Clinical Implication of Anti-Angiogenic Effect of Regorafenib in Metastatic Colorectal Cancer

PLoS One. 2015 Dec 15;10(12):e0145004. doi: 10.1371/journal.pone.0145004. eCollection 2015.

Abstract

Background: Regorafenib induces distinct radiological changes that represent its anti-angiogenic effect. However, clinical implication of the changes is unclear.

Methods: Tumor attenuation as measured by Hounsfield units (HU) in contrast-enhanced computed tomography (CT) and cavitary changes of lung metastases were analyzed in association with treatment outcome of metastatic colorectal cancer patients (N = 80) treated with regorafenib in a prospective study.

Results: 141 lesions in 72 patients were analyzed with HU. After 2 cycles of regorafenib, 87.5% of patients showed decrease of HU (Median change -23.9%, range -61.5%-20.7%). Lesional attenuation change was modestly associated with metabolic changes of 18-fluoro-deoxyglucose positron emission tomography-CT (Pearson's r = 0.37, p = 0.002). Among 53 patients with lung metastases, 17 (32.1%) developed cavitary changes. There were no differences in disease control rate, progression-free survival, or overall survival according to the radiological changes. At the time of progressive disease (PD) according to RECIST 1.1, HU was lower than baseline in 86.0% (43/50) and cavitary change of lung metastasis persisted without refilling in 84.6% (11/13).

Conclusion: Regorafenib showed prominent anti-angiogenic effect in colorectal cancer, but the changes were not associated with treatment outcome. However, the anti-angiogenic effects persisted at the time of PD, which suggests that we may need to develop new treatment strategies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Angiogenesis Inhibitors / therapeutic use*
  • Colorectal Neoplasms / blood supply*
  • Colorectal Neoplasms / drug therapy
  • Colorectal Neoplasms / pathology*
  • Disease-Free Survival
  • Female
  • Humans
  • Male
  • Middle Aged
  • Neoplasm Metastasis
  • Neovascularization, Pathologic / drug therapy*
  • Phenylurea Compounds
  • Pyridines
  • Treatment Outcome
  • Tumor Burden

Substances

  • Angiogenesis Inhibitors
  • Phenylurea Compounds
  • Pyridines
  • regorafenib

Grants and funding

This research was supported by a grant of the Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI, http://www.khidi.or.kr), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI14C1277), to TYK. Regorafenib was provided by Bayer Pharma AG (http://pharma.bayer.com). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.