An overview of oral antidiabetics
Oral antidiabetics are primarily used for the treatment of patients with type 2 diabetes mellitus (T2DM), although researchers are now investigating whether patients with type 1 diabetes would also benefit from using these types of drug in addition to their usual insulin regimen.
Metformin, an insulin sensitizer, is one of the most widely used and studied antidiabetic agents. It was shown to improve glucose control by reducing hepatic glucose output and improving insulin sensitivity. While it is regarded as the primary oral treatment option for overweight patients with T2DM, monotherapy is often insufficient when the disease progresses. Add-on therapies include insulin products or other oral antidiabetics, such as sulfonylureas, PPAR-gamma agonists, DPP-IV inhibitors or SGLT-2 inhibitors.
DPP-IV inhibitors, such as sitagliptin, saxagliptin and linagliptin, prevent the breakdown of incretins by blocking the enzymatic activity of DPP-IV. This enhances meal-induced insulin secretion. This drug class has great potential for improving glycemic control with a low risk of hypoglycemia and minimal effects on weight gain so that it can safely be combined with insulin.
SGLT-2 inhibitors, such as canagliflozin or empagliflozin, are a relatively new class of antidiabetics. They selectively inhibit the sodium glucose transporter 2 (SGLT-2) in the kidneys, causing an increase in urinary glucose excretion. This drug class was shown to improve glycemic control accompanied by reduction of body weight and blood pressure in patients with T2DM either as monotherapy or as add-on therapy to insulin treatment.
New approaches use dual inhibition of the SGLT-2 transporter and the SGLT-1 transporter of the intestine. The latter regulates glucose and galactose uptake after a meal. T2DM subgroups, such as patients with renal impairment, may benefit from dual SGLT-1/-2 dual inhibition. It was recently reported that post-prandial glucose excursions and increased GLP-1 production increased in this subgroup despite the expected reduction in urinary glucose excretion.
Several cardiovascular outcome trials have shown reduced mortality in people with type 2 diabetes at high risk for cardiovascular disease, through diminished occurence of heart failure.
Antidiabetic studies at Profil
Profil has been involved with trials and research into every class of antidiabetics developed since 1999. Our researchers have conducted numerous pharmacokinetic, pharmacodynamic
and mode of action studies to elucidate the effects of various oral antidiabetics. The focus of this research has been the efficacy, safety and dose–response of the drug and its performance as an add-on therapy compared to other diabetes treatments.