OPK88003 (Oxyntomodulin Analog)

About Oxyntomodulin

Oxyntomodulin is a naturally occurring hormone produced in the colon, shown to bind both the GLP-1 and glucagon receptor, regulating both blood glucose appetite and lipid metabolism. ˹ is developing OPK88003, a long-acting, once weekly oxyntomodulin analog for the treatment of type 2 diabetes and obesity.

About Diabetes & Obesity

Diabetes is a group of metabolic disorders that hamper the body's ability to produce or respond to the hormone insulin resulting in high blood sugar levels over a prolonged period. Type 1 diabetes results from the pancreas's failure to produce enough insulin. Type 2 diabetes begins with insulin resistance, a condition in which cells fail to respond to properly to insulin. Both type 1 and 2 diabetes results in long-term complications encompassing cardiovascular disease, stroke, chronic kidney disease, foot ulcers and damage to the eyes. Acute complications can include diabetic ketoacidosis (a high and dangerous level of acids called ketones in the blood), hyperosmolar hyperglycemic state (high level of blood sugars that can cause coma) or death. As of 2012, there are 29.3 million Americans, or 9.35% of the population suffering from diabetes, up from .93% in 1958 and 4.7% in 1980. There are also currently 79 million Americans that are considered insulin resistant. Internationally, over 380 million people suffer from diabetes. One reason for the sharp rise in diabetes in the U.S. has been the dramatic rise in obesity.

Obesity has become a major health issue in recent decades, resulting in diseases such as coronary heart disease, chronic kidney disease, and diabetes. The U.S. has one of the world's highest rates of obesity. In 2010, the Centers for Disease Control and Prevention (CDC) reported that 35.7% of American adults were obese and 17% of American children. Obesity has been cited as a contributing factor in approximately 100,000-400,000 deaths a year and direct and indirect costs to society of $117 billion, which exceeds the healthcare costs of tobacco, and accounts for 6-12% of national healthcare expenditures in the U.S. According to the World Health Organization, there are more than 500 million severely overweight or obese people.

OPK88003 (Oxyntomodulin) for Diabetes and Obesity

OPK88003 (Oxyntomodulin), a once weekly administered peptide for the treatment of type 2 diabetes and associated obesity, is a dual agonist of the GLP-1 (glucagon-l-ike peptide-1) and glucagon receptors. The receptors play an integral role in regulating appetite, food intake, satiety, lipid metabolism and energy utilization in the body. Stimulating both of the receptors, OPK88003 has the potential to regulate both food intake and blood glucose.

OPK88003 has been studied in a Phase 2 clinical trial enrolling 420 type 2 diabetes patients. Subjects receiving the highest dose of OPK88003 (Oxyntomodulin) once weekly demonstrated statistically significant weight loss compared with currently approved long-acting exenatide. OPK88003 also provided a reduction in glycosylated hemoglobin (HbA1c or A1c), a marker of sugar metabolism, similar to exenatide. ˹ initiated a Phase 2b dose-escalation clinical trial study for OPK88003 to optimize a dosing regimen that will increase weight loss and reduce HbA1c in diabetes patients in March 2018, this study was completed in 2019. This recent dosing regimen study showed improved weight loss (5.4 Kg), HbA1c (1.4) and lipid profile vs metformin. A more prominent decrease in triglycerides and total cholesterol was observed with OPK-88003 treatment compared to the GLP-1 incretin therapy in a previous phase 2 study.


Of the American population suffers from diabetes1


Direct medical costs related to diabetes in the U.S.1


Adults diagnosed with diabetes reported taking any medication2



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