[Federal Register Volume 82, Number 33 (Tuesday, February 21, 2017)]
[Notices]
[Page 11235]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2017-03306]


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DEPARTMENT OF HEALTH AND HUMAN SERVICES

National Institutes of Health


Government-Owned Inventions; Availability for Licensing

AGENCY: National Institutes of Health, HHS.

ACTION: Notice.

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SUMMARY: The inventions listed below are owned by an agency of the U.S. 
Government.

FOR FURTHER INFORMATION CONTACT: Licensing information may be obtained 
by emailing the indicated licensing contact at the National Heart, 
Lung, and Blood, Office of Technology Transfer and Development Office 
of Technology Transfer, 31 Center Drive, Room 4A29, MSC2479, Bethesda, 
MD 20892-2479; telephone: 301-402-5579. A signed Confidential 
Disclosure Agreement may be required to receive any unpublished 
information.

SUPPLEMENTARY INFORMATION: The following inventions are available for 
licensing in accordance with 35 U.S.C. 209 and 37 CFR part 404 to 
achieve expeditious commercialization of results of federally-funded 
research and development. Technology description follows.

Methods for Improving Drug Delivery to the Central Nervous System

    The invention relates to the uses of the tricyclic antidepressant 
amitriptyline, its bioactive metabolites, and other LPA1R activators to 
improve the bioavailability and delivery of therapeutics to the central 
nervous system. This invention demonstrates that amitriptyline and 
other agents selectively decrease P-glycoprotein (P-gp) transport 
activity by ligand activation of lysophosphatidic acid 1 receptor 
(LPA1R) at the blood-brain barrier. P-gp is an effective target for 
increasing drug delivery to the brain (CNS) for two major reasons: (1) 
Its substrates include a large portion of on-the-market drugs, 
including chemotherapeutics, and (2) its directionality results in a 
net efflux of drugs from the brain. Additionally, specifically 
targeting P-gp through LPA1R activation bypasses the clinical 
challenges resulting from the toxicity of substrate inhibitors of P-gp. 
This invention describes the inhibition of drug efflux by P-gp 
transport; thus, co-administration of therapeutics with amitriptyline 
and other LPA1R activators provides a method for increasing drug 
delivery to the CNS, and improving overall drug efficacy. Moreover, 
drug delivery to other barrier tissues will also be enhanced where a 
similar LPA1R-P-gp activity relationship exists.
    Potential Commercial Applications:
     Drug Delivery to the CNS.
     Co-administration of therapeutics.
     Blood-brain-barrier permeability.
    Development Stage:
     Early stage.
    Inventors: Ronald Cannon and David Banks (NIEHS).
    Publications:
     Cannon et al., Neurosci Lett. 2017 Feb 3;639:103-113 doi: 
10.1016/j.neulet.2016.12.049.
     Mesev, et al., Mol Pharmacol. 2017 Jan 24. pii: 
mol.116.107169. doi: 10.1124/mol.116.107169.
     More, et al., J Cereb Blood Flow Metab. 2016 May 18. pii: 
0271678X16650216.
     Miller, et. al, Curr Pharm Des. 2014;20(10):1463-71. 
Review.
     Cartwright, et al., J Cereb Blood Flow Metab. 2013 
Mar;33(3):381-8. doi: 10.1038/jcbfm.2012.174.
    Intellectual Property: HHS Reference No. E-179-2065/0 and/1; U.S. 
Provisional Patent Applications 62/332,888 filed May 6, 2016, and 62/
453,718 filed February 2, 2017, respectively.
    Licensing Contact: Michael Shmilovich, Esq., CLP; 301-435-5019; 
[email protected].

    Dated: February 10, 2017.
Michael Shmilovich,
Senior Licensing and Patenting Manager, National Heart, Lung, and Blood 
Institute, Office of Technology Transfer and Development.
[FR Doc. 2017-03306 Filed 2-17-17; 8:45 am]
 BILLING CODE 4140-01-P