GHRH Analog / SubQ / 1-2mg daily
Tesamorelin
Tesamorelin is native human GHRH(1-44) carrying one addition: a six-carbon acyl cap on the N-terminal tyrosine that blocks the enzyme which otherwise destroys the hormone within minutes. The molecule was designed backwards from a 1986 result explaining why the natural hormone could never be an injectable drug.
In plain words
Tesamorelin is the natural human hormone that tells the pituitary gland to release growth hormone, with one small chemical cap added at the front end so that an enzyme in the blood cannot destroy it within minutes. It is an approved prescription medicine in the United States, cleared in 2010 for one narrow purpose: reducing the deep abdominal fat that builds up in some people with HIV, which is still the only indication either of its current labels carries. The randomized evidence for that purpose is genuinely good. In the trial behind the approval, deep abdominal fat fell 15.2 percent while it rose 5.0 percent on placebo; the effect was specific to deep fat rather than the fat just under the skin, and it reversed once treatment stopped, so it lasts only as long as the dosing does. It is also narrow: nearly all of the randomized evidence comes from people with HIV, and the approved labeling carries a standing warning about glucose intolerance and new diabetes, so how it behaves in people with an intact growth hormone system is much less well established. Outside that indication it is supplied by research-chemical sellers and compounding pharmacies, where what varies is whether the fill was sterile and whether the number on the label describes peptide content or gross powder weight.
At a glance
| Half-life | 0.018 days |
|---|---|
| Tmax | 0.01 days |
| Route(s) | SubQ |
| Published dosing range | 1-2mg daily |
| Vial strengths | 2, 1, 5, 10, 11.6 mg |
Reference data from the DosePlot canon -- not a protocol recommendation.
Serum curve
Single 1.5 mg dose by SubQ, rendered from the same engine that powers the interactive chart. Relative levels, not lab values.
What does the evidence show?
Two things are labeled separately here because they answer different questions. The tier is how a study was built. The distance chips are whether that study touched this molecule, by this route, in a population resembling the reader. A randomized trial of a different molecule keeps its tier and still says nothing about this compound.
| Finding | Tier | Distance from use | Study |
|---|---|---|---|
| In the 26-week trial that supported approval, 412 adults with HIV and central fat accumulation were randomized to 2 mg of tesamorelin daily or placebo. Visceral fat fell 15.2 percent on tesamorelin and rose 5.0 percent on placebo, and IGF-1 rose 81.0 percent against a 5.0 percent fall on placebo. | rct | not recorded | Falutz J, Allas S, Blot K, et al. Metabolic effects of a growth hormone-releasing factor in patients with HIV.New England Journal of Medicine 357(23):2359-2370, 2007 |
| Pooling the two phase 3 trials (806 patients), the visceral fat effect against placebo at 26 weeks was -15.4 percent while abdominal subcutaneous fat was essentially unchanged (treatment effect -0.6 percent, P = 0.08). That selectivity for visceral over subcutaneous fat is what separates tesamorelin from general weight loss. The pooled analysis reported no clinically meaningful between-group differences in glucose parameters at 26 or 52 weeks. The approved labeling draws a different conclusion from the same trial program. Section 5.4 of the current labeling, not the paper cited here, carries a standing warning for glucose intolerance and diabetes mellitus: HbA1c at or above 6.5 percent by week 26 in 5 percent of tesamorelin patients against 1 percent on placebo, and an intent-to-treat hazard odds ratio of 3.3 (confidence interval 1.4 to 9.6) for developing diabetes. | rct | not recorded | Falutz J, Mamputu JC, Potvin D, et al. 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.Journal of Clinical Endocrinology and Metabolism 95(9):4291-4304, 2010 |
| The effect lasts only as long as the dosing does. Patients who stayed on tesamorelin held an 18 percent visceral fat reduction at 52 weeks; in patients rerandomized to placebo at week 26, visceral fat reaccumulated. The trial authors state plainly that the effect does not persist beyond the treatment period. | rct | not recorded | Falutz J, Allas S, Mamputu JC, et al. Long-term safety and effects of tesamorelin, a growth hormone-releasing factor analogue, in HIV patients with abdominal fat accumulation.AIDS 22(14):1719-1728, 2008 |
| In adults with HIV and non-alcoholic fatty liver disease, 2 mg daily for 12 months lowered hepatic fat fraction by 4.1 percentage points more than placebo (a 37 percent relative reduction from baseline). Among the participants with paired liver biopsies, fibrosis progressed in 10.5 percent of the tesamorelin group against 37.5 percent on placebo (P = 0.04). | rct | not recorded | 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.The Lancet HIV 6(12):e821-e830, 2019 |
