From rxpgnews.com
Pep:trans Technology Helps Drugs Cross Blood Brain Barrier with Ease
By Synt:em,
Apr 15, 2005 - 11:44:38 AM
Morphine 6 glucoronide (M6G) (an active, potent metabolite of morphine) was chemically linked to a small Pep:trans peptide vector in order to enhance the transfer of the metabolite across the blood brain barrier (BBB).
A proof of concept study was designed to demonstrate the transport of the resulting new drug, known as Syn1001.
Syn1001 was injected sub cutaneous to volunteers in a double-blind, randomised study where multiple biomarkers of brain activity of Syn1001 were assessed.
Biomarkers included pupillometry (a measurement of the pupil size which is an indicative of opioid central effect), central opioid activity and other psychological assessments through various scales.
Based on these biomarkers, evidence of fast central penetration of the Syn1001 in the brain was clearly observed.
Moreover the study shows that Syn1001 is active on pain and that it is an effective analgesic drug. Syn1001 has the potential to reduce the dose necessary for an effective analgesic effect as well as reducing the morphine-like side effects.
This demonstrates for the first time that a Pep:trans peptide vector is able to transport a drug across the human blood brain barrier.
Dr. Michel Kaczorek, Founder & Chief Executive Officer of Synt:em, commented, these results demonstrate that it is possible to re-engineer drugs with our Pep:trans technology in order to create new drugs which can efficiently enter the brain. We now have opened-up a way to rapidly develop new drugs which address the huge market of central nervous system diseases. We believe that Syn1001 is well positioned as a potential product to treat post-operative pain .
About the Pep :trans technology
Pep:trans is a series of proprietary peptide-derived molecules (vectors) that enable the efficient design of new chemical entities through conjugation to known drugs or new compounds. The peptide vector addition can result in improved pharmacology, increased solubility, altered plasma half life and protein binding, and modified biodistribution and pharmaco-kinetics.
Importantly, the Pep:trans drug conjugate is a fully patentable New Chemical Entity.
Drugs linked to Pep:trans have shown significant enhancement of brain or cell uptake in experimental models, resulting in an associated improvement of pharmacological activity in animal models. Pep:trans vectors can carry almost any type of molecule into cells, including classical small molecules and peptides, as well as small proteins and DNA fragments and across the blood brain barrier Pep:trans can carry small molecules and peptides.
The blood brain barrier (BBB) is a shield of specialized blood vessels that forms a protective barrier between the blood and brain, screening out all but a few selected classes of molecules that attempt to access the brain. Although new pharmaceutical compounds have the potential for treating specific brain diseases, their development is often frustrated by the inability of these drugs to cross the BBB.
Existing technologies used to get these drugs into the brain are often impractical, unsafe or limited in their application (require direct injection into the brain or invasive neurological delivery).
Pep:trans resolves these issues and can allow for the effective, rapid and safe passage of various drug molecules including anticancer drugs, antibiotics and peptides through the blood brain barrier.
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