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Hormones & Endocrine SignalingStabilised GHRH analogue — human GHRH(1-44) amide, N-terminally acylated

Tesamorelin

A stabilized growth hormone-releasing peptide approved to target visceral organ fat without shutting down natural hormone production.

ApprovedApproved PharmaceuticalAlso known as: Egrifta, TH9507, Tesamorelin acetateSkip to Human Evidence ↓
Endocrine Pathway Visualizer

The Hypothalamic–Pituitary–Liver Axis

FDA-Approved for HIV Lipodystrophy

Tesamorelin is a stabilized GHRH analogue that mimics the brain's natural trigger for growth hormone, targeting visceral abdominal fat while preserving natural hormonal feedback loops.

1

Pituitary GHRH

Binds pituitary somatotrophs, activating cAMP signaling.

2

Pulsatile GH

Stimulates natural pulses rather than constant supraphysiological flooding.

3

Liver IGF-1

GH reaches liver, prompting physiologic IGF-1 synthesis (+81%).

4

Visceral Lipolysis

Selectively triggers fat breakdown in deep abdominal organ deposits (-15.2%).

Preservation of Somatostatin Feedback: Direct growth hormone injections bypass the brain and suppress natural pituitary function. In contrast, tesamorelin works through the pituitary, allowing somatostatin to halt hormone release if levels become too high.
1

What is Tesamorelin?

Tesamorelin is a synthetic peptide that mimics human Growth Hormone-Releasing Hormone (GHRH). It consists of the first 44 amino acids of natural GHRH bonded to a trans-3-hexenoic acid group, which stabilizes the peptide and extends its activity in the body.

2

Why are people interested in it?

Interest in tesamorelin centers on its unique ability to reduce deep visceral abdominal fat (the dangerous fat packed around internal organs) without broadly shutting down the body's natural hormone production or spiking blood sugar the way synthetic growth hormone injections can.

Primary Research Categories

  • GHRH analogues
  • Approved drug substances
3

How does it work in the body?

Tesamorelin acts on the pituitary gland to encourage your body to manufacture and release its own natural growth hormone in normal, healthy pulses.

In Everyday Language: Rather than injecting artificial growth hormone directly, tesamorelin gently taps your pituitary gland on the shoulder, encouraging your body to release its own natural pulses of growth hormone in a balanced rhythm.
Cellular & Receptor Signaling: Trans-3-hexenoyl GHRH(1-44) amide binds specifically to pituitary GHRH receptors on somatotroph cells. This activates adenylyl cyclase and cAMP signaling, triggering episodic pulsatile secretion of endogenous growth hormone, which stimulates liver IGF-1 synthesis and selective visceral fat lipolysis while preserving somatostatin feedback inhibition.

Endocrine Pathway

The GHRH – Pituitary – IGF-1 Axis

Physiological Somatotropic Regulation

Instead of injecting direct growth hormone, GHRH analogues prompt the body’s own pituitary gland to manufacture and release growth hormone in natural, pulsatile bursts.

Step 1

GHRH Analogue

Tesamorelin enters circulation and binds GHRH receptors on anterior pituitary somatotrophs.

Step 2

Pulsatile GH

Stimulates natural, episodic pulses of endogenous human growth hormone (GH).

Step 3

Hepatic IGF-1

Circulating GH stimulates the liver to synthesize and release Insulin-Like Growth Factor 1.

Step 4: Target Effect

Lipolysis & Repair

Selectively triggers breakdown of abdominal visceral adipose tissue while maintaining lean mass.

Feedback Safety:Unlike synthetic GH injections (which flood the body constantly and shut down natural production), GHRH analogues preserve somatostatin negative-feedback loops, limiting over-accumulation.

1. Hypothalamus to Pituitary

Tesamorelin binds specifically to GHRH receptors on pituitary somatotroph cells.

2. Pulsatile Growth Hormone Release

Stimulates natural episodic spikes of growth hormone rather than a constant, unnatural flood.

3. Liver Production of IGF-1

Growth hormone reaches the liver, prompting the release of Insulin-Like Growth Factor 1 (IGF-1).

4. Visceral Fat Lipolysis

Elevated GH and IGF-1 selectively activate lipid breakdown in dense abdominal visceral fat deposits.

Key Distinction: Because tesamorelin preserves natural negative feedback loops (somatostatin regulation), it reduces the risk of excessive growth hormone levels seen with direct GH injections.

4

What has actually been demonstrated in humans?

Approved Pharmaceutical

Tesamorelin is an FDA-approved prescription drug (brand name EGRIFTA / EGRIFTA SV). It underwent extensive Phase 3 multicenter human trials demonstrating significant, measurable reductions in visceral adipose tissue in adult patients.

