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12:00 AM
Oct 26, 2009
 |  BioCentury  |  Product Development

Breaking through the BBB

The idea of using the brain's own transport receptors to ferry drugs across the blood-brain barrier has been around for more than a decade. AngioChem Inc., one of a new generation of companies trying to take advantage of natural transport molecules in the brain, is the first to report proof-of-concept data on delivering therapeutics across the divide in humans.

The next step will be to find a partner.

AngioChem's delivery technology uses peptides derived from endogenous ligands of the low-density lipoprotein receptor-related protein (LRP) receptor, which is expressed at the BBB. Under normal conditions, the LRP receptor interacts with tissue plasminogen activator (tPA) to control vasoactivity, permeability and post-ischemic lesion formation.

The company's lead compound, ANG1005, consists of three molecules of paclitaxel conjugated to a sequence of amino acids that bind to the LRP receptor. Paclitaxel does not normally cross the BBB. Attachment of ANG1005 to the LRP receptor mediates transport of the compound across the BBB. And because the LRP receptor also is expressed on tumor cells, ANG1005...

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