Activating Ion Channels Increases Drug Delivery to Brain Tumors

– Researchers at Cedars Sinai Medical Center in Los Angeles have devised a method of increasing the permeability of the blood-brain tumor barrier to enhance the delivery of chemotherapeutic agents.

Calcium-activated potassium channels play a pivotal role in blood-brain tumor barrier (BTB) permeability regulation, Dr. Keith L. Black and associates report in The Journal of Pharmacology and Experimental Therapeutics for June.

 Using rats, they found for the first time that these channels are overexpressed in brain tumor endothelial cells compared with normal brain tissue. The capillary dilator bradykinin can increase BTB permeability, but the effect is transient and variable, Dr. Black’s group notes.

They developed a synthetic form of bradykinin, NS-1619, which elicits enhanced and sustained drug delivery to tumor tissue by directly activating the calcium-activated potassium channels when infused into the carotid artery.

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