IT-139: A Novel GRP78 Inhibitor


KEY FACTS

 

✔  Clinically-validated with manageable toxicity
 

✔  Targets critical proliferation and survival pathway
 

✔  Reduces resistance to other anti-cancer agents


STRATEGIC OVERVIEW


 
  • Moderate-risk, high-reward development program
  • Clinical-stage with favorable safety and toxicity profile
  • Potential synergy with wide variety of existing agents
    • Platinum-based Antineoplastics
      • Platinol® (cisplatin or CDDP)
      • Paraplatin® (carboplatin)
      • Eloxatin® (oxaliplatin)
    • Chemotherapy
      • Gemzar® (gemcitabine)
      • Taxotere® (docetaxel)
      • Taxol® (paclitaxel)
      • Adriamycin® (doxorubicin)
      • Adrucil® (fluorouracil or 5-FU)
      • Tarceva® (erlotonib)
      • Nexavar® (sorafenib)
      • Afinitor® (everolimus)
 

GRP78


KEY FACTS

  • Master regulator of endoplasmic reticulum (ER) stress
    • Critical proliferation, survival and resistance pathway
    • Overexpressed in cancer cells relative to normal cells due to hostile conditions in the tumor microenvironment
  • Inhibiting GRP78 should increase the efficacy and safety of existing anti-cancer drugs
 
 
 

AN IMPORTANT TARGET IN CANCER

GRP78 is the master-regulator of the Unfolded Protein Response (UPR), a signaling pathway that allows cells to survive stressful conditions and evade the toxic insult from cancer drugs.

Normal cells can survive low levels of GRP78, where it is responsible for protein folding and regulation of cellular stress. Chemotherapy drugs stress cancer cells.  The cells that survive chemotherapy express high levels of GRP78.  IT-139 is unique because it down-regulates GRP78 in tumor cells WITHOUT affecting GRP78 in normal cells.

 

er stress / grp78 as a critical target


INTELLECTUAL PROPERTY


Robust patent protection


16 Families
 

42 Active patents
 

18 Pending patents


PRECLINICAL DATA


It-139's Effect on Protein Levels Limited to Cancer Cells

 

IT-139 Inhibits Metastasis

 

IT-139 Decreases Gemcitabine Resistance in Pancreatic Ductal Adenocarcinoma

 

IT-139 Exhibits Profound Synergy in combination with Cisplatin and Oxaliplatin


CLINICAL DATA


IT-139-01 Clinical study in solid tumors

 
 
 

Change in Target Lesions


DEVELOPMENT STRATEGY


Target Indications


LICENSING OPPORTUNITIES


 
  • Seeking development and commercialization partners with the capital and expertise to advance development in both core and non-core indications for IT-139
  • Open to discuss:
    • Exploratory / pilot studies in combination with existing agents
    • Worldwide license by indication
    • Geographic license by indication
 
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  • Pancreatic Cancer
  • Colorectal Cancer
  • Lung Cancer
  • Osteosarcoma
  • Gastroesophageal Cancer
  • Breast Cancer
  • Prostate Cancer
  • Metastatic Melanoma
  • Liver Cancer
  • Other Solid Tumors

Licensing Contact

E. Russell McAllister

Chief Financial Officer
russell.mcallister@intezyne.com

O: 813.910.2120
C: 415.794.2686