Investigation of novel circulating proteins, germ line single-nucleotide polymorphisms, and molecular tumor markers as potential efficacy biomarkers of first-line sunitinib therapy for advanced renal cell carcinoma

Cancer Chemother Pharmacol. 2014 Oct;74(4):739-50. doi: 10.1007/s00280-014-2539-0. Epub 2014 Aug 7.

Abstract

Purpose: Sunitinib is a first-line advanced renal cell carcinoma (RCC) standard of care. In a randomized phase II trial comparing sunitinib treatment schedules, separate exploratory biomarker analyses investigated the correlations of efficacy with selected serum, germ line single-nucleotide polymorphism (SNP), or tumor markers.

Methods: Advanced RCC patients received first-line sunitinib 50 mg/day on the approved 4-week-on-2-week-off schedule (n = 146) or 37.5 mg/day continuous dosing (n = 146). The following correlation analyses were performed: (1) response evaluation criteria in solid tumors-defined tumor response with serum soluble protein levels via two distinct multiplex (n < 1,000) platforms; (2) response and time-to-event outcomes with germ line SNPs in vascular endothelial growth factor (VEGF)-A and VEGF receptor (VEGFR)3 genes; and (3) response and time-to-event outcomes with tumor immunohistochemistry status for hypoxia-inducible factor 1-alpha (HIF-1α) and carbonic anhydrase-IX or tumor Von Hippel-Lindau (VHL) gene inactivation status.

Results: Lower baseline angiopoietin-2 (Ang-2) and higher baseline matrix metalloproteinase-2 (MMP-2) levels were identified by both platforms as statistically significantly associated with tumor response. There were no significant correlations between VEGF-A or VEGFR3 SNPs and outcomes. Progression-free survival was longer for HIF-1α percent of tumor expression groups 0-2 (HIF-1α low) versus 3-4 (HIF-1α high; p = 0.034). There were no significant correlations between outcomes and each VHL inactivation mechanism [mutation (86% of VHL-inactive patients), methylation (14%), and large deletion (7%)] or mechanisms combined.

Conclusions: Serum Ang-2 and MMP-2 and tumor HIF-1α were identified as relevant baseline biomarkers of sunitinib activity in advanced RCC, warranting further research into their prognostic versus predictive value.

Trial registration: ClinicalTrials.gov NCT00267748.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Angiogenesis Inhibitors / administration & dosage
  • Angiogenesis Inhibitors / adverse effects
  • Angiogenesis Inhibitors / pharmacokinetics
  • Angiopoietin-2 / blood*
  • Antigens, Neoplasm / blood
  • Antigens, Neoplasm / genetics
  • Biomarkers, Tumor / blood
  • Biomarkers, Tumor / genetics
  • Carbonic Anhydrase IX
  • Carbonic Anhydrases / blood
  • Carbonic Anhydrases / genetics
  • Carcinoma, Renal Cell* / drug therapy
  • Carcinoma, Renal Cell* / genetics
  • Carcinoma, Renal Cell* / metabolism
  • Carcinoma, Renal Cell* / pathology
  • Disease-Free Survival
  • Drug Administration Schedule
  • Drug Monitoring / methods
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / blood
  • Hypoxia-Inducible Factor 1, alpha Subunit / genetics
  • Indoles* / administration & dosage
  • Indoles* / adverse effects
  • Indoles* / pharmacokinetics
  • Kidney Neoplasms* / drug therapy
  • Kidney Neoplasms* / genetics
  • Kidney Neoplasms* / metabolism
  • Kidney Neoplasms* / pathology
  • Male
  • Matrix Metalloproteinase 2 / blood*
  • Polymorphism, Single Nucleotide
  • Prognosis
  • Pyrroles* / administration & dosage
  • Pyrroles* / adverse effects
  • Pyrroles* / pharmacokinetics
  • Sunitinib
  • Treatment Outcome
  • Vascular Endothelial Growth Factor A / genetics*
  • Vascular Endothelial Growth Factor Receptor-3 / genetics*
  • Von Hippel-Lindau Tumor Suppressor Protein* / blood
  • Von Hippel-Lindau Tumor Suppressor Protein* / genetics

Substances

  • Angiogenesis Inhibitors
  • Angiopoietin-2
  • Antigens, Neoplasm
  • Biomarkers, Tumor
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Indoles
  • Pyrroles
  • Vascular Endothelial Growth Factor A
  • Von Hippel-Lindau Tumor Suppressor Protein
  • Vascular Endothelial Growth Factor Receptor-3
  • Matrix Metalloproteinase 2
  • CA9 protein, human
  • Carbonic Anhydrase IX
  • Carbonic Anhydrases
  • Sunitinib

Associated data

  • ClinicalTrials.gov/NCT00267748