Products
Dulaglutide was approved as a solution for injection in many countries in 2015 (Trulicity).
Structure and properties
Dulaglutide (ATC A10BJ05) is a fusion protein consisting of two identical chains linked by disulfide bridges. The chains contain:
- The GLP-1 analog (sequence segment 7-37), which is 90% the same as the natural GLP-1 segment. It has been modified so that it is not degraded by dipeptidyl peptidase 4 (DPP-4).
- A linker
- A human IgG4 Fc domain
The molecular weight is approximately 63 kDa. These modifications are primarily to extend the half-life to 5 days.
Effects
Dulaglutide (ATC A10BJ05) has antidiabetic and antihyperglycemic properties. The effects are due to binding to the GLP-1 receptor, a GPCR (G protein-coupled receptor). This receptor is also activated by the incretin GLP-1. GLP-1 receptor agonists:
- Promote insulin secretion from pancreatic beta cells.
- Decrease glucagon secretion from alpha cells, resulting in decreased glucose release by the liver (lowering gluconeogenesis).
- Increase insulin sensitivity.
- Slow gastric emptying, reducing the rate at which glucose enters the bloodstream.
- Increase satiety (central), reduce the feeling of hunger and may contribute to weight loss.
GLP-1 receptor agonists tend to cause less hypoglycemia because their effect does not occur until glucose levels are elevated. The orally available gliptins (see there) inhibit the breakdown of GLP-1, thereby enhancing its effects.
Indications
For the treatment of type 2 diabetes.
Dosage
According to the SmPC. The drug is injected subcutaneously once a week, regardless of meals.
Contraindications
Dulaglutide is contraindicated in cases of hypersensitivity. For complete precautions, see the drug label.
Interactions
Dulaglutide slows gastric emptying and therefore may affect the absorption of other agents.
Adverse effects
The most common possible adverse effects include nausea, diarrhea, vomiting, and abdominal pain.
