α-particle therapy for synovial sarcoma in the mouse using an astatine-211-labeled antibody against frizzled homolog 10

Cancer Sci. 2018 Jul;109(7):2302-2309. doi: 10.1111/cas.13636. Epub 2018 Jun 27.

Abstract

Synovial sarcoma (SS) is a rare yet refractory soft-tissue sarcoma that predominantly affects young adults. We show in a mouse model that radioimmunotherapy (RIT) with an α-particle emitting anti-Frizzled homolog 10 (FZD10) antibody, synthesized using the α-emitter radionuclide astatine-211 (211 At-OTSA101), suppresses the growth of SS xenografts more efficiently than the corresponding β-particle emitting anti-FZD10 antibody conjugated with the β-emitter yettrium-90 (90 Y-OTSA101). In biodistribution analysis, 211 At was increased in the SS xenografts but decreased in other tissues up to 1 day after injection as time proceeded, albeit with a relatively higher uptake in the stomach. Single 211 At-OTSA101 doses of 25 and 50 μCi significantly suppressed SS tumor growth in vivo, whereas a 50-μCi dose of 90 Y-OTSA101 was needed to achieve this. Importantly, 50 μCi of 211 At-OTSA101 suppressed tumor growth immediately after injection, whereas this effect required several days in the case of 90 Y-OTSA101. Both radiolabeled antibodies at the 50-μCi dosage level significantly prolonged survival. Histopathologically, severe cellular damage accompanied by massive cell death was evident in the SS xenografts at even 1 day after the 211 At-OTSA101 injection, but these effects were relatively milder with 90 Y-OTSA101 at the same timepoint, even though the absorbed doses were comparable (3.3 and 3.0 Gy, respectively). We conclude that α-particle RIT with 211 At-OTSA101 is a potential new therapeutic option for SS.

Keywords: frizzled homolog 10; radioimmunotherapy; synovial sarcoma; α-particle; β-particle.

MeSH terms

  • Alpha Particles / therapeutic use
  • Animals
  • Antibodies, Monoclonal / therapeutic use
  • Astatine / therapeutic use*
  • Cell Line, Tumor
  • Frizzled Receptors / antagonists & inhibitors*
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Radioimmunotherapy / methods*
  • Radioisotopes / therapeutic use*
  • Sarcoma, Synovial / radiotherapy*
  • Xenograft Model Antitumor Assays

Substances

  • Antibodies, Monoclonal
  • Astatine-211
  • FZD10 protein, human
  • Frizzled Receptors
  • Radioisotopes
  • Astatine