Semaglutide (trade name Ozempic) is a pharmaceutical drug in development by a Danish company Novo Nordisk for the treatment of type 2 diabetes. Semaglutide is a once-daily glucagon-like peptide-1 analog that differs to others by the presence of an acyl group with a steric diacid at Lys26 and a large synthetic spacer and modified by the presence of a α-aminobutyric acid in position 8 which gives stability against the dipeptidylpeptidase-4. Semaglutide is a GLP-1 analogue with 94% sequence homology to human GLP-1. Semaglutide acts as a GLP-1
receptor agonist that selectively binds to and activates the GLP-1 receptor, the target for native GLP-1.
GLP-1 is a physiological hormone that has multiple actions on glucose, mediated by the GLP-1 receptors.
The principal mechanism of protraction resulting in the long half-life of semaglutide is albumin binding, which
results in decreased renal clearance and protection from metabolic degradation. Furthermore, semaglutide is
stabilized against degradation by the DPP-4 enzyme.
Semaglutide reduces blood glucose through a mechanism where it stimulates insulin secretion and lowers
glucagon secretion, both in a glucose-dependent manner. Thus, when blood glucose is high, insulin secretion is
stimulated and glucagon secretion is inhibited. The mechanism of blood glucose lowering also involves a minor
delay in gastric emptying in the early postprandial phase.
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Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
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OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
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Drug as perpetrator
Tox targets
PubMed
Sample Use Guides
Start at 0.25 mg once weekly. After 4 weeks, increase the dose to 0.5 mg once weekly. If after at least 4 weeks additional glycemic control is needed, increase to 1 mg once weekly (2.1).
Administer once weekly at any time of day, with or without meals (2.1).
If a dose is missed administer within 5 days of missed dose (2.1).
Inject subcutaneously in the abdomen, thigh, or upper arm (2.2).
Route of Administration:
Other
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