Serum C-Telopeptide Collagen Crosslinks and Plasma Soluble VEGFR2 as Pharmacodynamic Biomarkers in a Trial of Sequentially Administered Sunitinib and Cilengitide

Clin Cancer Res. 2015 Nov 15;21(22):5092-9. doi: 10.1158/1078-0432.CCR-15-0427. Epub 2015 Jul 21.

Abstract

Purpose: Fit-for-purpose pharmacodynamic biomarkers could expedite development of combination antiangiogenic regimens. Plasma sVEGFR2 concentrations ([sVEGFR2]) mark sunitinib effects on the systemic vasculature. We hypothesized that cilengitide would impair microvasculature recovery during sunitinib withdrawal and could be detected through changes in [sVEGFR2].

Experimental design: Advanced solid tumor patients received 50 mg sunitinib daily for 14 days. For the next 14 days, patients were randomized to arm A (cilengitide 2,000 mg administered intravenously twice weekly) or arm B (no treatment). The primary endpoint was change in [sVEGFR2] between days 14 and 28. A candidate pharmacodynamic biomarker of cilengitide inhibition of integrin αvβ3, serum c-telopeptide collagen crosslinks (CTx), was also measured.

Results: Of 21 patients, 14 (7 per arm) received all treatments without interruption and had all blood samples available for analysis. The mean change and SD of [sVEGFR2] for all sunitinib-treated patients was consistent with previous data. There was no significant difference in the mean change in [sVEGFR2] from days 14 to 28 between the arms [arm A: 2.8 ng/mL; 95% confidence interval (CI), 2.1-3.6 vs. arm B: 2.0 ng/mL; 95% CI, 0.72-3.4; P = 0.22, 2-sample t test]. Additional analyses suggested (i) prior bevacizumab therapy to be associated with unusually low baseline [sVEGFR2] and (ii) sunitinib causes measurable changes in CTx.

Conclusions: Cilengitide had no measurable effects on any circulating biomarkers. Sunitinib caused measurable declines in serum CTx. The properties of [sVEGFR2] and CTx observed in this study inform the design of future combination antiangiogenic therapy trials.

Publication types

  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Angiogenesis Inhibitors / administration & dosage
  • Angiogenesis Inhibitors / pharmacokinetics
  • Biomarkers, Tumor / blood*
  • Biomarkers, Tumor / pharmacokinetics
  • Collagen Type I / blood*
  • Collagen Type I / pharmacokinetics
  • Female
  • Humans
  • Indoles / administration & dosage
  • Indoles / pharmacokinetics
  • Male
  • Middle Aged
  • Neoplasm Staging
  • Neoplasms / blood
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / pathology
  • Neovascularization, Pathologic / blood
  • Neovascularization, Pathologic / drug therapy*
  • Neovascularization, Pathologic / genetics
  • Neovascularization, Pathologic / pathology
  • Peptides / blood*
  • Peptides / pharmacokinetics
  • Pyrroles / administration & dosage
  • Pyrroles / pharmacokinetics
  • Snake Venoms / administration & dosage
  • Snake Venoms / pharmacokinetics
  • Sunitinib
  • Vascular Endothelial Growth Factor Receptor-2 / blood*
  • Vascular Endothelial Growth Factor Receptor-2 / genetics

Substances

  • Angiogenesis Inhibitors
  • Biomarkers, Tumor
  • Collagen Type I
  • Indoles
  • Peptides
  • Pyrroles
  • Snake Venoms
  • collagen type I trimeric cross-linked peptide
  • Cilengitide
  • KDR protein, human
  • Vascular Endothelial Growth Factor Receptor-2
  • Sunitinib