Tesamorelin

Growth Hormone Secretagogue (GHRH Analogue)approved

Also known as: Egrifta, TH9507, Trans-3-hexenoic acid-GHRH(1-44)-NH2

An FDA-approved synthetic analogue of growth hormone-releasing hormone (GHRH) with a trans-3-hexenoic acid modification, indicated for HIV-associated lipodystrophy and studied for cognitive benefits and visceral fat reduction.

Overview

Tesamorelin is a synthetic 44-amino acid analogue of human growth hormone-releasing hormone (GHRH) with a trans-3-hexenoic acid group attached to the tyrosine at position 1, which enhances its stability and bioactivity. It is the only GHRH analogue approved by the FDA (2010) and is marketed under the brand name Egrifta for the reduction of excess abdominal (visceral) fat in HIV-infected patients with lipodystrophy. Tesamorelin works by stimulating the anterior pituitary gland to produce and release endogenous growth hormone in a pulsatile, physiological manner. This distinguishes it from exogenous GH administration, as the body's natural feedback mechanisms remain intact, reducing the risk of supraphysiological GH levels. Beyond its FDA-approved indication, Tesamorelin has gained significant popularity in the anti-aging and longevity communities for visceral fat reduction, body composition improvement, and potential cognitive benefits. Studies have shown it can reduce visceral adipose tissue by 15-20% and may improve cognitive function in older adults at risk for Alzheimer's disease by modulating brain amyloid and improving executive function.

Mechanism of Action

Tesamorelin acts through the GHRH receptor pathway: (1) Binds to GHRH receptors on anterior pituitary somatotroph cells, stimulating synthesis and secretion of endogenous growth hormone; (2) The trans-3-hexenoic acid modification protects against N-terminal enzymatic degradation, increasing half-life and receptor binding affinity; (3) Maintains pulsatile GH release patterns, preserving normal hypothalamic-pituitary feedback; (4) Elevated GH stimulates hepatic IGF-1 production, which mediates many downstream effects; (5) GH and IGF-1 promote lipolysis preferentially in visceral adipose tissue; (6) GH modulates lipid metabolism, reducing triglycerides and improving lipid profiles; (7) IGF-1 signaling in the brain may support neuronal health and cognitive function; (8) Unlike exogenous GH, does not suppress endogenous GH production or cause pituitary downregulation.

Molecular Formula

C221H366N72O67S1

Molecular Weight

5135.9 g/mol

Sequence

Modified GHRH(1-44)-NH2 with trans-3-hexenoic acid at Tyr1

Dosage Protocols

Dose Range

2mg2mg

Frequency

Once daily

Route

subcutaneous

Cycle Length

Ongoing, with periodic reassessment

FDA-approved dose is 2mg daily by subcutaneous injection in the abdomen. Inject at the same time each day, rotating injection sites. Results typically visible after 3-6 months of consistent use.

Source: FDA prescribing information (Egrifta SV)

Side Effects

EffectSeverity
Injection site reactionsmild
Arthralgiamild
Peripheral edemamild
Paresthesiamild
Nauseamild
Carpal tunnel symptomsmoderate
Hyperglycemiamoderate

Pros & Cons

FDA-approved medication with extensive clinical trial safety and efficacy data

Stimulates natural GH production with preserved pulsatile release and feedback regulation

Clinically proven to reduce visceral adipose tissue by 15-20%

Promising cognitive benefits shown in studies of older adults at risk for Alzheimer's

Does not suppress endogenous GH production like exogenous GH administration

Expensive, especially the branded Egrifta product ($800-1500+/month)

Requires daily subcutaneous injections for optimal results

GH-related side effects (joint pain, edema, insulin resistance) can occur

Fat loss reverses upon discontinuation; ongoing use needed for sustained results

Contraindicated in patients with active malignancy due to GH/IGF-1 elevation

Research Studies

Legal Status

FDA-approved (2010) for HIV-associated lipodystrophy under the brand name Egrifta/Egrifta SV. Prescription required. Off-label use is common. Available through specialty pharmacies and compounding pharmacies.

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