Incretin hormones are peptides released in the intestine in response to the 
presence of nutrients in its lumen. The main incretins are glucagon-like 
peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). GLP-1 
stimulates insulin secretion, inhibits glucagon secretion at pancreatic α cells 
and has also extrapancreatic influences as slowing of gastric emptying which 
increases the feeling of satiety. GIP is the main incretin hormone in healthy 
people, causative of most the incretin effects, but the insulin response after 
GIP secretion in type 2 diabetes mellitus (T2DM) is strongly reduced. Therefore, 
in the past GIP has been considered an unappealing therapeutic target for T2DM. 
This conception has been changing during recent years, since it has been 
reported that resistance to GIP can be reversed and its effectiveness restored 
by improving glycemic control. This fact paved the way for the development of a 
GIP receptor agonist-based therapy for T2DM, looking also for the possibility of 
finding a combined GLP-1/GIP receptor agonist. In this framework, the novel dual 
GIP and GLP-1 receptor agonist tirzepatide seems to be not just a new 
antidiabetic medication. Administered as a subcutaneous weekly injection, it is 
a manifold single pharmacological agent that has the ability to significantly 
lower glucose levels, as well as improve insulin sensitivity, reduce weight and 
amend dyslipidemia favorably modifying the lipid profile. Tirzepatide and 
additional dual GLP-1/GIP receptor agonists that could eventually be developed 
in the future seem to be a promising furthest advance for the management of 
several cardiometabolic settings. Obviously, it is too early to be overly 
hopeful since it is still necessary to determine the long-term effects of these 
compounds and properly verify the potential cardiovascular benefits. Anyway, we 
are currently facing a novel and very appealing therapeutic option.