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Tesamorelin

The only FDA-approved GHRH analog

Injection · Prescription

Educational content. This page describes Tesamorelin for informational purposes only and is not medical advice, diagnosis, or treatment. Consult a licensed provider before starting, stopping, or modifying any therapy.

Researched and maintained by the PepHookup team. Regulatory status last verified April 12, 2026.

Primary Use
A stabilized 44-residue GHRH analog that stimulates endogenous growth hormone secretion.
Administration
injection
Typical Cycle
Ongoing (benefit reverses on discontinuation)
Legal Status
Legal
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Key Benefits

Visceral Fat Reduction

In a pooled analysis of two Phase III trials in over 800 HIV patients, tesamorelin reduced visceral adipose tissue by a treatment effect of about 15% versus placebo at 26 weeks, with the original pivotal trial showing a 15.2% decrease against a 5% rise on placebo.[1][2]

Physiologic Pulsatile GH Release

In healthy men, two weeks of tesamorelin increased mean overnight growth hormone and GH pulse area while preserving the natural pulsatile pattern, raising IGF-1 without the flat supraphysiologic exposure of injected growth hormone.[3]

Reduced Liver Fat

A randomized trial in HIV patients with fatty liver disease cut hepatic fat fraction by a relative 37% over 12 months, and 35% of treated patients reached a liver fat fraction below 5% versus 4% on placebo.[5][6]

Cognitive Function Signal

A 20-week controlled trial of 152 older adults found a favorable effect of the GHRH analog on cognition, with the strongest signal in executive function, in both healthy aging and mild cognitive impairment.[7][8]

What is Tesamorelin?

Tesamorelin is a synthetic analog of human growth hormone-releasing hormone built on the full 44-amino-acid GHRH(1-44) sequence. What sets it apart from native GHRH is a trans-3-hexenoic acid group attached to the alpha-amino position of the N-terminal tyrosine. This lipophilic modification sterically blocks dipeptidyl peptidase-4 (DPP-4), the enzyme that rapidly clears endogenous GHRH, giving tesamorelin a longer functional half-life while it retains the natural GHRH sequence rather than substituting amino acids the way some other analogs do.

Developed by Theratechnologies in Montreal, tesamorelin is the first and only therapy approved specifically to reduce excess abdominal fat in HIV-infected patients with lipodystrophy. The FDA approved it in November 2010 as Egrifta. A more concentrated single-vial formulation, Egrifta SV, followed, and in March 2025 the FDA approved Egrifta WR, an eight-fold concentrated F8 formulation that needs reconstitution only once a week while still being injected daily. It is not approved for general weight loss, athletic performance, or obesity.

How Does It Work?

Tesamorelin binds GHRH receptors on the somatotroph cells of the anterior pituitary. These are G-protein-coupled receptors linked to the Gs alpha subunit, so activation stimulates adenylyl cyclase, raises intracellular cAMP, and engages protein kinase A. The result is phosphorylation of CREB and increased transcription and secretion of growth hormone.

Because the signal acts one step upstream of the pituitary rather than replacing growth hormone directly, the body's own pulsatile release pattern is preserved. In healthy men, tesamorelin raised mean overnight GH, GH pulse area, and basal secretion and increased IGF-1, while leaving fasting glucose and insulin-stimulated glucose uptake statistically unchanged. The released GH then acts on the liver and peripheral tissues to drive IGF-1 production.

The growth hormone and IGF-1 axis favors lipolysis in visceral fat, which carries a higher density of GH receptors than subcutaneous fat. That selectivity is the leading explanation for the targeted reduction in abdominal fat seen in trials. Secondary metabolic shifts have included lower triglycerides and improvements in hepatic fat and liver-related gene expression.

Mechanism of Action

Tesamorelin activates pituitary GHRH receptors through the cAMP/PKA/CREB cascade, prompting pulsatile, physiologic growth hormone release. The resulting GH and IGF-1 signaling preferentially mobilizes visceral fat while preserving the hypothalamic-pituitary feedback loop, producing targeted abdominal fat reduction alongside lower triglycerides and reduced liver fat.

TesamorelinGHRH-R ActivationPituitary somatotrophscAMP / PKA / CREBGH gene transcriptionPulsatile GH ReleasePhysiologic pattern preservedVisceral LipolysisPreferential fat reductionvia GH receptor densityIGF-1 ProductionHepatic & peripheralanabolic signalingMetabolic ImprovementTriglycerides, adiponectin& inflammatory markersPulsatile GH Secretion for Targeted Visceral Fat Reduction

Clinical Evidence

Pivotal Phase III Trial in HIV Lipodystrophy (NEJM)

Multicenter, randomized, double-blind, placebo-controlled Phase III trial over 26 weeks412 HIV-infected patients with excess abdominal fat on stable antiretroviral therapy

Tesamorelin 2 mg subcutaneously once daily reduced visceral adipose tissue by 15.2% versus a 5% increase on placebo (P<0.001). Triglycerides fell by about 50 mg/dL versus a 9 mg/dL rise on placebo. Self-image and IGF-1 also improved.

