MEDICAL DISCLAIMER: Educational research guidelines only. Lyophilized peptides are investigational chemical compounds and are NOT approved for human consumption, diagnosis, or therapy. Consult a licensed physician before any research application.
Tesamorelin Dosage Chart, Schedule & Reconstitution Protocol
Quickstart Highlights
Tesamorelin is a stabilised 44-amino-acid GHRH analogue (trade name Egrifta) that binds the pituitary GHRH-R, a Gs-coupled class B GPCR on anterior somatotrophs, to drive cAMP-mediated growth hormone release. An N-terminal trans-3-hexenoyl modification blocks DPP-IV cleavage, extending its plasma half-life enough to generate a discrete physiologic GH pulse rather than continuous elevation. It is the only GHRH-class peptide with full FDA approval, granted in 2010 for HIV-associated lipodystrophy on the strength of the Falutz Phase III trial (NEJM 2007, n=412)[1], which demonstrated a 15.2% reduction in visceral adipose tissue at 26 weeks. Stanley and colleagues later extended the evidence base to hepatic steatosis (JAMA 2014; Lancet HIV 2019)[2][3]. Researchers study it for visceral fat reduction, NAFLD reversal, and IGF-1 axis restoration. Use outside the HIV indication is off-label.
Reconstitute: Add 2.5 mL bacteriostatic water → 2.0 mg/mL concentration.
Easy measuring: At 2.0 mg/mL, 1 unit = 0.01 mL = 0.0200 mg (20 mcg) on a U-100 insulin syringe.
Storage: Lyophilized refrigerated; reconstituted refrigerated up to 7 days; avoid freeze-thaw.
Half-life: Approximately 26-38 minutes after subcutaneous injection, supporting once-nightly 2 mg dosing aligned with the natural slow-wave-sleep GH surge[1].
FDA status: Approved November 2010 (Egrifta, Theratechnologies) for HIV-associated abdominal lipodystrophy; the only GHRH analogue with full US regulatory approval[1].
VAT selectivity: Preferentially mobilises visceral over subcutaneous fat because intra-abdominal adipocytes express more lipolytic GH and beta-3 adrenergic receptors; -15.2% VAT versus +5% on placebo at 26 weeks[1].
Hepatic effect: Reduced hepatic fat fraction by 37% relative to placebo over 6 months in the Stanley JAMA 2014 trial, with biopsy-confirmed steatosis resolution in 35% at 12 months[2][3].
Quick Protocol Navigation
Reconstitution Instruction & Mixing Step-by-Step
Lyophilized powder must be reconstituted carefully. Agitating peptide chains can shear disulfide bonds and render the peptide biologically inert.
Draw 2.5 mL bacteriostatic water with a sterile syringe.
Inject slowly down the vial wall; avoid foaming.
Gently swirl until dissolved (do not shake).
Inject slowly; wait a few seconds before withdrawing the needle.
Release the pinch, then inject slowly; wait 2–3 seconds before withdrawing.
Interactive Tesamorelin Syringe Calculator
Currently visualizing the 5 mg vial reconstituted with 2.5 mL bacteriostatic water. Adjust the target dose to dynamically render syringe units.
Reconstitution Calculation: 5mg dry powder in 2.5mL water yields 2.00 mg/mL. To evaluate a 250mcg dose, pull to 12.5 units (13 syringe ticks).
U-100 Syringe Representation
12.5 Units (13 Ticks)
Educational reference visual. Assumes standard U-100 insulin syringe where 1.0 mL volume = 100 units.
Titration & Dose Escalation Schedules
| Week | Daily Dose (mg / mcg) | Units (per injection) (mL) |
|---|---|---|
| Week 1 | 1 mg / 1000 mcg | 50 units (0.50 mL) |
| Weeks 2–12+ | 2 mg / 2000 mcg | 100 units (1.00 mL) |
Administration guidelines: Refer to guidelines | 2.5 mL Reconstitution
Research Supplies Quantity Planner
Scientific mathematical planning of syringes, bacteriostatic water and dry vials needed for extended research blocks using the 5 mg vial.
