Teduglutide — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Teduglutide, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| GLP-2 receptor (GLP2R) | Agonist | Expressed on intestinal subepithelial myofibroblasts and enteric neurons rather than on enterocytes directly |
§2.2Mechanism of action
GLP-2 receptor agonism promotes intestinal mucosal growth, increases villus height and crypt depth, slows gastric emptying and reduces intestinal secretion. The therapeutic consequence in short-bowel syndrome is improved fluid and nutrient absorption and reduced dependence on parenteral support. The trophic mechanism is also the source of the principal safety concern: any agent that promotes intestinal mucosal proliferation carries a theoretical neoplasia risk that requires colonoscopic surveillance.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈2 h in adults
- Time to maximum concentration
- 3–5 h
- Volume of distribution
- ≈26 L
- Plasma protein binding
- not extensively bound
- Clearance
- ≈123 mL/h/kg
- Bioavailability
- ≈88 %
Renal clearance with proteolytic degradation. Dose reduction is required in moderate and severe renal impairment.
§2.4Interactions
- Increased absorption of oral medicines including benzodiazepines, psychotropics and narrow-therapeutic-index agents — dose reduction may be needed
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.
- 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
- Müller TD, Finan B, Bloom SR, D’Alessio D, Drucker DJ, Flatt PR, Fritsche A, Gribble F, Grill HJ, Habener JF, Holst JJ, Langhans W, Meier JJ, Nauck MA, Perez-Tilve D, Pocai A, Reimann F, Sandoval DA, Schwartz TW, Seeley RJ. Glucagon-like peptide 1 (GLP-1). Molecular Metabolism 2019;30:72–130. doi:10.1016/j.molmet.2019.09.010 · PMID 31767182
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.