Safe and Effective Sarcoma Therapy through Bispecific Targeting of EGFR and uPAR

Mol Cancer Ther. 2017 May;16(5):956-965. doi: 10.1158/1535-7163.MCT-16-0637. Epub 2017 Feb 13.

Abstract

Sarcomas differ from carcinomas in their mesenchymal origin. Therapeutic advancements have come slowly, so alternative drugs and models are urgently needed. These studies report a new drug for sarcomas that simultaneously targets both tumor and tumor neovasculature. eBAT is a bispecific angiotoxin consisting of truncated, deimmunized Pseudomonas exotoxin fused to EGF and the amino terminal fragment of urokinase. Here, we study the drug in an in vivo "ontarget" companion dog trial as eBAT effectively kills canine hemangiosarcoma and human sarcoma cells in vitro We reasoned the model has value due to the common occurrence of spontaneous sarcomas in dogs and a limited lifespan allowing for rapid accrual and data collection. Splenectomized dogs with minimal residual disease were given one cycle of eBAT followed by adjuvant doxorubicin in an adaptive dose-finding, phase I-II study of 23 dogs with spontaneous, stage I-II, splenic hemangiosarcoma. eBAT improved 6-month survival from <40% in a comparison population to approximately 70% in dogs treated at a biologically active dose (50 μg/kg). Six dogs were long-term survivors, living >450 days. eBAT abated expected toxicity associated with EGFR targeting, a finding supported by mouse studies. Urokinase plasminogen activator receptor and EGFR are targets for human sarcomas, so thorough evaluation is crucial for validation of the dog model. Thus, we validated these markers for human sarcoma targeting in the study of 212 human and 97 canine sarcoma samples. Our results support further translation of eBAT for human patients with sarcomas and perhaps other EGFR-expressing malignancies. Mol Cancer Ther; 16(5); 956-65. ©2017 AACR.

MeSH terms

  • ADP Ribose Transferases / administration & dosage
  • ADP Ribose Transferases / chemistry
  • ADP Ribose Transferases / genetics
  • Animals
  • Bacterial Toxins / administration & dosage
  • Bacterial Toxins / chemistry
  • Bacterial Toxins / genetics
  • Cell Line, Tumor
  • Disease Models, Animal
  • Dogs
  • Doxorubicin / administration & dosage
  • Epidermal Growth Factor / chemistry
  • Epidermal Growth Factor / genetics
  • ErbB Receptors / antagonists & inhibitors
  • ErbB Receptors / genetics*
  • Exotoxins / administration & dosage
  • Exotoxins / chemistry
  • Exotoxins / genetics
  • Hemangiosarcoma / drug therapy*
  • Hemangiosarcoma / genetics
  • Hemangiosarcoma / pathology
  • Humans
  • Mice
  • Molecular Targeted Therapy*
  • Neoplasm Staging
  • Pseudomonas aeruginosa Exotoxin A
  • Receptors, Urokinase Plasminogen Activator / antagonists & inhibitors
  • Receptors, Urokinase Plasminogen Activator / genetics*
  • Urokinase-Type Plasminogen Activator / chemistry
  • Urokinase-Type Plasminogen Activator / genetics
  • Virulence Factors / administration & dosage
  • Virulence Factors / chemistry
  • Virulence Factors / genetics

Substances

  • Bacterial Toxins
  • Exotoxins
  • Receptors, Urokinase Plasminogen Activator
  • Virulence Factors
  • Epidermal Growth Factor
  • Doxorubicin
  • ADP Ribose Transferases
  • EGFR protein, human
  • ErbB Receptors
  • Urokinase-Type Plasminogen Activator