Targeted α-therapy using 227Th-APOMAB and cross-fire antitumour effects: preliminary in-vivo evaluation

Nucl Med Commun. 2014 Dec;35(12):1284-90. doi: 10.1097/MNM.0000000000000199.

Abstract

Resistance to conventional cancer treatments is a major problem associated with solid tumours. Tumour hypoxia is associated with a poor prognosis and with poor treatment outcomes; therefore, there is a need for treatments that can kill hypoxic tumour cells. One potential option is targeted α-radioimmunotherapy, as α-particles can directly kill hypoxic tumour cells. The murine monoclonal antibody DAB4 (APOMAB), which binds dead tumour cells after DNA-damaging treatment, was conjugated and radiolabelled with the α-particle-emitting radionuclide thorium-227 (Th). Mice bearing Lewis lung tumours were administered Th-DAB4 alone or after chemotherapy and the tissue biodistribution of the radioimmunoconjugate was examined, as was the effect of these treatments on tumour growth and survival. Th-DAB4 accumulated in the tumour particularly after chemotherapy, whereas the distribution in healthy tissues did not change. Th-DAB4 as a monotherapy increased survival, with more pronounced responses observed when given after chemotherapy. We have shown that targeted α-therapy of necrotic tumour cells with Th-DAB4 had significant and surprising antitumour activity as it would occur only through a cross-fire effect.

MeSH terms

  • Alpha Particles / therapeutic use*
  • Animals
  • Antibodies, Monoclonal / pharmacokinetics
  • Antibodies, Monoclonal / therapeutic use*
  • Carcinoma, Lewis Lung / drug therapy
  • Carcinoma, Lewis Lung / metabolism
  • Carcinoma, Lewis Lung / radiotherapy*
  • Cell Line, Tumor
  • Combined Modality Therapy
  • Female
  • Mice
  • Radioimmunotherapy / methods*
  • Radioisotopes / therapeutic use*
  • Thorium / therapeutic use*
  • Tissue Distribution

Substances

  • Antibodies, Monoclonal
  • Radioisotopes
  • Thorium
  • apomab