Generex Provides Update on Success of Buccal Insulin Formulation Enhancement Project

Generex Biotechnology Corporation recently provided an update on the status of the buccal insulin formulation enhancement project for the company’s proprietary Generex Oral-lyn buccal insulin spray product. As previously announced, Generex engaged the University of Toronto’s Center for Molecular Design and Pre-formulations (CMDP) (www.cmdp.uhnres.utoronto.ca) through the University Health Network (www.uhn.ca) with the goal of enhancing the Generex Oral-lyn formulation to make it more attractive to patients and prospective commercialization partners by increasing the bioavailability of insulin in the product and reducing the number of sprays required to achieve effective prandial metabolic control for patients with diabetes. The project moved forward under the supervision of Dr. David Brusegard, PhD, the company’s Chief Operating Officer, Dr. James H. Anderson, Jr., MD, the Company’s Senior Scientific Advisor, and Generex consultant Dr. Lakshmi P. Kotra, B. Pharm.(Hons), PhD, of CMDP.

Dr. Brusegard commented “We are pleased to report that our preliminary efforts have succeeded in increasing the insulin concentration in the product by approximately 400% to 500% as confirmed by a variety of in vitro testing procedures while preserving the solubility, stability, and biologic activity and potency of the insulin in the formulation.”

Generex subsequently entered into a Research Services Agreement with the University of Guelph (www.uoguelph.ca) pursuant to which Dr. Dana Allen, DVM, MSc, and Dr. Ron Johnson, DVM, PhD, of the Ontario Veterinary College of the University of Guelph conducted a study of the relative bioavailability of the enhanced formulation in dogs in the University’s Comparative Clinical Research Facility. The University had previously conducted the studies of the original formulation of Generex Oral-lyn for proof-of- concept, safety, and toxicity.

In the new studies, the enhanced Generex Oral-lyn formulation was compared with the original formulation in a blinded, parallel controlled study involving fasted, awake, healthy mature beagle dogs. Each dog received three sprays of either the enhanced formulation or the original formulation. Each dog was observed with assessments of serum insulin and glucose measured over a 2-hour period. There were no adverse events observed in any of the animals.

In the dogs given the enhanced Generex Oral-lyn formulation, there was a 9-fold increase in serum insulin at 15 minutes (excluding one dog who had little response) and almost 500% greater absorption of insulin over the 2-hour test period compared to dogs given the original formulation. There was a 33% decrease in serum glucose at 30 minutes in dogs treated with the enhanced Generex Oral-lyn formulation, compared to a 12% increase in serum glucose in dogs treated with the original formulation.

“The outstanding results of these dog studies coupled with the positive findings from the in vitro work provide support and confidence to move forward as quickly as possible with the remaining clinical and regulatory work necessary to achieve FDA approval of the enhanced Generex Oral-lyn formulation,” said Dr. Anderson.
Generex Oral-lyn is designed to be a safe, simple, fast, flexible, and effective alternative to prandial insulin injections in people with either type 1 or type 2 diabetes mellitus.

Generex is engaged in the research, development, and commercialization of drug delivery systems and technologies. Generex has developed a proprietary platform technology for the delivery of drugs into the human body through the oral cavity (with no deposit in the lungs). The company’s proprietary liquid formulations allow drugs typically administered by injection to be absorbed into the body by the lining of the inner mouth using the company’s proprietary RapidMist device. Antigen Express, Inc. is a wholly owned subsidiary of Generex. The core platform technologies of Antigen Express comprise immunotherapeutic vaccines for the treatment of malignant, infectious, allergic, and autoimmune diseases. Antigen Express has pioneered the use of specific CD4+ T-helper stimulation technologies in immunotherapy. One focuses on modification of peptides with Ii-Key to increase potency, while a second relies on inhibition of expression of the Ii protein. Antigen Express scientists, and others, have shown clearly that suppression of expression of the Ii protein in cancer cells allows for potent stimulation of T-helper cells and prevents the further growth of cancer cells. For more information, visit the Generex website at www.generex.com or the Antigen Express website at www.antigenexpress.com.