| In 152 older adults randomized with and without mild cognitive impairment, a population unrelated to the approved indication, 1 mg injected nightly for 20 weeks had a favorable overall effect on cognition against placebo (P = 0.03 by intention to treat, P = 0.002 among the 137 who completed). Executive function carried the effect (P = 0.005); verbal memory showed a trend that did not reach significance (P = 0.08). The same trial cut percent body fat by 7.4 percent (P < 0.001). | rct | not recorded | Baker LD, Barsness SM, Borson S, et al. Effects of growth hormone-releasing hormone on cognitive function in adults with mild cognitive impairment and healthy older adults: results of a controlled trial.Archives of Neurology 69(11):1420-1429, 2012 |
| The trans-3-hexenoyl group is what turns the hormone into a drug. In the nonclinical package the modified peptide resisted dipeptidyl aminopeptidase-IV, and repeat dosing raised growth hormone and IGF-1 in rats, dogs and pigs. Dogs given repeated subcutaneous doses developed reversible liver, kidney and blood-count changes that the authors attributed to prolonged exposure to supraphysiological growth hormone and IGF-1. | preclinical | not recorded | Ferdinandi ES, Brazeau P, High K, et al. Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue.Basic and Clinical Pharmacology and Toxicology 100(1):49-58, 2007 |
| Randomized data outside HIV do exist. Sixty abdominally obese adults with reduced growth hormone secretion took 2 mg daily or placebo for 12 months; visceral fat fell against placebo by 35 square centimeters (95 percent confidence interval -58 to -12, P = 0.003), abdominal subcutaneous fat did not change significantly, and fasting glucose, 2-hour glucose and glycated hemoglobin were unchanged. That cohort was selected for reduced growth hormone secretion, so it is not a test in people with an intact axis, and nearly all of the randomized evidence for the compound still comes from people with HIV. | rct | not recorded | Makimura H, Feldpausch MN, Rope AM, et al. Metabolic effects of a growth hormone-releasing factor in obese subjects with reduced growth hormone secretion: a randomized controlled trial.Journal of Clinical Endocrinology and Metabolism 97(12):4769-4779, 2012 |
| Outside the approved HIV indication, tesamorelin is used at 1 to 2 mg injected before bed for visceral fat and body composition, mostly by people whose growth hormone axis is intact. Community practice also runs to reconstituting one vial, keeping it in the refrigerator, and drawing from it across several days rather than mixing a fresh dose for each injection. The approved labeling for the single-dose presentation says the opposite: give the dose immediately after reconstitution, discard what is left, and do not freeze or refrigerate the reconstituted solution. | anecdotal | not recorded | community reports aggregated from reddit, MESO-Rx, and similar forumsno study |
How did it get here?
- preclinical1982
- Human GHRH is isolated and sequenced, not from hypothalamus but from pancreatic islet tumors that had caused acromegaly. The 44-residue amidated form, GHRH(1-44)-NH2, becomes the parent of every later analog.
- preclinical1986
- Frohman and colleagues show that plasma clips the first two residues off GHRH(1-44)-NH2, leaving GHRH(3-44)-NH2 with under a thousandth of the parent's activity. Half-life after an intravenous bolus in humans: 6.8 minutes. That result defines the problem any injectable GHRH has to solve.
- preclinical1993-2001
- Theratechnologies, founded in Montreal in 1993, works through acyl-modified GRF analogs and settles on TH9507, which carries a trans-3-hexenoyl group on tyrosine-1. The nonclinical package, published in 2007, reports resistance to dipeptidyl aminopeptidase-IV and sustained growth hormone and IGF-1 responses in rats, dogs and pigs.
- first-human2002-2007
- The earliest human study on the public trial registry is a Theratechnologies phase 2 that ran from February to November 2002: 55 adults with stable type 2 diabetes, randomized double-blind to placebo or 1 or 2 mg of TH9507 daily for 12 weeks. It was registered retrospectively in 2010 and no results were ever posted. The first published human trial follows in 2005, randomizing 61 patients with HIV and central fat accumulation to placebo or 1 or 2 mg daily for 12 weeks: trunk fat falls 9.2 percent in the 2 mg group against a 0.8 percent rise on placebo, while the visceral fat change does not reach significance. The first phase 3 trial, published in 2007, randomizes 412 patients to 2 mg daily for 26 weeks and meets its visceral fat endpoint; a second phase 3 trial of the same design brings the program to 806 patients.
- clinical-adoption2010-2026
- The FDA approves Egrifta in November 2010; it is still the only drug approved for excess abdominal fat in HIV-associated lipodystrophy. Two later reformulations lower the labeled daily dose without touching the molecule: 1.4 mg from a 2 mg vial in 2019, then 1.28 mg from an 11.6 mg vial reconstituted once a week in March 2025. Development outside HIV has not produced a second approved indication: both current labels carry the HIV lipodystrophy indication and nothing else. A randomized, double-blind phase 2 trial at Massachusetts General Hospital assigned 51 adults with obesity and non-alcoholic fatty liver disease, none of them selected for HIV, to 2 mg daily (given as 1.4 mg of the F4 formulation) or placebo for 12 months. Liver fat was measurable in 34 of them, 18 on drug and 16 on placebo, and the median relative change in hepatic fat fraction was a 5.3 percent fall on tesamorelin against a 3.6 percent rise on placebo. Those results reached the public trial registry in November 2025.
