In vivo RAF signal transduction as a potential biomarker for sorafenib efficacy in patients with neuroendocrine tumours

Br J Cancer. 2013 Apr 2;108(6):1298-305. doi: 10.1038/bjc.2013.64. Epub 2013 Feb 14.

Abstract

Background: Targeted therapies elicit anticancer activity by exerting pharmacodynamic effects on specific molecular targets. Currently, there is limited use of pharmacodynamic assessment to guide drug administration in the routine oncology setting.

Methods: We developed a phosphoshift (pShift) flow cytometry-based test that measures RAF signal transduction capacity in peripheral blood cells, and evaluated it in a phase II clinical trial of oral sorafenib plus low-dose cyclophosphamide in patients with advanced neuroendocrine tumours (NETs), in order to predict clinical course and/or guide individual dose-titration.

Results: Twenty-two patients were enrolled. Median progression-free survival (PFS) was 3 months (95% CI 2-10.7), and one patient had a partial response. PFS was longer among five patients who demonstrated an increase in pShift after 7 days of sorafenib compared with those who did not (14.9 months vs 2.8 months; P=0.047). However, pShift did not add value to toxicity-based dose-titration.

Conclusion: The pharmacodynamic assessment of RAF transduction may identify selected patients with advanced NETs most likely to benefit from the combination of sorafenib plus cyclophosphamide. Further investigation of this test as a potential biomarker is warranted.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Combined Chemotherapy Protocols / pharmacokinetics
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Biomarkers, Tumor / metabolism*
  • Cyclophosphamide / administration & dosage
  • Female
  • Flow Cytometry
  • Follow-Up Studies
  • Humans
  • Male
  • Middle Aged
  • Neuroendocrine Tumors / drug therapy
  • Neuroendocrine Tumors / metabolism
  • Neuroendocrine Tumors / mortality*
  • Niacinamide / administration & dosage
  • Niacinamide / analogs & derivatives
  • Phenylurea Compounds / administration & dosage
  • Prognosis
  • Prospective Studies
  • Sorafenib
  • Survival Rate
  • Tissue Distribution
  • raf Kinases / metabolism*

Substances

  • Biomarkers, Tumor
  • Phenylurea Compounds
  • Niacinamide
  • Cyclophosphamide
  • Sorafenib
  • raf Kinases