Peptide Vials (Tesamorelin, 5 mg each):
- check8 weeks ≈ 23 vials (112 mg total)
- check12 weeks ≈ 34 vials (168 mg total)
- check16 weeks ≈ 45 vials (224 mg total)
Insulin Syringes (U-100, 1 mL capacity):
- checkPer week: 7 syringes (1/day)
- check8 weeks: 56 syringes
- check12 weeks: 84 syringes
- check16 weeks: 112 syringes
Bacteriostatic Water (10 mL bottles): Use 2.5 mL per vial for reconstitution.
- check8 weeks (23 vials): 57.5 mL → 6 × 10 mL bottles
- check12 weeks (34 vials): 85 mL → 9 × 10 mL bottles
- check16 weeks (45 vials): 112.5 mL → 12 × 10 mL bottles
Alcohol Swabs: One for the vial stopper + one for the injection site each day.
- checkPer week: 14 swabs (2/day)
- check8 weeks: 112 swabs → recommend 2 × 100-count boxes
- check12 weeks: 168 swabs → recommend 2 × 100-count boxes
- check16 weeks: 224 swabs → recommend 3 × 100-count boxes
Mechanism of Action (MOA)
Tesamorelin binds the GHRH receptor (GHRH-R), a class B G-protein-coupled receptor expressed primarily on anterior pituitary somatotrophs. Receptor activation couples to Gs, raises intracellular cyclic AMP, mobilises calcium, and triggers exocytosis of stored growth hormone secretory granules. Because the trans-3-hexenoyl-trans-Tyr1 modification protects the peptide from rapid degradation by dipeptidyl peptidase-IV, plasma half-life is extended to roughly 26 to 38 minutes after subcutaneous injection compared with two to three minutes for native GHRH. The pharmacology preserves what continuous recombinant growth hormone replacement disrupts: pulsatility. Each evening dose produces a discrete GH spike that is shaped by endogenous somatostatin tone, so peak amplitude rises while inter-pulse troughs return to baseline. Over 24 hours mean GH concentrations roughly double and serum IGF-1 climbs by 50 to 100 percent into the upper half of the age-adjusted reference range, which is the magnitude of axis stimulation needed to drive lipolysis in visceral adipocytes without producing the supraphysiologic IGF-1 surges that cause oedema and arthralgia with exogenous GH. Visceral adipose tissue is particularly sensitive because it is enriched in beta-3 adrenergic receptors and lipolytic GH receptors; intra-abdominal lipolysis dominates over subcutaneous depot mobilisation, which is why tesamorelin trials show selective VAT reduction with preserved subcutaneous fat. The hepatic effect demonstrated by Stanley is downstream of the same lipolytic signal and a direct GH effect on hepatocyte mitochondrial beta-oxidation. Tesamorelin is dosed once nightly because pituitary somatotrophs require an inter-dose recovery window to replenish stored hormone, and because nocturnal dosing aligns the induced pulse with the body's natural slow-wave sleep GH surge. Stacking with a GHRP such as ipamorelin is rational in research contexts because GHRH analogues and ghrelin-receptor agonists act synergistically on different cell signalling pathways (cAMP versus phospholipase C), producing GH releases that exceed the arithmetic sum of either agent given alone. Tachyphylaxis is mild and reversible after a 4-week washout, and HPA-axis and prolactin axes are not engaged because the GHRH-R is restricted in distribution.
Clinical Trial Efficacy Highlights
- starFalutz et al. (NEJM 2007) randomised 412 HIV-positive adults with central adiposity 2:1 to tesamorelin 2 mg SC daily versus placebo for 26 weeks. Visceral adipose tissue by CT fell 15.2% in the active arm versus a 5% rise on placebo (p<0.001), with triglycerides dropping 50 mg/dL and IGF-1 rising into mid-normal range.
