Albiglutide
GLP-1 receptor agonist fused to human albumin for once-weekly type 2 diabetes treatment with reduced immunogenicity.
Chemical Identity
| Property | Value |
|---|---|
| Molecular Weight | ~73 kDa |
| CAS Number | 782500-75-8 |
| Peptide Class | GLP-1 Receptor Agonist (Albumin Fusion) |
| Structure | 2x GLP-1(7-36) fused to human albumin |
| Route | SC injection |
Structure
Albiglutide (Tanzeum) is a recombinant fusion protein consisting of two tandem copies of modified GLP-1(7-36) fused to human serum albumin. The GLP-1 sequence contains an Aib substitution at position 8 for DPP-4 resistance. Albumin fusion provides extended half-life through albumin recycling.
Mechanism of Action
Albiglutide activates GLP-1 receptors, enhancing glucose-dependent insulin secretion and suppressing glucagon. The albumin fusion provides a 5-day half-life with reduced immunogenicity compared to Fc fusion proteins. Lower CNS penetration may explain reduced GI side effects and weight loss.
Clinical Applications
- Type 2 diabetes: Glycemic control (Tanzeum) - withdrawn from market 2018
- Cardiovascular outcomes: HARMONY trial showed CV benefit
- Weight loss: Modest (0.6-1.1 kg)
- Historical significance: Demonstrated albumin fusion approach
Pharmacokinetics
- Half-life: 5 days
- Tmax: 3-5 days
- Bioavailability: 36-49%
- Metabolism: Proteolytic degradation
- Dosing: 30-50 mg SC once weekly
- Route: SC injection
Safety and Side Effects
Nausea (8-11%), diarrhea (6-10%), injection site reactions (10-18%), upper respiratory infections, and arthralgia. Lower GI side effects compared to other GLP-1 RAs. Discontinued commercially in 2018.
References
- Pratley, R.E., et al. (2014). HARMONY-5: albiglutide for type 2 diabetes. Lancet Diabetes & Endocrinology, 2, 470-478.
- Hernandez, A.F., et al. (2018). HARMONY Outcomes: albiglutide and cardiovascular events. Lancet, 392, 1519-1529.
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