Small Interfering RNA Inhibition of Cannabanoid-1 Receptor (CB1R) for Treating Type 2 Diabetes

The invention pertains to the use of glucan encapsulated non-immunostimulatory small interfering RNAs (siRNAs) to treat type-2 diabetes. Endocannabinoids (EC) are lipid signaling molecules that act on the same cannabinoid receptors that recognize and mediate the effects of endo- and phytocannabanoids. EC receptor CB1R activation is implicated in the development of obesity and its metabolic consequences, including insulin resistance and type 2 diabetes. Beta-cell loss has been demonstrated in a Zucker diabetic fatty (ZDF) rat model of type-2 diabetes through CB1R-mediated activation of a macrophage-mediated inflammatory response. Conversely, rats treated with a peripheral CB1R antagonist restores normoglycemia and preserves beta-cell function. Similar results are seen following selective in vivo knockdown of macrophage CB1R by daily treatment of ZDF rats with the instant D-glucan-encapsulated CB1R Small interfering RNA (siRNA). Knock-down of CB1R with using glucan encapsulated siRNA may represent a new commecializable method of treating type-2 diabetes or preventing the progression of insulin resistance to overt diabetes.

Potential Commercial Applications: Competitive Advantages:
    Treatment of obesity, insulin resistance, and diabetes.
    A new means of inhibiting the endocannabinoid receptor CB1R.

Development Stage:
In vivo data available (animal)


George Kunos (NIAAA)  ➽ more inventions...

Tony Jourdan (NIAAA)  ➽ more inventions...

Michael Czech

Myriam Aouadi

Intellectual Property:
U.S. Pat: 10,077,446 issued 2018-09-18
US Application No. 61/839,239
PCT Application No. PCT/US2014/043924
European Patent Application pending

Licensing Contact:
Michael Shmilovich, J.D.
Phone: 301-435-5019

OTT Reference No: E-103-2013-0
Updated: Oct 13, 2017