Sunitinib Treatment Exacerbates Intratumoral Heterogeneity in Metastatic Renal Cancer

Clin Cancer Res. 2015 Sep 15;21(18):4212-23. doi: 10.1158/1078-0432.CCR-15-0207. Epub 2015 May 26.

Abstract

Purpose: The aim of this study was to investigate the effect of VEGF-targeted therapy (sunitinib) on molecular intratumoral heterogeneity (ITH) in metastatic clear cell renal cancer (mccRCC).

Experimental design: Multiple tumor samples (n = 187 samples) were taken from the primary renal tumors of patients with mccRCC who were sunitinib treated (n = 23, SuMR clinical trial) or untreated (n = 23, SCOTRRCC study). ITH of pathologic grade, DNA (aCGH), mRNA (Illumina Beadarray) and candidate proteins (reverse phase protein array) were evaluated using unsupervised and supervised analyses (driver mutations, hypoxia, and stromal-related genes). ITH was analyzed using intratumoral protein variance distributions and distribution of individual patient aCGH and gene-expression clustering.

Results: Tumor grade heterogeneity was greater in treated compared with untreated tumors (P = 0.002). In unsupervised analysis, sunitinib therapy was not associated with increased ITH in DNA or mRNA. However, there was an increase in ITH for the driver mutation gene signature (DNA and mRNA) as well as increasing variability of protein expression with treatment (P < 0.05). Despite this variability, significant chromosomal and transcript changes to key targets of sunitinib, such as VHL, PBRM1, and CAIX, occurred in the treated samples.

Conclusions: These findings suggest that sunitinib treatment has significant effects on the expression and ITH of key tumor and treatment specific genes/proteins in mccRCC. The results, based on primary tumor analysis, do not support the hypothesis that resistant clones are selected and predominate following targeted therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Antineoplastic Agents / therapeutic use
  • Biomarkers / metabolism
  • Carcinoma, Renal Cell / drug therapy
  • Carcinoma, Renal Cell / pathology*
  • Clinical Trials, Phase II as Topic
  • Cluster Analysis
  • Comparative Genomic Hybridization
  • DNA-Binding Proteins
  • Drug Design
  • Female
  • Gene Expression Profiling
  • Genotype
  • Humans
  • Hypoxia
  • Indoles / pharmacology*
  • Kidney Neoplasms / drug therapy
  • Kidney Neoplasms / pathology*
  • Male
  • Middle Aged
  • Mutation
  • Neoplasm Metastasis
  • Nephrectomy
  • Nuclear Proteins / metabolism
  • Pilot Projects
  • Protein Array Analysis
  • Protein Kinase Inhibitors / pharmacology*
  • Pyrroles / pharmacology*
  • RNA, Messenger / metabolism
  • Sunitinib
  • Transcription Factors / metabolism
  • Von Hippel-Lindau Tumor Suppressor Protein / genetics
  • Von Hippel-Lindau Tumor Suppressor Protein / metabolism

Substances

  • Antineoplastic Agents
  • Biomarkers
  • DNA-Binding Proteins
  • Indoles
  • Nuclear Proteins
  • PBRM1 protein, human
  • Protein Kinase Inhibitors
  • Pyrroles
  • RNA, Messenger
  • Transcription Factors
  • Von Hippel-Lindau Tumor Suppressor Protein
  • VHL protein, human
  • Sunitinib