Tesamorelin — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Tesamorelin, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| GHRH receptor (GHRHR) | Agonist | Pituitary somatotroph receptor; stimulates pulsatile endogenous growth hormone release |
§2.2Mechanism of action
Tesamorelin stimulates the pituitary to release endogenous growth hormone in a pulsatile pattern, preserving the physiological feedback architecture that exogenous growth hormone bypasses. Downstream IGF-1 elevation drives lipolysis with a preferential effect on visceral adipose tissue. Because feedback is intact, the risk of the supraphysiological IGF-1 exposure associated with exogenous growth hormone is reduced, though not abolished.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈26–38 min
- Time to maximum concentration
- ≈0.15 h
- Volume of distribution
- ≈9.4 L/kg
- Plasma protein binding
- not extensively bound
- Clearance
- ≈30–40 L/h
- Bioavailability
- ≈4 % (subcutaneous, in healthy subjects)
Rapid proteolytic degradation. The short half-life is not a limitation because the pharmacodynamic effect is mediated by a downstream hormone cascade with its own kinetics.
§2.4Interactions
- Cortisol conversion — growth hormone inhibits 11β-hydroxysteroid dehydrogenase type 1 and may unmask central hypoadrenalism
- Cytochrome P450 substrate metabolism may be modestly altered by growth hormone
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.
- Falutz J, Allas S, Blot K, Potvin D, Kotler D, Somero M, Berger D, Brown S, Richmond G, Fessel J, Turner R, Grinspoon S. Metabolic effects of a growth hormone-releasing factor in patients with HIV. New England Journal of Medicine 2007;357(23):2359–2370. doi:10.1056/NEJMoa072375 · PMID 18052660
- Prakash A, Goa KL. Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency. BioDrugs 1999;12(2):139–157. doi:10.2165/00063030-199912020-00007 · PMID 18031173
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.