Falutz J, Allas S, Blot K, Potvin D, Kotler D, Somero M, Berger D, Brown S, Richmond G, Fessel J, Turner R, Grinspoon S · N Engl J Med, 357(23):2359-2370 (2007) · PubMed

Pooled Phase III Analysis with Safety Extension (JCEM)

Pooled analysis of two multicenter, double-blind, placebo-controlled Phase III trials with 52-week safety extension806 HIV-infected patients with excess abdominal fat across both trials

At 26 weeks the treatment effect on visceral adipose tissue was -15.4% versus placebo (P<0.001) with a -12.3% treatment effect on triglycerides. Anti-tesamorelin IgG antibodies developed in roughly half of treated patients but were generally non-neutralizing.

Falutz J, Mamputu JC, Potvin D, Moyle G, Soulban G, Loughrey H, Marsolais C, Turner R, Grinspoon S · J Clin Endocrinol Metab, 95(9):4291-4304 (2010) · PubMed

Durability and Rebound After Discontinuation (JAIDS)

Randomized, placebo-controlled trial with a 26-week efficacy phase and a 26-week extension in which some patients switched treatment404 HIV-infected patients with excess abdominal fat

Visceral fat gains made during the first 26 weeks were rapidly lost in patients switched from tesamorelin to placebo, while continued treatment maintained the reduction. This established that ongoing therapy is required to sustain benefit.

Falutz J, Potvin D, Mamputu JC, Assaad H, Zoltowska M, Michaud SE, Berger D, Somero M, Moyle G, Brown S, Martorell C, Turner R, Grinspoon S · J Acquir Immune Defic Syndr, 53(3):311-322 (2010) · PubMed

Liver Fat Reduction in HIV-Associated NAFLD (Lancet HIV)

Randomized, double-blind, placebo-controlled multicenter trial over 12 monthsHIV-infected adults with nonalcoholic fatty liver disease

Tesamorelin lowered hepatic fat fraction with an absolute effect of -4.1% and a relative reduction of 37% versus placebo. By 12 months, 35% of treated patients reached a hepatic fat fraction below 5% versus 4% on placebo, with a lower rate of fibrosis progression.

Stanley TL, Fourman LT, Feldpausch MN, Purdy J, Zheng I, Pan CS, Aepfelbacher J, Buckless C, Tsao A, Kellogg A, Branch K, Lee H, Liu CY, Corey KE, Chung RT, Torriani M, Kleiner DE, Hadigan CM, Grinspoon SK · Lancet HIV, 6(12):e821-e830 (2019) · PubMed

Cognitive Function in Aging and Mild Cognitive Impairment (Arch Neurol)

Randomized, double-blind, placebo-controlled trial over 20 weeks152 adults aged 55 to 87 (66 with mild cognitive impairment, the remainder healthy)

Tesamorelin 1 mg subcutaneously once daily produced a favorable effect on cognition (P=0.03 in the intent-to-treat analysis), strongest for executive function, in both healthy older adults and those with mild cognitive impairment. A companion study found increased brain GABA levels.

Baker LD, Barsness SM, Borson S, Merriam GR, Friedman SD, Craft S, Vitiello MV · Arch Neurol, 69(11):1420-1429 (2012) · PubMed

Dosing & Administration

Subcutaneous Injection (Egrifta WR, F8 formulation)

Dosage
1.28 mg daily
Frequency
Once daily
Cycle
Ongoing (benefit reverses on discontinuation)

Subcutaneous Injection (Egrifta SV)

Dosage
1.4 mg daily
Frequency
Once daily
Cycle
Ongoing (benefit reverses on discontinuation)

Subcutaneous Injection (cognitive research dose)

Dosage
1 mg daily
Frequency
Once daily
Cycle
20 weeks

Subcutaneous Injection (Egrifta WR, F8 formulation): FDA-approved 2025 formulation. Reconstituted once weekly; one vial supplies seven daily 1.28 mg doses injected into the abdomen.

Subcutaneous Injection (Egrifta SV): Earlier single-vial formulation. Reconstituted daily and injected into the abdomen with rotation of sites. The original Egrifta was dosed at 2 mg daily.

Subcutaneous Injection (cognitive research dose): Lower dose used in the Baker et al. cognitive function trial, not an approved indication.

