Lixisenatide — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Lixisenatide, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| GLP-1 receptor (GLP1R) | Full agonist | Affinity approximately four-fold higher than native GLP-1 |
§2.2Mechanism of action
A short-acting prandial GLP-1 receptor agonist. Its dominant pharmacodynamic effect is marked slowing of gastric emptying, which produces substantial postprandial glucose reduction with comparatively modest effects on fasting glucose and HbA1c. This makes it mechanistically complementary to basal insulin, which is the basis of the fixed-combination products.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈3 h
- Time to maximum concentration
- 1–3.5 h
- Volume of distribution
- ≈100 L
- Plasma protein binding
- ≈55 %
- Clearance
- ≈35 L/h
- Bioavailability
- not formally reported
Glomerular filtration with proteolytic degradation. Exposure rises with declining renal function and use is not recommended below an eGFR of 15 mL/min/1.73 m².
§2.4Interactions
- Oral medicines requiring rapid absorption — administer at least 1 hour before lixisenatide
- Sulfonylureas and basal insulin — hypoglycaemia
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- Pfeffer MA, Claggett B, Diaz R, Dickstein K, Gerstein HC, Køber LV, Lawson FC, Ping L, Wei X, Lewis EF, Maggioni AP, McMurray JJV, Probstfield JL, Riddle MC, Solomon SD, Tardif JC. Lixisenatide in patients with type 2 diabetes and acute coronary syndrome. New England Journal of Medicine 2015;373(23):2247–2257. doi:10.1056/NEJMoa1509225 · PMID 26630143
- Drucker DJ. Mechanisms of action and therapeutic application of glucagon-like peptide-1. Cell Metabolism 2018;27(4):740–756. doi:10.1016/j.cmet.2018.03.001 · PMID 29617641
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.