- grey-marketafter 2010
- Research-chemical suppliers begin selling lyophilized tesamorelin labeled not for human use, in vial sizes with no pharmaceutical counterpart. Compounding pharmacies and wellness clinics were the other route. The compounding exemption in the Food, Drug, and Cosmetic Act reaches a compounded drug product's new-drug approval requirement, not the separate license a biological product needs, so the March 2020 reclassification took the footing out from under that route; tesamorelin powder is nonetheless still listed in the FDA national drug code directory as a bulk ingredient for human prescription compounding, with registrations dated into 2026. The sequence runs backwards from the usual grey-market peptide: tesamorelin finished a full phase 3 program and was approved first, and the unapproved supply copied the approved dose afterward.
How is it made?
Production happens in four stages.
1. Building the chain. The 44-residue backbone is assembled by solid-phase synthesis, one residue at a time on a resin bead, each coupled and deprotected before the next. A coupling that succeeds 99 percent of the time still leaves about a third of the chains incomplete after 44 rounds, so peptides this long are usually built as fragments and joined.
2. Adding the cap. The finished chain is acylated with trans-3-hexenoic acid at the free amine of the N-terminal tyrosine, six carbons with a double bond at position 3. Without it, dipeptidyl peptidase-4 clips the first two residues in circulation and leaves an inactive fragment.
3. Cleaving and purifying. The peptide comes off the resin, protecting groups are stripped, and preparative reverse-phase chromatography must resolve the correct 44-mer from deletion sequences one residue short. What survives is isolated as an acetate salt.
4. Filling the vial. The two approved presentations differ. The 2 mg Egrifta SV vial is freeze-dried with mannitol and sucrose, histidine as buffer and a trace of polysorbate 20, then mixed with sterile water, injected at once, the rest discarded. The 11.6 mg Egrifta WR vial swapped that for hydroxypropyl betadex and mannitol; one reconstituted vial covers seven daily doses at room temperature, never refrigerated.
The chemistry is ordinary. What varies outside regulated manufacturing is whether the deletion sequences were separated out, whether the fill was sterile, and whether the number on the label describes peptide content or gross powder weight.
Worth knowing
Human GHRH was not first purified from a hypothalamus. It was purified from pancreatic islet tumors removed from patients whose acromegaly the tumors had caused by secreting the hormone; hypothalamic tissue yielded too little to sequence. The second author on that 1982 paper, Paul Brazeau, had first-authored the paper that isolated somatostatin, the hormone that brakes growth hormone release (Brazeau P, Vale W, Burgus R, et al. Hypothalamic polypeptide that inhibits the secretion of immunoreactive pituitary growth hormone. Science 179(4068):77-79, 1973). Twenty-five years later his name appears again, second author on the 2007 nonclinical package for TH9507 cited above, the compound that became tesamorelin.
Guillemin R, Brazeau P, Bohlen P, et al. Growth hormone-releasing factor from a human pancreatic tumor that caused acromegaly.Science 218(4572):585-587, 1982
Tesamorelin is 44 amino acids long. A 2020 FDA rule defined a protein as any amino acid polymer longer than 40 residues, so on 23 March 2020 tesamorelin became a biological product rather than a drug. Nothing about the molecule changed. The consequence is procedural: its 2025 reformulation went to the FDA as a supplemental biologics license application, not a supplemental new drug application.
US Food and Drug Administration. Definition of the term biological product: final rule.Federal Register 85:10057-10063, 2020
Less than 4 percent of a subcutaneous tesamorelin dose reaches the circulation intact. That figure was measured on the original 1 mg per vial formulation, and both current labels still quote it as the only absolute bioavailability on record. What does reach the circulation is largely cleared within the hour. That is enough, because the peptide is a trigger rather than a replacement: it sets off a pituitary growth hormone pulse whose downstream IGF-1 signal outlasts the injected molecule by a wide margin. Reformulation has since let the labeled daily dose fall twice with no change to the molecule, from 2 mg in 2010 to 1.4 mg in 2019 to 1.28 mg in 2025, each delivering similar systemic exposure.
US Food and Drug Administration approved labeling for tesamorelin (Egrifta SV, Egrifta WR), sections 2.1, 11 and 12.3.Biologics license 022505, labeling effective July 2026
Reconstitution
Tesamorelin ships lyophilized and is mixed before use; the published vial strengths are 2, 1, 5, 10, 11.6 mg. The water volume you add sets the concentration, not the dose -- the calculator turns a vial size and a water volume into mg/mL, draw volume, and units on an insulin syringe.
Open in the reconstitution calculatorWritten and reviewed by Evan Marlow, developer of DosePlot · Updated 2026-08-27
Not medical advice. DosePlot is an informational tool, not a healthcare provider, and using it creates no provider-patient relationship. Do not start, stop, or change any protocol without the approval of a licensed healthcare professional.
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