Dosing is determined by a licensed provider, and the approved indication is HIV-associated lipodystrophy rather than general weight loss or anti-aging use.

Visceral fat reduction reverses after stopping. In the 52-week extension, patients switched from tesamorelin to placebo lost the gains they had made, so continued treatment is needed to maintain results.

IGF-1 should be monitored periodically. Treatment is typically discontinued if IGF-1 stays elevated above the age-adjusted upper limit of normal, since the long-term effects of sustained IGF-1 elevation are unknown.

Anti-tesamorelin IgG antibodies developed in about 50% of patients at 26 weeks and 47% at 52 weeks. They are generally non-neutralizing and have not been linked to loss of efficacy, though incidence was higher in patients who had hypersensitivity reactions.

Side Effects & Safety

Common

  • Injection site reactions: Erythema, pruritus, pain, swelling, irritation, or bruising at the injection site, reported as injection site reactions in about 17% of treated patients versus 6% on placebo
  • Arthralgia: Joint pain in about 13% of treated patients versus 11% on placebo, often part of the fluid-retention pattern

Uncommon

  • Peripheral edema: Fluid retention in about 6% of treated patients versus 2% on placebo, usually transient
  • Pain in extremity / myalgia: Limb pain (about 6%) and muscle pain (about 6%), modestly above placebo rates
  • Paresthesia / hypoesthesia: Tingling or reduced sensation in the extremities in roughly 4 to 5% of patients, occasionally as carpal tunnel syndrome from fluid retention
  • Hyperglycemia: Glucose intolerance can emerge; HbA1c reached 6.5% or higher in 5% of treated patients versus 1% on placebo. Glucose should be checked before and during treatment

Safety Profile

Tesamorelin has the strongest clinical evidence base among GHRH analogs, with more than 800 HIV patients studied across two pivotal Phase III randomized controlled trials plus extension data. Most adverse reactions were mild injection site or fluid-retention effects.

The pulsatile GH release pattern preserves hypothalamic-pituitary feedback, a meaningful contrast with injected growth hormone. In healthy men at the 2 mg dose, fasting glucose and insulin-stimulated glucose uptake were not significantly affected, and a separate 12-week trial in type 2 diabetics found no worsening of insulin response or glycemic control.

Long-term IGF-1 monitoring is advised because the consequences of sustained IGF-1 elevation are unknown and carry a theoretical proliferative risk. Treatment is reassessed if IGF-1 consistently exceeds age-appropriate limits.

Contraindications

  • Disruption of the hypothalamic-pituitary axis from hypophysectomy, pituitary tumor, surgery, head radiation, or trauma
  • Active malignancy (tesamorelin raises IGF-1, which can promote cell proliferation); preexisting cancer must be inactive and treated before starting
  • Pregnancy (fetal harm is expected based on the mechanism and animal data; discontinue if pregnancy occurs)
  • Known hypersensitivity to tesamorelin or to any excipient, including mannitol

Compare with Similar Peptides

PeptidePrimary UseAdministrationCycle LengthKey Differentiator
TesamorelinVisceral Fat & GHRH SignalingSubcutaneous InjectionOngoing dailyThe only FDA-approved GHRH analog, with Phase III data in over 800 patients, documented liver-fat reduction, and physiologic pulsatile GH release
SemaglutideWeight Management & Metabolic HealthInjection (weekly), Oral (daily)OngoingThe most clinically validated GLP-1 medicine, with outcomes data spanning weight, heart, kidney, and liver disease
TirzepatideWeight Loss & Type 2 DiabetesInjection (weekly)OngoingOnly dual GIP/GLP-1 agonist; the deepest weight loss of any approved obesity drug, up to about 21% of body weight
SermorelinGH restoration and healthy agingSubcutaneous injection, daily at bedtime3-6 monthsThe GHRH analog with prior FDA approval and a multi-decade clinical record, preserving natural feedback rather than replacing growth hormone
IpamorelinGH stimulation for body composition and recoverySubcutaneous injection (1-3x daily)Determined by providerThe most selective GH secretagogue in preclinical work: a clean GH pulse without the cortisol, prolactin, or appetite effects of older GHRPs

Regulatory Status

FDA-Approved

Prescription

This peptide is an FDA-approved drug available via standard prescription.

Regulatory Detail

FDA-approved as Egrifta (2010) and Egrifta WR (2025) for HIV-associated lipodystrophy. As a biologic, compounding is restricted. Pharmacies cannot compound biologics without a biologics license.

