2799

Novel Pt(IV) Anti-Cancer Based Prodrug Acting on Multiple Cellular Targets

Gibson Dan, HUJI, School of Medicine - IMRIC, School of Pharmacy- Institute for Drug Research

 

Categories:

Life science and biotechnology

Technology Keywords

Oncology, cancer drug resistance , chemotherapy, prodrug

Development Stage

Preliminary POC with supporting in-vivo data

 

Our Innovation

  • Major depressive disorder (MDD), also known as clinical depression, is widely recognized as one the greatest challenges to human health and well-being, and is associated with substantial morbidity and an enormous social and economic burden.
  • Despite decades of intensive research, the biological mechanisms that causally underlie depression are still unclear, hindering the development of effective preventive and therapeutic procedures.
  • Based on his previous findings that microglial activators exert anti-depressive effects, the researcher was able to prove that Electroconvulsion therapy (ECT)-induced microglial alterations are causally related to the anti-depressive effects of ECT
  • Our invention suggest a new treatment for depression and other related disorders  using an immune checkpoint blocker that restrains microglial activity in a manner mimicking ECT treatment effects

 

Highlights

  • The lead compound releases two potent Pt(II) complexes that act by fundamentally different mechanisms as well as two bioactive ligands (DCA and PhB) that act on different cellular targets ("cluster bombs“). 
  • This multiple attacks on different cellular targets by a single moiety may overcome the limitations of classical combination therapy.
  • May overcoming resistance to cisplatin

 

The Opportunity

  • Although FDA approved Pt(II) drugs are used in 50% of all chemotherapeutic regimens, their inability to overcome acquired resistance, necessitates development of improved drugs. Clinicians attempt to overcome resistance by using combination chemotherapy.  The drawback of combination chemotherapy is that each of the drugs has a different pharmacokinetic profile making overall control difficult.
  • We can synthesize a library of “cluster bombs” that will be screened against a panel of different cancers characterized by a diverse grade of sensitivity/resistance to classical chemotherapeutic drugs.  This will enable us to address several types of cancers.

 

Researcher Information

https://medicine.ekmd.huji.ac.il/en/publications/researchersPages/pages/dang.aspx