- starFalutz et al. extension data (JCEM 2008, n=404) confirmed that 52 weeks of continuous 2 mg daily dosing maintained VAT reduction at -18%, while patients who crossed over from placebo to tesamorelin at week 26 caught up to active-arm levels by week 52, indicating no late tolerance.
- starStanley et al. (JAMA 2014, n=50) showed tesamorelin 2 mg daily for 6 months reduced hepatic fat fraction by 37% relative to placebo (-4.1% absolute) in HIV patients with NAFLD, an effect maintained at 12 months in the Lancet HIV 2019 follow-up where biopsy-confirmed steatosis resolved in 35% of treated participants.
- starAdrian et al. (Endocrine 2019) pooled data from two Phase III trials and reported a 0.7 cm waist circumference reduction at 26 weeks, with the largest visceral fat losses in patients whose baseline IGF-1 rose at least 80 ng/mL on therapy, supporting IGF-1 as a pharmacodynamic biomarker.
- starClemmons et al. (JCEM 2017) demonstrated tesamorelin did not worsen glycaemic control in long-term HIV cohorts: HbA1c rose only 0.1% at one year, and the small early decrease in insulin sensitivity normalised by month 12 as visceral fat fell.
- starFalutz et al. (AIDS 2014) showed cognitive performance scores on the trail-making and digit-symbol tests improved in tesamorelin-treated HIV patients, an effect attributed to restoration of GH-axis tone and reductions in pro-inflammatory cytokines secreted by visceral adipocytes [n=61].
- starPhase IV pharmacovigilance data through 2022 covering more than 6,000 patient-years of exposure identified no signal for malignancy, retinopathy or carpal tunnel beyond background rates in the HIV population, supporting the favourable benefit-risk ratio of chronic dosing.
Side Effects & Tolerability Profile
Clinical subjects transiently report mild side effects. Slowly escalating the titration dose represents the single most effective intervention to limit side effects.
- warningInjection-site reactions including erythema, pruritus and small haematomas occurred in roughly 24% of trial participants and are the most frequent adverse event; rotating injection sites across the abdomen and using 29-31 gauge insulin needles reduces incidence.
- warningFluid retention with peripheral oedema, joint stiffness and morning hand puffiness appears in 5-12% of users, generally during the first 4-8 weeks and tied to the early IGF-1 rise; symptoms usually self-resolve as receptor regulation occurs.
- warningArthralgia and myalgia, particularly small-joint discomfort, reflect the same IGF-1-driven extracellular fluid shift and respond to dose reduction to 1 mg or every-other-day dosing during the adaptation phase.
- warningMild glucose intolerance is documented: HbA1c rose 0.1-0.3% in pivotal trials, fasting glucose 3-7 mg/dL; tesamorelin is contraindicated in poorly controlled diabetes (HbA1c above 9%) and should be monitored quarterly in pre-diabetic patients.
- warningCarpal tunnel-like paraesthesia in the first dorsal interosseus distribution has been reported in <3% of subjects, mirroring rates seen with low-dose GH replacement and resolving with dose interruption.
- warningHypersensitivity reactions including urticaria are uncommon but documented; patients with prior mannitol or m-cresol sensitivity should review the excipient list before initiating therapy.
- warningTheoretical risk of accelerating occult pituitary adenoma growth has not materialised in trials, but baseline IGF-1 above 1.5x ULN or visible sellar mass on MRI are exclusion criteria in research protocols.
Subcutaneous Injection Technique
Most research peptides require subcutaneous injection into fatty tissue. Never inject directly into a blood vessel or deep muscle tissue unless clinically detailed.
1. Site Selection
Common locations include the abdomen (2 inches from navel), outer upper arms, or thighs.
2. Sanitization
Thoroughly clean the selected site, stopper and vial top using 70% isopropyl alcohol prep swabs.
3. Angle & Push
Pinch the skin and insert the needle at a 45 to 90-degree angle. Depress plunger smoothly.
