Arhalofenate: Effects, Uses & Risks

Once clinical development is complete and the arhalofenate compound has the necessary clearances, it will be used in the treatment of type 2 diabetes. In animal studies, it has been shown to effectively lower not only blood glucose levels but also triglyceride levels in the bloodstream. However, this mechanism is still largely unexplored.

What is arhalofenate?

Once clinical development is complete and the drug arhalofenate has the necessary approvals, it is expected to be used in the treatment of type 2 diabetes. The drug arhalofenate is currently still in clinical development and is expected to be used in the future as an antidiabetic agent for patients suffering from type 2 diabetes. This drug is a so-called partial agonist, which occupies a specific receptor according to the lock-and-key principle and partially replaces or mimics a transmitter. Unlike agonists, partial agonists are not able to completely trigger the desired effect in a cell. Partial agonists such as arhalofenate are developed when the maximum effect that can be achieved with an antagonist is not desired in therapy, for example for safety reasons. The US company Metabolex is responsible for the clinical development of the compound. To date, it has already been demonstrated in animal studies that the compound can lower blood glucose levels as well as triglyceride levels in the blood.

Pharmacological effect

The active ingredient arhalofenate is a prodrug. This means that arhalofenate in itself has no pharmacological effect. This unfolds only after it has been converted by metabolism into an active ingredient. Arholfenat achieves the desired effect via peroxisome proliferator-activated receptors, which are located directly in the cell nucleus and regulate a large number of genes here. These receptors are activated via so-called ligands, which bind specifically to a certain receptor. Unlike substrates, ligands cannot be converted by the respective target molecule. However, they can change the molecular structure of the target molecule. Animal studies have shown that arhalofenate can effectively lower blood glucose levels. It thus acts indirectly on insulin, which is produced in the pancreas and has the primary task in the human body of lowering blood glucose levels. This is done by insulin stimulating the cells to absorb more glucose from the blood. As a further effect, it has been observed that arhalofenate can also lower blood triglyceride levels. Blood triglyceride levels play an important role in the diagnosis of diseases. For example, an elevated triclycerol level may indicate that a metabolic disorder or other disease, such as kidney disease, is present. However, the mechanism by which arhalofenate lowers triglyceride levels is still unknown.

Medicinal application and use

Once clinical trials are completed and arhalofenate is approved, it will be used to treat patients with type 2 diabetes-also known as diabetes mellitus. This condition, popularly known as diabetes, is a metabolic disease. Among other things, it is manifested by the symptom that sugar is excreted in the urine. Based on this symptom, the English physician Thomas Willis was able to diagnose diabetes in 1645 using taste samples of urine. Type 2 diabetes is a collective term for various metabolic disorders that have hyperglycemia as a leading finding. In affected patients, the regulation of the nutrient glucose is disturbed. In the early stages, patients often complain of a dry mouth and a relatively great feeling of thirst. If the disease is not treated, visual disturbances and, in extreme cases, even hyperglycemic coma may occur in the further course. This occurs when there is a relative lack of insulin and requires immediate treatment by hospitalization. The long-term consequences of untreated diabetes can include further illnesses, such as loss of vision, kidney weakness or even a stroke. Diabetes is treated by medical regulation of glucose levels.For example, by administering insulin or by stimulating the body’s own insulin production.

Risks and side effects

Because arhalofenate is still in the clinical development stage, there are no known risks or side effects as yet.