Pharmacokinetics in animal models
A study in beagle dogs examined plasma levels of a dry powder formulation by radioimmunoassay, with bioavailability, terminal half-life and mean residence time as endpoints2.
Sources [2]
Research Peptide · For laboratory research use only
Tesamorelin
Also known as TH9507
- Formula
- C221H366N72O67S
- CAS
- 218949-48-5
Available as
Certificates of analysis
Overview
Tesamorelin (development code TH9507) is a synthetic 44-residue analogue of human growth hormone-releasing factor (GRF, also GHRH)1,2. PubChem lists it as N-[(3E)-hex-3-enoyl] somatoliberin: the full 1-44 sequence of human GRF with a trans-3-hexenoyl group on the N-terminal tyrosine.
It has been characterised in pharmacokinetic studies in dogs2, in in vitro metabolism and anti-doping detection work3, and in registered clinical trials, which are described here by design and primary endpoint only4,5.
Mechanism of action
As described in the research literature
As described in the research literature, tesamorelin was developed as one of a group of GRF analogues intended to stimulate endogenous growth hormone secretion, as an alternative approach to recombinant human growth hormone1.
In male beagle dogs, plasma levels were measured by radioimmunoassay, and bioavailability, terminal half-life and mean residence time were reported2. In vitro incubation studies identified major metabolites of tesamorelin and related GRF analogues, which were synthesised as reference materials for a urine LC-MS/MS detection method3. Paired liver biopsy specimens from a registered trial have also been used for hepatic gene set enrichment analysis comparing tesamorelin with placebo6.
Research areas
What published studies have examined
Metabolism and analytical detection
In vitro metabolism of sermorelin, tesamorelin and two CJC-1295 forms was characterised, and nineteen major metabolites were synthesised and used to develop an LC-MS/MS method for detecting GRF analogues in urine3.
Sources [3]
Registered clinical trials
A multicentre, randomised, placebo-controlled trial in adults with HIV and abdominal fat accumulation used percent change from baseline in visceral adipose tissue on computed tomography as its primary end point (NCT00123253)4. A randomised, double-blind, multicentre trial in people with HIV and non-alcoholic fatty liver disease used change in hepatic fat fraction between baseline and 12 months as its primary endpoint (NCT02196831)5, and paired liver biopsies from that trial were used for transcriptomic analysis6.
Development overview
A 2009 review describes the development of tesamorelin as a GRF analogue and the indications that had been considered for it1.
Sources [1]
Specifications
- Sequence
- trans-3-Hexenoyl-YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL-NH2 (human GRF 1-44 amide, N-terminally acylated)
- Molecular formula
- C221H366N72O67S
- Molecular weight
- 5135.8 g/mol
- CAS number
- 218949-48-5
- Form
- White to off-white lyophilised powder in a sealed vial (10 mg)
- Storage
- Store lyophilised powder at -20 °C, protected from light and moisture. Once reconstituted, keep refrigerated at 2 to 8 °C and protect from light.
- Solubility and reconstitution
- Reconstitute with bacteriostatic water. Add the diluent slowly down the inside wall of the vial and swirl gently until clear; do not shake.
References
- 1
Tesamorelin, a human growth hormone releasing factor analogue.
Wang Y, Tomlinson B Expert Opinion on Investigational Drugs, 2009.
- 2
Pulmonary delivery of TH9507, a growth hormone releasing factor analogue, in the dog.
Jansen M, Darby I, Abribat T, et al. International Journal of Pharmaceutics, 2004.
- 3
Advances in the detection of growth hormone releasing hormone synthetic analogs.
Memdouh S, Gavrilović I, Ng K, et al. Drug Testing and Analysis, 2021.
- 4
Metabolic effects of a growth hormone-releasing factor in patients with HIV.
Falutz J, Allas S, Blot K, et al. The New England Journal of Medicine, 2007.
- 5
Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial.
Stanley TL, Fourman LT, Feldpausch MN, et al. The Lancet HIV, 2019.
- 6
Effects of tesamorelin on hepatic transcriptomic signatures in HIV-associated NAFLD.
Fourman LT, Billingsley JM, Agyapong G, et al. JCI Insight, 2020.
This page is provided for research and educational reference only. It does not constitute medical advice, dosing guidance, or a recommendation for use. All compounds are strictly for laboratory and in-vitro research purposes.