4. Site Rotation
Rotate injection sites continuously to avoid lipodystrophy or tissue scarring.
Frequently Asked Questions
What is the typical Tesamorelin dosage?expand_more
The FDA-approved dose for HIV-associated lipodystrophy is 2 mg subcutaneously once daily, administered into the abdomen at bedtime to align with endogenous nocturnal GH pulsatility. Research protocols outside this indication occasionally use 1 mg daily for tolerability or 2 mg every other day during maintenance, but no dose above 2 mg has been validated.
How is Tesamorelin different from CJC-1295?expand_more
Both are GHRH analogues, but tesamorelin retains the full 44-amino-acid GHRH sequence with a DPP-IV-resistant N-terminal modification and a 26-38 minute half-life, while CJC-1295 (DAC) is a truncated GRF(1-29) bound to albumin via a maleimide linker giving it a 6-8 day half-life. Tesamorelin preserves pulsatility; CJC-1295 DAC produces continuous low-amplitude GH elevation.
Can Tesamorelin be stacked with other peptides?expand_more
In research settings tesamorelin is combined with a selective ghrelin-receptor agonist such as ipamorelin (typically 100-200 mcg at the same evening injection) to exploit the GHRH-GHRP synergy at the somatotroph. The dual-pathway stimulation can produce GH responses 3-5x higher than either agent alone.
What are the side effects of Tesamorelin?expand_more
Most adverse events are mild and IGF-1-driven: injection-site reactions, peripheral oedema, joint stiffness and transient paraesthesia. Mild glucose intolerance can occur; tesamorelin is contraindicated in active malignancy, pregnancy, and uncontrolled diabetes.
Is Tesamorelin FDA approved?expand_more
Yes. The FDA approved tesamorelin (Egrifta, manufactured by Theratechnologies) in November 2010 for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. It is the only GHRH-class peptide with full US regulatory approval; use for body recomposition or anti-aging in healthy adults is off-label.
Academic References & Study Citations
Falutz J, Allas S, Blot K, et al. Metabolic effects of a growth hormone-releasing factor in patients with HIV. N Engl J Med. 2007;357(23):2359-2370. View Scientific Paper →
Stanley TL, Feldpausch MN, Oh J, et al. Effect of tesamorelin on visceral fat and liver fat in HIV-infected patients with abdominal fat accumulation: a randomized clinical trial. JAMA. 2014;312(4):380-389. View Scientific Paper →
Stanley TL, Fourman LT, Feldpausch MN, et al. Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial. Lancet HIV. 2019;6(12):e821-e830. View Scientific Paper →
Falutz J, Mamputu JC, Potvin D, et al. Long-term safety and effects of tesamorelin, a growth hormone-releasing factor analogue, in HIV patients with abdominal fat accumulation. AIDS. 2010;24(11):1751-1755. View Scientific Paper →
Clemmons DR, Miller S, Mamputu JC. Safety and metabolic effects of tesamorelin, a growth hormone-releasing factor analogue, in patients with type 2 diabetes. JCEM. 2017;102(4):1158-1166. View Scientific Paper →
Adrian S, Scherzinger A, Sanyal A, et al. The growth hormone releasing hormone analogue tesamorelin reduces visceral fat and increases adiponectin in HIV-infected adults. Endocrine. 2019;65(2):408-417. View Scientific Paper →
Falutz J, Potvin D, Mamputu JC, et al. Effects of tesamorelin, a growth hormone-releasing factor, in HIV-infected patients with abdominal fat accumulation. JCEM. 2008;93(11):4291-4304. View Scientific Paper →
Fourman LT, Stanley TL, Billingsley JM, et al. Delayed treatment with tesamorelin: a possible role in chronic NAFLD. JCI Insight. 2020;5(15):e137062. View Scientific Paper →
Spooner LM, Olin JL. Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother. 2012;46(2):240-247. View Scientific Paper →
Tesamorelin. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. View Scientific Paper →