Potent Chemotherapeutic Compound for Treatment of Brain Cancer

Amphiphilic Fatty Acid Ether Compounds for Targeting Cancerous Cells of the Central Nervous System

Analogs of isopropyl aminopropanol (AIP) have been linked to the beta-adrenergic receptor polar head to generate chimeric molecules with potent antitumor properties. These novel compounds readily penetrate the blood-brain barrier and have been shown to suppress growth of glioblastoma cells, while demonstrating no toxicity towards normal cortical cells. According to the National Cancer Institute, the 5-year relative survival rate in individuals diagnosed with a malignant tumor of the central nervous system (CNS) in the United States is 35 percent1. Cancer of the CNS can take many forms, with malignant glioblastomas being the most prevalent brain tumor and the most difficult to treat. Available brain cancer treatments include tumor ablation, radiation, and use of chemotherapeutic drugs. Tumor ablation and treatment with radiation compromises the immune system, allowing persisting cells to continue to proliferate. Therapeutic drugs are often hard to synthesize, ineffective at crossing the blood-brain-barrier, and can be toxic to the natural brain environment. Available chemotherapeutic drug options are not specific and often target normal brain cells. Additionally, they fail at preventing cancer recurrence, prolonging treatment and increasing health care costs.

Researchers at the University of Florida have developed a series of novel compounds that show great promise for treatment of glioblastomas because they readily cross the blood-brain barrier and specifically target cancerous cells, while minimizing harm to normal brain cells.

Application

Potent chemotherapeutic compounds for treatment of cancers of the central nervous system, particularly glioblastomas

Advantages

• Readily crosses the blood-brain barrier, reducing the need for additional formulation work needed to deliver treatment to cancerous cells in the CNS
• Selectively targets proliferating cancerous cells, with negligible toxicity towards normal, non-cancerous brain cells
• Straightforward to synthesize and easy to generate derivatives, providing opportunities to modify the core AIP and create additional therapeutics

Technology

These chimeric isopropyl aminopropanol (AIP) compounds target proliferating cancerous brain cells. These compounds consist of analogs of isopropyl aminopropanol (AIP) linked to the beta-adrenergic receptor polar head. Additionally, AIP-containing nanoparticles can work with other chemotherapeutic treatments, collectively forming a self-emulsifying delivery system that increases efficacy and decreases toxicity. Compelling in vitro data shows that AIP compounds readily cross the blood-brain-barrier due to their amphiphilic nature and demonstrate selective toxicity towards proliferating cancerous cells.