Successful Oral Insulin Toxicity Result - Oradel(TM), Loaded With Generic Insulin

Announced today that the final report confirms the success of its oral insulin in Phase 1 toxicology trials. Apollo's oral insulin consists of its oral delivery technology, Oradel™, loaded with generic insulin. The treatment proved safe at both low and high doses.

LONDON, UK | Feb 01, 2007 |
Apollo Life Sciences (ASX:AOP) announced today that the final report confirms the success of its oral insulin in Phase 1 toxicology trials. Apollo's oral insulin consists of its oral delivery technology, Oradel™, loaded with generic insulin. The treatment proved safe at both low and high doses.

The toxicology study was designed to test the safety of Apollo's oral insulin for people with diabetes. Oradel™ insulin was administered daily to two animal species for 14 days, followed by a 14-day recovery period. Control groups received treatment with the vehicle alone.

The key findings are that Oradel™ insulin caused no toxic effects or treatment-related changes in body weights, food consumption, blood analysis, urinalysis, gross necroscopy or histopathology.

"These favourable results provide strong supporting safety data for taking our oral insulin to Phase 1 human clinical trials, which we expect to undertake in the coming months," said Dr Greg Russell-Jones, Apollo's Science Director.

Diabetes is responsible for approximately 4 million deaths worldwide every year. It is estimated that there are now 246 million people with diabetes, growing to 380 million by 2025. A recent United Nations resolution calling on all countries to develop national policies for the prevention, treatment and care of diabetes acknowledges global concern at the prevalence of diabetes.

"Our innovative oral insulin could mean the end of needles for many people with diabetes. Some need up to five insulin shots a day to manage their condition," said Dr Russell-Jones. "It is only a matter of time before we enter the marketplace with our insulin in a tablet, and we believe that most people prefer to take a tablet instead of an injection."

The global market for diabetes medications is valued at $18 billion per annum.

About Apollo's toxicity study

The trial took the form of a repeated dose, 14-day oral toxicity study of Apollo's oral insulin, with a 14-day recovery period in two species - rats and rabbits. The objective of the test study was to evaluate the potential toxicity of Apollo's oral insulin at two dose levels (low and high) following repeated oral administration in Sprague Daeley rats and New Zealand White rabbits, followed by a recovery phase.

Two groups of rats and rabbits, 20 animals/group (10/sex) were administered Apollo's oral insulin (dissolved in water for irrigation) for 14 days. One group received a low dose, and the other a high dose. The low dose in this study was the anticipated daily therapeutic dose of Oradel™ insulin. The high dose was set at a maximal level. A third group, the vehicle control group, was administered the vehicle only. From each treatment group, 10 animals (5/sex) were observed for an additional treatment-free period of 14 days to assess reversibility of any potential toxicity post-treatment.

The following parameters were evaluated in all animals: mortality, daily general clinical observations, body weights, food consumption, blood analysis, urinalysis, organ weights, and gross necropsy. Extensive histopathology was performed on the high dose and vehicle control groups.

No mortalities were observed during the experimental period. No treatment-related findings were noted in clinical observations, body weight and feed intake. Haematology, biochemistry and urinalysis were unremarkable in both the laminal study and recovery groups. No treatment-related abnormalities were noted in gross necropsy and histopathology. No toxic effects were seen in the low and high dose treated animals.

Haematological and biochemical testing were performed by IDEXX Laboratories (ISO.IEC17025, NATA accredited 10166). Tissue processing and staining were performed by Symbion Vetnostics (ISO/IEC17025, NATA accredited 14599).

ICP Firefly Pty Ltd, which performed the toxicity study, is accredited as an Animal Research Establishment (Ref. No. AW96/042) with the Animal Welfare Unit of New South Wales Agriculture. The experimental protocol was approved by the ICP Firefly Animal Ethics Committee, and was found to be in compliance with all appropriate regulations.

The study was conducted in compliance with the OECD Principles of Good Laboratory Practice.

About Apollo's insulin in a tablet/OradelTM

Insulin is the therapy of choice for many people with diabetes mellitus. But the existing need for insulin injection creates both compliance and dosing effectiveness problems for a significant proportion of patients with diabetes. Apollo's insulin in a tablet would overcome these problems. First, its higher patient acceptability will increase compliance, which will in turn reduce the risk of complications such as cardiovascular disease, neuropathy, retinopathy, and nephropathy. Second, because of its particular oral formulation, Apollo's oral insulin slowly releases the insulin, avoiding initial spikes in insulin levels, which can be toxic, and allowing the sustained release of insulin for a period of at least eight hours.

These characteristics are particularly valuable for basal, long-acting insulin, which currently has no alternative delivery forms to injection. Basal insulin is required for all those with type 1 and gestational diabetes, as well as for many in the advanced stages of type 2 diabetes.

About Apollo's oral delivery technology

Apollo's oral delivery technology, Oradel™, provides a coating that protects insulin from the stomach and uses targeting agents to promote absorption of insulin from the intestine.

Oral delivery of proteins is a breakthrough because the stomach's digestive acids usually destroy proteins before they can be taken up by the body, and the stomach lining typically prevents material passing into the bloodstream.

OradelTM technology enables controlled release of the active molecule and, thus, a long-acting therapeutic effect. Pre-clinical studies indicate it transports large protein molecules, up to 150kDa in weight in sub-micron structures of around 200 nm in size. Each cell in the stomach wall transports the sub-micron structures at a different rate, allowing for a controlled release of the drug into the circulation. Once the structures containing the drug or protein are released into circulation, the structure collapses and the drug is released.

Preclinical studies on the oral delivery technology using large proteins have been conducted in more than 120 animals, demonstrating effective delivery of bioactive molecules. The oral insulin studies confirm these findings. This technology is the subject of provisional patents and trademarks.

SOURCE: Apollo Life Sciences

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