Tesamorelin

Overview

Tesamorelin is a synthetic 44-amino-acid analog of native human growth hormone releasing hormone (GHRH), modified at the N-terminus with a trans-3-hexenoic acid moiety that confers resistance to dipeptidyl peptidase-IV (DPP-IV) degradation. The compound has been studied in preclinical and clinical research models for its role in GHRH-R-mediated pathway activation and visceral adipose tissue research (Falutz et al., 2007 — PMID: 17971457).

History

Tesamorelin was developed by Theratechnologies as a stabilized GHRH analog designed to overcome the short plasma half-life of native GHRH(1-29). Research has historically focused on metabolic pathway investigations, including studies characterizing changes in body composition parameters in HIV-associated lipodystrophy research models, as well as broader investigations of GH/IGF-1 axis dynamics (Dhillon, 2011).

Structure & Molecular Data

CAS Number	901758-09-6
Molecular Formula	C₂₂₁H₃₆₆N₇₂O₆₇S
Molecular Weight	5,135.79 g/mol
Amino Acid Count / Structure	44-amino-acid GHRH analog with N-terminal modification
PubChem CID	16137828
Sequence	trans-3-hexenoyl-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH₂
Appearance	Lyophilized white powder
Storage	Store at -20°C. Refrigerate post-reconstitution for research use.
Solubility	Soluble in sterile water and bacteriostatic water for research preparation

 

Compound Class & Mechanism

Tesamorelin binds to the GHRH receptor (GHRH-R) on anterior pituitary somatotrophs, activating cAMP-PKA signaling cascades in preclinical models. This pathway activation has been associated with pulsatile growth hormone release patterns and downstream IGF-1 pathway modulation in experimental settings.

The N-terminal hexenoic acid modification provides DPP-IV resistance, extending plasma stability relative to native GHRH(1-29). Research has characterized pharmacodynamic effects on visceral adipose tissue (VAT) parameters in preclinical and clinical investigation models, with particular focus on the mechanistic relationship between pulsatile GH elevation and adipose tissue metabolism (Falutz et al., 2007).

Research Findings

Tesamorelin has been investigated in preclinical and clinical research spanning metabolic, body composition, and endocrine systems. Published research has documented findings in the following domains:

Key Research Areas

• Adipose Tissue Research: visceral adipose tissue dynamics in metabolic research models
• GH/IGF-1 Axis: pulsatile GH release, IGF-1 response patterns in research protocols
• Metabolic Pathway Research: glucose and lipid metabolism in preclinical models
• Comparative GHRH Analog Studies: stability and selectivity profiles versus other GHRH analogs

Collectively, the research literature surrounding Tesamorelin has positioned it as a widely referenced GHRH-R agonist for investigating the relationship between GH axis activation and metabolic endpoints in controlled research settings (Stanley & Grinspoon, 2015).

Research Context

Researchers study Tesamorelin to investigate GHRH-R pharmacology, adipose tissue biology, and the metabolic consequences of pulsatile GH release. Its extended stability profile relative to native GHRH(1-29) makes it a frequently referenced tool in research designs requiring prolonged receptor activation while preserving endogenous pulsatile characteristics.

References

Falutz J. et al. (2007). Metabolic effects of a growth hormone-releasing factor in patients with HIV. NEJM. PMID: 17971457

Dhillon S. (2011). Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy. Drugs.

Stanley TL., Grinspoon SK. (2015). Effects of growth hormone-releasing hormone on visceral fat, metabolic, and cardiovascular indices. Growth Hormone & IGF Research.

Ferdinandi ES. et al. (2007). Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic & Clinical Pharmacology & Toxicology.

Clemmons DR. et al. (2017). Long-term effects of tesamorelin in HIV-infected patients with abdominal fat accumulation. Clinical Infectious Diseases.

Koutkia P. et al. (2004). Growth hormone-releasing hormone in HIV-infected men with lipodystrophy. JAMA.

 

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