FDA Action History

  • FDA approved Egrifta WR (tesamorelin F8 formulation) with improved weekly reconstitution convenience

  • FDA approved Egrifta (tesamorelin) for reduction of excess abdominal fat in HIV-infected adults with lipodystrophy

    FDA NDA 022505
What do these terms mean?
503A compounding
Licensed pharmacies that prepare custom prescriptions for individual patients based on a physician's order. 503A is the section of the federal law that governs them.
503B outsourcing
FDA-registered facilities that compound in larger batches under stricter federal oversight (closer to a manufacturer than a pharmacy). Used mostly by hospitals and clinics.
Bulk drug substance
The active pharmaceutical ingredient a compounder starts with, before it's made into a finished medication.
Category 1
Interim bucket for bulk substances that have been nominated and don't appear to present significant safety risks. 503A pharmacies may compound them under FDA enforcement discretion while the agency continues its review. Not the same as FDA approval.
Category 2
Bulk substances the FDA has flagged for significant safety risks. 503A compounding carries FDA enforcement risk, so most pharmacies decline to prepare them and many physicians hesitate to prescribe them.
PCAC
Pharmacy Compounding Advisory Committee. The FDA advisory committee that reviews nominated bulk substances and recommends whether they belong in Category 1, Category 2, or on the final 503A Bulks List.

Last verified April 12, 2026. PepHookup tracks public FDA actions. This is not legal or medical advice.

Frequently Asked Questions

Research & References

  1. 1

    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.” N Engl J Med, 357(23):2359-2370 (2007)

  2. 2

    Falutz J, Mamputu JC, Potvin D, Moyle G, Soulban G, Loughrey H, Marsolais C, Turner R, Grinspoon S Effects of tesamorelin (TH9507), a growth hormone-releasing factor analog, in human immunodeficiency virus-infected patients with excess abdominal fat: a pooled analysis of two multicenter, double-blind placebo-controlled phase 3 trials with safety extension data.” J Clin Endocrinol Metab, 95(9):4291-4304 (2010)

  3. 3

    Stanley TL, Chen CY, Branch KL, Makimura H, Grinspoon SK Effects of a growth hormone-releasing hormone analog on endogenous GH pulsatility and insulin sensitivity in healthy men.” J Clin Endocrinol Metab, 96(1):150-158 (2011)

  4. 4

    Falutz J, Potvin D, Mamputu JC, Assaad H, Zoltowska M, Michaud SE, Berger D, Somero M, Moyle G, Brown S, Martorell C, Turner R, Grinspoon S Effects of tesamorelin, a growth hormone-releasing factor, in HIV-infected patients with abdominal fat accumulation: a randomized placebo-controlled trial with a safety extension.” J Acquir Immune Defic Syndr, 53(3):311-322 (2010)

  5. 5

    Stanley TL, Fourman LT, Feldpausch MN, Purdy J, Zheng I, Pan CS, Aepfelbacher J, Buckless C, Tsao A, Kellogg A, Branch K, Lee H, Liu CY, Corey KE, Chung RT, Torriani M, Kleiner DE, Hadigan CM, Grinspoon SK Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial.” Lancet HIV, 6(12):e821-e830 (2019)

  6. 6

    Fourman LT, Billingsley JM, Agyapong G, Ho Sui SJ, Feldpausch MN, Purdy J, Zheng I, Pan CS, Corey KE, Torriani M, Kleiner DE, Hadigan CM, Stanley TL, Chung RT, Grinspoon SK Effects of tesamorelin on hepatic transcriptomic signatures in HIV-associated NAFLD.” JCI Insight, 5(16):e140134 (2020)

  7. 7

    Baker LD, Barsness SM, Borson S, Merriam GR, Friedman SD, Craft S, Vitiello MV Effects of growth hormone-releasing hormone on cognitive function in adults with mild cognitive impairment and healthy older adults: results of a controlled trial.” Arch Neurol, 69(11):1420-1429 (2012)

  8. 8

    Friedman SD, Baker LD, Borson S, Jensen JE, Barsness SM, Craft S, Merriam GR, Otto RK, Novotny EJ, Vitiello MV Growth hormone-releasing hormone effects on brain gamma-aminobutyric acid levels in mild cognitive impairment and healthy aging.” JAMA Neurol, 70(7):883-890 (2013)

  9. 9

    Clemmons DR, Miller S, Mamputu JC Safety and metabolic effects of tesamorelin, a growth hormone-releasing factor analogue, in patients with type 2 diabetes: a randomized, placebo-controlled trial.” PLoS One, 12(6):e0179538 (2017)

  10. 10

    Dhillon S Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy.” Drugs, 71(8):1071-1091 (2011)

  11. 11

    Spooner LM, Olin JL Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy.” Ann Pharmacother, 46(2):240-247 (2012)

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