Preclinical data on ANG4043, a first-in-class peptide antibody conjugate, presented at the 2013 San Antonio Breast Cancer Symposium

MONTREAL, Canada I December 16, 2013 I Angiochem, a clinical stage biotechnology company developing drugs that are uniquely capable of crossing the blood-brain barrier (BBB), today announced that its peptide-antibody conjugate, ANG4043 successfully crosses the BBB, reduces tumor size and significantly increases survival in mice with intracranial HER2-positive brain tumors. These results underscore the potential for development of novel antitumor therapeutics for neuro-oncology indications. The data presentation revealed that the company’s technology has been successfully applied to monoclonal antibodies (mAbs) for creation of brain-penetrant antibody conjugates of anti-Human Epidermal Growth Factor Receptor 2 (HER2). The data was presented at the 2013 San Antonio Breast Cancer Symposium, held December 10-14, 2013 in San Antonio, TX.

During a poster presentation, entitled “ANG4043, a brain-penetrant anti-HER2 mAb increases survival of mice bearing intracranial BT-474 breast tumor cells,” Angiochem researchers described the ANG4043 preclinical results, including:

  • In vivo, in mice that were implanted intracranially with HER2+ human breast tumor cells (BT-474), it was observed:
    • ANG4043 crosses the BBB and reaches the tumor using near-infrared imaging, where a strong signal is observed in brain following IV administration of fluorescent ANG4043, but not of fluorescent anti-HER2
    • Reduction in tumor size correlating with increased survival
  • In vitro, ANG4043 binding affinity for HER2 receptor and anti-proliferative properties were similar to the native, unconjugated mAb.

“The therapeutic potential of mAbs to treat a variety of tumor types is well established, however, this class of agents is generally unable to have therapeutic effects in the brain due to poor blood-brain barrier permeability,” said Jean Paul Castaigne, MD, President and CEO of Angiochem. “We have clearly demonstrated creation of a peptide-mAb conjugate that enters the CNS, extending the potential for mAbs to be applied to cancers appearing in the brain. These data continue to validate the breadth and power of our technology, beyond small molecules and peptides, to include larger molecules such as monoclonal antibodies that open new opportunities to develop brain-penetrating antitumor therapeutics.”

About Angiochem

Angiochem is a clinical-stage biotechnology company discovering and developing new breakthrough peptide drug conjugates that leverage the LRP-1 mediated pathway to cross the BBB to treat neurological diseases. These new compounds have the potential to address significant medical needs, many of which are insurmountable due to the fundamental physiological challenge posed by the BBB.

Angiochem is developing a focused product pipeline, including small molecules and biologics, for the potential treatment of a wide range of CNS diseases, including primary brain cancer, brain metastases, lysosomal storage diseases and pain. Founded in 2003, Angiochem maintains headquarters in Montreal, Canada. For additional information about the Company, please visit  http://www.angiochem.com.

SOURCE: Angiochem