phase 1 sVEGFR-2, Collagen IV 50 ↓sVEGFR-2 ↓collagen IV NS
Heymach et al (2008) Vandetanib (AZD6474) NSCLC: 3; Phase 2 trials VEGF 251 NS Low baseline VEGF: low risk of disease progression
Kiura et al (2008) Vandetanib (AZD6474) NSCLC; Phase 2 VEGF, sVEGFR-2, Tie-2 53 ↑VEGF ↓sVEGFR-2 Low baseline VEGF and TTP Low baseline VEGF in patients with PR
Yamada et al (2008) E7080 Advanced cancer; Phase 1 VEGF, FGF-2 PDGF 24 ↑VEGF NS
Drevs et al (2005) Vatalanib (PTK/ZK) Advanced cancer, liver mets; Phase1/2 VEGF, FGF-2, sTie-2, and E-selectin 30 ↑VEGF, FGF-2 Change in VEGF correlates with outcome (P=0.027)
Heymach et al (2004) Semaxinib (SU5416) Soft tissue sarcoma Phase 2 Urine VEGF Urine FGF-2 13 ↑VEGF, FGF-2 High baseline VEGF associated with ↓OS (P=0.04)
Lara et al (2003) IFNα+Semaxinib (SU5416) RCC; Phase 2 VEGF PAI-1 25 ↓VEGF, ↓PAI-1 ↓PAI-1 levels in patients with SD ↓baseline VEGF in pts with PD
Stopeck et al (2002) Semaxinib (SU5416) Advanced cancer; Phase 1 Urine VEGF Urine FGF-2 22 ↑Urine VEGF ↑Urine FGF-2 ↑Urine VEGF in responders (P<0.05)
Fury et al (2007) Semaxinib (SU5416) Head and neck cancer; Phase 2 VEGF 35 ↑VEGF NS
Peterson et al (2004) Semaxinib (SU5416) Melanoma; Phase 2 VEGF 13 ↑VEGF NS
Stadler et al (2004) Semaxinib (SU5416) Homone refractory prostate cancer; Phase 2 VEGF bFGF 22 NA NS
Norden-Zfoni et al (2007) Sunitinib (SU11248) Imatin-resistant GIST Phase1/2 CEC PBMC 90 ↑CECs ↓PBMC Significant clinical correlation (P=0.03)
Batchelor et al (2007) Cediranib (AZD2171) Glioblastoma Phase 2 CEC CEPCs 16 ↓CEC ↓CEPC ↑CECs with tumour progression. ↑CEPCs with relapse after drug holidays

Abbreviations: VEGF=vascular endothelial growth factor; RTKi=receptor tyrosine kinase inhibitor; CEC=circulating endothelial cell; CEPC=circulating endothelial progenitor cell; FGF-2=fibroblast growth factor-2; GIST=gastrointestinal stromal tumour; HGF=hepatocyte growth factor; RCC=renal cell carcinoma; NA=not applicable; NS=not significant; NSCLC=non-small-cell lung cancer; OR=overall response; ORR=objective response rate; OS=overall survival; PAI-1=plasminogen activator inhibitor-1; PBMC=peripheral blood mononuclear cells; PD=progressive disease; PDGF=platelet-derived growth factor; PFS=progression-free survival PlGF=placental growth factor; PR=partial response; RR=response rate; SD=stable disease; SDF-1=stromal-cell derived factor-1; sVEGFR=soluble VEGF receptor; TTP=time to progression.