NEJM Phase 3 Clinical Trial (Falutz et al., 2007)

Duration: 26 weeks · Population: 412 patients with excess abdominal fat accumulation

Published Finding: Visceral abdominal fat decreased by an average of 15.2% in the tesamorelin group compared to an increase of 2.1% with placebo. IGF-1 increased by 81%.

Pharmaceutical Reality vs. Unregulated Research Chemicals

Tesamorelin is FDA-approved exclusively for reducing excess abdominal visceral fat in HIV-infected patients with lipodystrophy. The FDA label explicitly states that tesamorelin is not indicated for general weight loss or cosmetic body contouring in the general public. IGF-1 levels must be monitored clinically because elevated IGF-1 carries theoretical proliferative risks.

5

What is still uncertain or unknown?

No controlled clinical trials support its safety or effectiveness for general cosmetic fat loss or athletic enhancement in healthy individuals without HIV lipodystrophy. Long-term safety of sustained IGF-1 elevation in non-deficient populations remains unstudied.

Regulatory Position: FDA-approved prescription medicine (EGRIFTA) restricted to HIV-associated lipodystrophy. It is NOT approved for general weight loss or cosmetic fitness.

Clinical Perspectives & Expert Discussions

Explore all perspectives

What identifiable clinicians, researchers, and professional bodies have publicly discussed regarding Tesamorelin.

Clinical Practice Observation

Dr. Edwin Lee, M.D., F.A.C.E.

Board-certified in Internal Medicine and Endocrinology, Diabetes and Metabolism; Fellow of the American College of Endocrinology; founder of the Clinical Peptide Society.

10 June 2022

Dr. Lee emphasizes that any clinical exploration of growth hormone secretagogues must be accompanied by comprehensive baseline and ongoing laboratory evaluation, including serum IGF-1, fasting insulin, HbA1c, and cancer screening. He cautions that secretagogues are biologically active molecules that influence cellular proliferation and glucose counter-regulation.

Context: Clinical Peptide Society / Institute for Hormonal BalanceView source discussion

An FDA-approved growth hormone-releasing factor analogue specifically indicated for HIV-associated lipodystrophy. Other cosmetic, bodybuilding, or anti-aging uses discussed online are unapproved.

Therapept separates official product labels, published clinical study interventions, animal research, clinical references, and community-reported ranges — never blended into one number.

3 records in this file

  • CLINICAL TRIAL1
  • REGULATORY2

Publication span: 2007–2026

What Has Actually Been Studied

  • WADA Prohibited List — S2.2.4 GHRH analogues (WADA Prohibited List, 2026) — Anti-doping listing.
  • Drugs@FDA — EGRIFTA (BLA 022505) (Drugs@FDA, 2010) — Approved-drug labelling.
  • Metabolic effects of a growth hormone-releasing factor in patients with HIV (New England Journal of Medicine, 2007) — Randomised, double-blind, placebo-controlled trial.

What is Still Unknown

What we know

  • FDA-approved as EGRIFTA (BLA 022505, 2010). Falutz et al. 2007 (NEJM) is a primary interventional paper in the HIV-lipodystrophy programme.
  • It is the only GHRH analogue in this library with a currently marketed United States approval.
  • Also named on the WADA GHRH-analogue list — approval and sporting prohibition are different questions.

Editorial reading of the records below, labelled as Therapept analysis. How records are built

What remains uncertain

  • Orthopaedic or “performance” endpoints: 2026 sports-medicine reviews report no supporting evidence in those settings.

Preparation and Handling

Lyophilized peptides ship as freeze-dried powders; whatever happens next involves diluents, concentrations and storage conditions that are compound- and product-specific.

United States Regulatory Status

FDA-approved drug substance

Application: BLA 022505 (EGRIFTA)

Approved Indication: Marketed in the United States as EGRIFTA, an approved prescription product administered subcutaneously.

  • EGRIFTA, BLA 022505, approved 10 November 2010. Active prescription product.
  • Not listed on FDA's Category 2 or withdrawn-nomination compounding tables.

WADA Anti-Doping Status

Named at S2.2.4 among GHRH analogues. Prohibited at all times; non-Specified.

Technical Chemical SpecificationsClick to view CAS, sequence, and molecular formulas
Molecular weight
5136 g/mol
Sequence length
31 chars
CAS number
218949-48-5
PubChem CID
16137828
Compound class
Stabilised GHRH analogue — human GHRH(1-44) amide, N-terminally acylated
Sequence
trans-3-hexenoyl-GHRH(1-44)-NH2
Molecular formula
C221H366N72O67S
Molecular weight
5136 g/mol
CAS number
218949-48-5
PubChem CID
16137828

Sources

  1. PubChem CID 16137828
  2. Drugs@FDA — approved drug products
  3. WADA 2026 Prohibited ListEffective 1 January 2026.

Last reviewed 3 September 2026 · Compiled by Therapept Editorial · How these records are built