Liraglutide

Also known as: Victoza, Saxenda, NN2211

Evidence: Clinical

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Overview

Once-daily acylated GLP-1 analog; FDA-approved for type 2 diabetes (2010) and obesity (2014), with generics since 2024. In SCALE, 3 mg lost 8.4 kg over 56 weeks versus 2.8 kg on placebo.

Liraglutide (NN2211) is a GLP-1(7-37) analog from Novo Nordisk with Lys34 replaced by Arg and a palmitic acid on Lys26 through a glutamic acid spacer, which allows albumin binding and once-daily dosing (Knudsen 2000). In SCALE Obesity, 3 mg daily gave 8.4 kg weight loss over 56 weeks versus 2.8 kg with placebo (Pi-Sunyer 2015). In LEADER, it cut major cardiovascular events in type 2 diabetes (Marso 2016). FDA approved Victoza for type 2 diabetes in 2010 and Saxenda for weight in 2014, including adolescents from 12 years. Generic liraglutide has been approved since 2024 and is marketed alongside both brands.

Benefits

Weight loss (human RCT, 3 mg daily), improved glycemic control in type 2 diabetes (approved use), fewer major cardiovascular events in type 2 diabetes (human RCT)

Dosing reference

Research dose: 0.6-3mg daily
Range: 600 to 3000 mcg, 1x daily
Common vial sizes: 6 mg, 18 mg

Subcutaneous, once daily, in the abdomen, thigh or upper arm. Saxenda label titration starts at 0.6 mg daily and rises by 0.6 mg each week to 3 mg; Victoza for type 2 diabetes uses 1.2 to 1.8 mg daily. Approved products are prefilled pens (18 mg/3 mL), not vials.

Mechanism

Liraglutide is a GLP-1 analog with 97% sequence homology to native GLP-1(7-37), made by substituting arginine for lysine at position 34 and attaching palmitic acid through a glutamic acid spacer at Lys26 (Saxenda label). It activates the GLP-1 receptor, raising glucose-dependent insulin secretion, lowering glucagon, delaying gastric emptying and reducing appetite. Self-association and albumin binding slow absorption and protect it from DPP-4 and neutral endopeptidase, extending plasma half-life from 1.5 to 2 minutes for native GLP-1 to about 13 hours (Knudsen 2000; label).

Evidence

Clinical: at least one published human trial or an approved drug

SCALE Obesity (n=3731, 56 weeks): 3 mg daily gave 8.4 kg weight loss versus 2.8 kg with placebo; 63.2% versus 27.1% lost at least 5% (Pi-Sunyer et al., 2015)
LEADER (n=9340, type 2 diabetes, median 3.8 years): major cardiovascular events 13.0% versus 14.9%, hazard ratio 0.87; cardiovascular death hazard ratio 0.78 (Marso et al., 2016)
Healthy men: subcutaneous half-life 12.6 h with dose-proportional exposure (Agersø et al., 2002)
Designed by fatty-acid acylation of GLP-1 for once-daily PK (Knudsen et al., 2000)
Status: FDA-approved and marketed. Victoza (type 2 diabetes, 2010), Saxenda (weight, 2014); generic liraglutide approved from 2024

References

Side effects

Nausea, vomiting, diarrhea, and constipation are the most common effects and are generally worst during dose escalation. Pancreatitis, gallbladder disease, and increased heart rate are reported risks, and delayed gastric emptying raises aspiration risk under anesthesia. Contraindicated with a personal or family history of medullary thyroid carcinoma or MEN2.

Storage

Storage: Refrigerated (2-8°C)
Lyophilized: 24+ months refrigerated
Reconstituted: 30 days at room temp after first use

Pharmacology

Half-life: ~13 h (subcutaneous, Saxenda label); 12.6 h in healthy men (Agersø 2002)
Bioavailability: Subcutaneous: ~55%
Molecular weight: 3751.2 Da
Sequence: HAEGTFTSDVSSYLEGQAAK[gamma-Glu-palmitoyl]EFIAWLVRGRG