COMPOUND

Compounds / GH secretagogues

Tesamorelin

Tesamorelin (Egrifta SV / Egrifta WR, TH9507)

GH secretagogues SubQ FDA approved

The only FDA-approved GHRH analog (NDA 022505, approved 10 Nov 2010 by Theratechnologies). Indicated for reduction of excess abdominal fat in HIV-infected adults with lipodystrophy. Increasingly used off-label for visceral fat reduction in non-HIV adults and for HIV-associated NAFLD/NASH (Stanley 2019 PMID 31611038). Structurally: native human GHRH(1-44) with a trans-3-hexenoic acid moiety on the N-terminus that prevents enzymatic degradation while preserving GHRH-receptor binding.

At a glance

Half-life
~30 min Mean elimination t½ ~26-38 minutes. EGRIFTA SV (1.4 mg dose) reports mean t½ 8 minutes; original 1 mg/vial formulation reported 26 min. Despite short serum t½, GH pulse persists ~1-2h post-dose.
Routes
SubQ
Vial sizes
1.4 mg · 2 mg
Evidence base
3 studies 3 human

Mechanism

Binds the GHRH receptor on pituitary somatotrophs → stimulates synthesis and pulsatile release of endogenous GH. Downstream IGF-1 elevation drives lipolysis preferentially in visceral adipose tissue (VAT). Pulsatile release means GH/IGF-1 are elevated during the post-injection window but feedback (via somatostatin and IGF-1) eventually limits sustained exposure. Pharmacologically distinct from CJC-1295-DAC's tonic profile.

Dosing

Any amounts shown here are reported from published studies only. 3 of 3 catalogued studies involved human subjects. COMPOUND does not publish its own dosing guidance.

Where a study reports an amount, it appears in that study's entry below, attributed to the source.

Published evidence

  1. Human RCT 2019

    Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: randomised double-blind multicentre trial

    Stanley TL, Fourman LT, Feldpausch MN, et al. Lancet HIV

    n=61 HIV+ adults with hepatic fat fraction ≥5%. 12-month tesamorelin 2 mg/d: HFF -4.1% absolute vs placebo (p=0.018), -37% relative. 35% vs 4% reached HFF <5%. Prevented fibrosis progression. Establishes tesamorelin as the only therapy with positive RCT data for HIV-associated NAFLD.

    PMID 31611038

  2. Human RCT 2010

    Effects of tesamorelin in HIV-infected patients with abdominal fat accumulation: a randomized placebo-controlled trial with safety extension

    Falutz J, Potvin D, Mamputu JC, et al. J Acquir Immune Defic Syndr

    404 HIV+ patients, 12-month RCT. VAT -10.9% (-21 cm²) at 6 mo (p<0.0001), ~18% at 12 mo. Trunk fat, waist circumference, waist-hip ratio improved. Pivotal long-term safety dataset for FDA approval.

    PMID 20101189

  3. Human RCT 2007

    Metabolic effects of a growth hormone–releasing factor in patients with HIV

    Falutz J, Allas S, Blot K, et al. N Engl J Med

    26-wk Phase 3 RCT, n=412 HIV+ adults. Tesamorelin 2 mg/d SC reduced visceral adipose tissue 15.2% vs +5.0% placebo. Triglycerides ↓50 mg/dL vs ↑9. IGF-1 ↑81% vs ↓5%. No significant glucose change at population level.

    PMID 18057338

Reported side effects

Injection site reactions (erythema, pruritus, pain)
Very common Mild · 25% incidence in pivotal trial vs 14% placebo over 26 weeks. Usually mild and self-limiting.
Arthralgia
Common Mild · 13% incidence (FDA label). Class effect of GH-elevating agents.
Peripheral edema
Common Moderate · 6% incidence. GH-mediated fluid retention. May trigger or worsen carpal tunnel.
Myalgia
Common Mild · 6% incidence.
Glucose intolerance / new-onset diabetes
Common Serious · HR 3.3 (95% CI 1.4-9.6) vs placebo. ~5-7% develop new-onset glucose intolerance. Monitor fasting glucose and HbA1c.
Hypersensitivity reactions
Occasional Serious · 4% in pivotal trial. Includes rash, urticaria, anaphylaxis. The Egrifta label directs discontinuation if a hypersensitivity reaction is suspected.
IGF-1 elevation >2 SDS above normal
Very common Moderate · 47% exceed 2 SDS at 26 wk; 36% exceed 3 SDS. Persistent supraphysiologic IGF-1 → consider dose reduction or discontinuation. Long-term cancer risk theoretical concern.
Increased risk of malignancy progression
Rare Serious · Contraindicated in active malignancy. Monitor pre-existing benign lesions.
Carpal tunnel syndrome
Occasional Moderate · GH-mediated fluid retention compresses median nerve at the wrist. Class effect.

Interactions

  • CJC-1295 (no DAC) Redundant

    Both are GHRH-receptor agonists.

  • CJC-1295 (DAC) Redundant

    Both are GHRH-receptor agonists; DAC variant gives sustained, tesamorelin gives pulsatile.

  • Ipamorelin Synergy

    GHRH (tesamorelin) + GHRP (ipamorelin) supra-additive GH pulse via independent receptor pathways.

  • Insulin Caution

    GH antagonizes insulin action. ~5-7% of tesamorelin recipients develop glucose intolerance (HR 3.3 vs placebo).

  • Corticosteroids Caution

    GH affects glucocorticoid metabolism. Patients on glucocorticoid replacement may need maintenance/stress dose adjustment.

  • CYP450 substrates Caution

    GH treatment can decrease CYP450 enzyme activity in some patients. May alter levels of CYP-metabolized drugs.

Reconstitution and storage

EGRIFTA SV (F4, 2 mg vial): reconstitute with 0.5 mL sterile water for injection (provided diluent). Roll vial gently 30 sec. Do not shake. Yields 4 mg/mL. Do NOT freeze, do NOT refrigerate the reconstituted solution; discard if not used immediately. EGRIFTA WR (F8) is a different formulation with a smaller injection volume.

Lyophilized SV vials: room temperature 20-25°C (excursions 15-30°C). Protect from light; keep in original carton. Reconstituted: use immediately, do NOT refrigerate or freeze (per SV label).

Open the reconstitution calculator for Tesamorelin