Current anti-diabetes drugs also have limited long-term efficacy, leading to patients being prescribed a combination of two or
more different drugs until the ultimate drug of last resort, insulin, is given. Patients are aware of the long-term health
consequences if proper glycaemic control is not achieved and thus patients have a strong desire to improve the control of their
blood glucose levels. They are also aware of the finite use of current diabetes drugs before insulin treatment is required.
Therefore, treatment regimes that improve glycaemic control, eliminate the side effects or extend the efficacy of existing drugs
and improve patient well-being will represent a breakthrough.
We have invented a simple, natural and cost-effective solution for one of the world’s fastest growing disease. We are a clinical
stage pharmaceutical company planning to revolutionize the treatment for Type 2 diabetes mellitus (T2DM).
Within the past few decades pharmaceutical companies strived to develop new therapeutics for the treatment of T2DM. There
were a number of new drugs brought to the market targeting different axis to assist T2DM patient’s glucose control. However,
long terms use of currently available drugs cause major side effects. Unfortunately, long term use of some of these drug even
resulted in the evolution of drug-induced cancer, heart disease and kidney failure. Instead of developing New Chemical
entities to treat T2DM, that may cause major side effects, we asked a question – Would it be possible to abrogate clinically
significant side effects of an existing and well-established anti-diabetes drug(s) that are exposed to patients for the past 50
years? The short answer was "Yes". We have discovered and are developing an add-on/combination treatment to an existing
anti-diabetes drug to abrogate its clinically significant side effects and extend its efficacy in terms of duration and strength.
Our treatment ameliorates the side effects associated with an established and globally used sulfonylurea class of anti-diabetes
drugs. These anti-diabetes drugs are still widely used and their long-term side effects are well characterized; with nearly
half of patients with T2DM in China, India and Indonesia still being treated with sulfonylurea and about quarter of USA diabetes
patients receive sulfonylurea. This is because sulfonylurea is cheap and deemed sufficiently effective.
The use of this therapy improves glycaemic control and overall well-being in T2DM patients. The therapy involves an OZ101
tablet containing a proprietary oligosaccharide, which regulators worldwide deem safe and suitable for human consumption.
Type 2 Diabetes Mellitus
Diabetes is the fourth leading cause of global mortality by disease. Every year ~5 million diabetic patients die from diabetes
associated complications. T2DM is caused by a combination of insulin resistance and insufficient insulin production. Insulin is a
hormone secreted from pancreatic beta cells and is responsible for removing glucose from the blood to maintain normal blood
glucose levels. When food is digested, glucose is released into the blood stream causing an increase in blood glucose levels.
The increase in glucose triggers insulin secretion to assist with glucose transfer out of the blood. In T2DM, the presence of
insulin resistance requires an increase in insulin to be produced. However, when the pancreatic beta cells fail to produce
sufficient insulin, T2DM patients are unable to lower blood glucose levels back to the recommended level (5.5-7mmol/L).
According to International Diabetes Federation long term implications of elevated blood glucose include the risk of cardiovascular
disease, kidney damage, loss in vision, lower limb amputation. Risk factors include family history, unhealthy eating, lack of
exercise and overweight. Diabetes is an old disese and the earliest mention of diabetes was around 1552 BCE.
The number of patients diagnosed with type 2 diabetes increasing in an alarming rate and type 2 diabetes announced as a
pandemic disease by the United Nations. In 2015, the world had at least 415 million diagnosed type 2 diabetes patient,
accounting for over 5.7% of the world population, and is drastically rising. Over 50% of the world diabetes patients reside just in 3
countries: USA, China and India. USA carries highest percentage of diabetes population and pays the highest price for this
debilitating disease. For example management/caring/hospitalization of these patients consume very large portion of each
countries health budget, with USA paying at least $320 Billion a year. This is because the number of diabetes patients doubled in
US within the past 10 years (2005 – 2015) and is estimated to reach 30-40% of US population by 2030.
Currently marketed anti-diabetes drugs
T2DM can be prevented through life style changes but there is no cure. Current treatments for diabetes include anti-diabetes
drugs, the most commonly prescribed forms are metformin and sulfonylureas. Anti-diabetes drugs assist control of blood
glucose levels through a number of different ways. However, they can produce harmful side effects, including:
- Weight gain
- Hypoglycaemia (critically low blood glucose levels)
- Significant congestive heart failure
- Bone fractures
- Increased cardiovascular risks
- Lactic acidosis
- Hypersensitivity reactions
- Low blood pressure
- Kidney failure
Currently marketed newer oral anti-diabetes drug classes provide moderate glycemic control but may have serious side
effects and high costs, which restrict their use. The long-term use of currently available drugs may cause cancer or failure of
the heart and the kidney. Thus, there is an immediate need for better, safer and ideally cheaper treatments for T2DM.
Advantage of OZ101
The competitive landscape of OZ101 is illustrated in Table 2. Based on a number clinical case studies, Sulfonylurea + OZ101
anti-diabetes add-on/combination treatment is predicted to exert similar sustained efficacy to insulin in lowering fasting and
postprandial blood glucose and HbA1c levels. In contrast, Sulfonylurea + OZ101 treatment is (i) oral not injectable, therefore
eliminates local problems such as allergy/infections at insulin injection sites and would be more acceptable to patients, (ii)
affordable as opposed to expensive insulin treatment, (iii) little or no hypoglycaemic episodes as opposed to high incidence of
hypoglycemia through insulin injection, (iv) results in weight loss as opposed to weight gain induced by insulin administration, (v)
may be safer than other currently marketed newer treatments, (vi) will add to patient and health professional choice to aid
individualization of therapies.
Based on a number of clinical case studies, competitive advantage of OZ101 is highlighted in table 3.
OzStar’s innovation is based on the discovery that when patients with
T2DM use sulfonylurea therapy in combination with the new OZ101
therapy the major side effects of sulfonylurea, such as hypoglycaemia and
weight gain, are significantly reduced or eliminated and management of
this chronic disease is greatly improved such that sulfonylurea efficacy is
extended in terms of both strength and duration (from 6-12 months to over
5 years). This increased duration of efficacy is unusual for sulfonylurea
class of anti-diabetes drugs as demonstrated thorough conduct of 10
different clinical trials worldwide that illustrated in Figure 5 of a peer-
reviewed article published by (DeFronzo et al. Diabetes Care, 36, Supp 2,
S127-S138 (2013). Figure 1 depicts an illustration of the synergy between
sulfonylurea and OZ101.