90Y-Labeled Anti-ROBO1 Monoclonal Antibody Exhibits Antitumor Activity against Small Cell Lung Cancer Xenografts

PLoS One. 2015 May 27;10(5):e0125468. doi: 10.1371/journal.pone.0125468. eCollection 2015.

Abstract

Introduction: ROBO1 is a membrane protein that contributes to tumor metastasis and angiogenesis. We previously reported that 90Y-labeled anti-ROBO1 monoclonal antibody (90Y-anti-ROBO1 IgG) showed an antitumor effect against ROBO1-positive tumors. In this study, we performed a biodistribution study and radioimmunotherapy (RIT) against ROBO1-positive small cell lung cancer (SCLC) models.

Methods: For the biodistribution study, 111In-labeled anti-ROBO1 monoclonal antibody (111In-anti-ROBO1 IgG) was injected into ROBO1-positive SCLC xenograft mice via the tail vein. To evaluate antitumor effects, an RIT study was performed, and SCLC xenograft mice were treated with 90Y-anti-ROBO1 IgG. Tumor volume and body weight were periodically measured throughout the experiments. The tumors and organs of mice were then collected, and a pathological analysis was carried out.

Results: As a result of the biodistribution study, we observed tumor uptake of 111In-anti-ROBO1 IgG. The liver, kidney, spleen, and lung showed comparably high accumulation of 111In-labeled anti-ROBO1. In the RIT study, 90Y-anti-ROBO1 IgG significantly reduced tumor volume compared with baseline. Pathological analyses of tumors revealed coagulation necrosis and fatal degeneration of tumor cells, significant reduction in the number of Ki-67-positive cells, and an increase in the number of apoptotic cells. A transient reduction of hematopoietic cells was observed in the spleen, sternum, and femur.

Conclusions: These results suggest that RIT with 90Y-anti-ROBO1 IgG is a promising treatment for ROBO1-positive SCLC.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry
  • Antibodies, Monoclonal / immunology
  • Antibodies, Monoclonal / pharmacokinetics
  • Antibodies, Monoclonal / pharmacology*
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / pathology
  • Lung Neoplasms / radiotherapy
  • Male
  • Mice, Inbred BALB C
  • Mice, Nude
  • Nerve Tissue Proteins / immunology*
  • Nerve Tissue Proteins / metabolism
  • Radioimmunotherapy / methods
  • Receptors, Immunologic / immunology*
  • Receptors, Immunologic / metabolism
  • Roundabout Proteins
  • Small Cell Lung Carcinoma / drug therapy*
  • Small Cell Lung Carcinoma / pathology
  • Small Cell Lung Carcinoma / radiotherapy
  • Tissue Distribution
  • Xenograft Model Antitumor Assays / methods
  • Yttrium Radioisotopes / chemistry
  • Yttrium Radioisotopes / pharmacokinetics
  • Yttrium Radioisotopes / therapeutic use*

Substances

  • Antibodies, Monoclonal
  • Nerve Tissue Proteins
  • Receptors, Immunologic
  • Yttrium Radioisotopes

Grants and funding

This research was supported by a grant from the Japan Society for the Promotion of Science (JSPS) through the “Funding Program for World-Leading Innovative R&D on Science and Technology (FIRST Program),” initiated by the Council for Science and Technology Policy (CSTP). Co-authors Yasutaka Saito, Akihiro Hino and Hiroyuki Kasahara are employed by FUJIFILM RI Pharma Co., Ltd. FUJIFILM RI Pharma Co., Ltd. joined this study as a collaborating company in the Japan Society for the Promotion of Science through the “Funding Program for World-Leading Innovative R&D on Science and Technology.” It was responsible for radiolabelling of antibodies. Co-author Kosuke Suga is employed by SANKYO LABO SERVICE Co., Ltd. SANKYO LABO SERVICE Co., Ltd. provided support in the form of salary for author KS, but did not have any additional role in the study design, data collection and analysis, decision to publish, or preparation of the manuscript. The specific role of this author is articulated in the ‘author contributions’ section.