Semaglutide

GLP-1 Receptor AgonistFDA-approved

Also known as: Ozempic, Wegovy, Rybelsus, NN9535

An FDA-approved GLP-1 receptor agonist used for type 2 diabetes and chronic weight management, producing significant weight loss of 15-17% body weight in clinical trials.

Overview

Semaglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist originally developed by Novo Nordisk for type 2 diabetes (marketed as Ozempic) and later approved at a higher dose for chronic weight management (Wegovy). It is a modified analog of human GLP-1 with 94% structural homology, engineered with key amino acid substitutions and a fatty acid side chain that dramatically extends its half-life to approximately 7 days, allowing once-weekly dosing. Semaglutide has become one of the most prescribed and culturally prominent peptide drugs in history, catalyzing the 'GLP-1 revolution' in obesity treatment. Beyond weight loss and glycemic control, emerging research suggests cardiovascular benefits, potential neuroprotective effects, and applications in addiction, liver disease (MASH/NASH), and kidney disease. An oral formulation (Rybelsus) is also available, making it one of the first oral peptide drugs.

Mechanism of Action

Semaglutide mimics the incretin hormone GLP-1, acting through multiple mechanisms: (1) Stimulates glucose-dependent insulin secretion from pancreatic beta cells, lowering blood sugar only when glucose is elevated; (2) Suppresses glucagon secretion, reducing hepatic glucose output; (3) Slows gastric emptying, prolonging satiety after meals; (4) Acts on hypothalamic GLP-1 receptors to reduce appetite and food intake centrally; (5) May improve beta-cell function and survival over time; (6) Reduces cardiovascular inflammation and atherosclerosis markers; (7) Emerging evidence for direct effects on reward circuitry in the brain, potentially reducing cravings for food and addictive substances.

Molecular Formula

C187H291N45O59

Molecular Weight

4113.58 g/mol

Sequence

Modified GLP-1 analog (His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(C18 fatty diacid)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly)

Dosage Protocols

Dose Range

0.25mg2mg

Frequency

Once weekly

Route

subcutaneous

Cycle Length

Ongoing (chronic therapy)

Start at 0.25mg for 4 weeks, escalate to 0.5mg, then optionally to 1mg or 2mg. Inject in abdomen, thigh, or upper arm. Rotate injection sites.

Source: FDA prescribing information (Ozempic)

Side Effects

EffectSeverity
Nauseamoderate
Vomitingmoderate
Diarrheamild
Constipationmild
Injection site reactionsmild
Pancreatitissevere
Gallbladder eventssevere
Thyroid C-cell tumorssevere
Muscle lossmoderate
Gastroparesismoderate

Pros & Cons

Produces the most significant weight loss of any approved pharmaceutical — average 15-17% body weight reduction

FDA-approved with extensive Phase 3 clinical trial data (STEP and SUSTAIN programs) in thousands of patients

Proven cardiovascular benefits — reduced MACE events by 20% in the SELECT trial

Once-weekly dosing provides excellent convenience and adherence

Dual benefits for weight loss and blood sugar control in diabetic patients

Significant GI side effects (nausea, vomiting) especially during dose escalation, causing ~7% discontinuation rate

Weight regain is common after discontinuation — two-thirds of lost weight may return within a year

High cost without insurance ($1,000-1,300/month) and frequent insurance coverage issues for weight loss indication

Loss of lean muscle mass alongside fat, requiring deliberate resistance training to mitigate

Supply shortages have been persistent since 2022 due to overwhelming demand

Research Studies

Legal Status

FDA-approved for type 2 diabetes (Ozempic, 2017) and chronic weight management (Wegovy, 2021). Prescription required. Available as oral formulation (Rybelsus). Covered by many insurance plans for diabetes; weight loss coverage varies.

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