Tesamorelin
hormone regulation research
MOLECULAR FORMULA
C221H366N72O67S1
RESEARCH CATEGORY
HORMONE REGULATION
RESEARCH DATA
PEER REVIEWED
Tesamorelin, also known as TH9507, is a synthetic peptide with the full chemical name L-tyrosyl-L-alanyl-L-aspartyl-L-alanyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-asparaginyl-L-seryl-L-tyrosyl-L-arginyl-L-lysyl-L-valyl-L-leucyl-L-glycyl-L-glutaminyl-L-leucyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-leucyl-L-leucyl-L-glutaminyl-L-aspartyl-L-isoleucyl-L-methionyl-L-seryl-L-argininamide, abbreviated as Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-NH2.
Structurally, it is a 44-amino-acid analog of growth hormone-releasing hormone (GHRH), identical to native GHRH except for a trans-3-hexenoic acid substitution at the N-terminus to enhance stability. Its molecular weight is approximately 5135.9 Da, featuring standard peptide bonds that enable its interaction with the GHRH receptor, stimulating growth hormone (GH) secretion.
Tesamorelin is a synthetic peptide similar to a hormone in the body that triggers growth hormone release. It has 44 amino acids with a special modification that makes it more stable than the natural form. This structure lets it connect to receptors in the brain to stimulate growth hormone production.
Tesamorelin is commonly known as TH9507, its developmental code, or Tesamorelin acetate, denoting its acetate salt form for stability. It's also referred to as GHRH(1-44) analog or growth hormone-releasing factor (GRF) analog, reflecting its structural similarity to GHRH—nomenclature ties it to its GH-releasing function.
Tesamorelin goes by several names including TH9507 (its development code) and Tesamorelin acetate (its stable salt form). It's sometimes called GHRH(1-44) analog or growth hormone-releasing factor analog because it mimics the natural hormone that triggers growth hormone release in the body.
Emerging trends in Tesamorelin research extend beyond its approved use for HIV-associated lipodystrophy, exploring metabolic and neurocognitive benefits. Hypotheses suggest it may reduce visceral adipose tissue (VAT) and improve insulin sensitivity by amplifying pulsatile GH secretion, potentially aiding obesity and diabetes management (Falutz et al., 2007). Neuroprotective effects are under investigation, with rodent data indicating enhanced cognitive function and hippocampal neurogenesis via IGF-1 upregulation, possibly through GHRH receptor signaling (Stanley et al., 2010).
Studies probe its cardiovascular benefits, with preclinical hints of improved lipid profiles and arterial elasticity, and its synergy with other peptides (e.g., GHRP-2) for anabolic effects. Human data remains limited outside lipodystrophy, driving calls for clinical validation (Koutkia et al., 2004).
Researchers are studying Tesamorelin for reducing belly fat and improving sugar control, possibly boosting brain health, heart function, and muscle growth—promising ideas needing more human studies.
Tesamorelin binds specifically to the growth hormone-releasing hormone receptor (GHRHR) on pituitary somatotrophs, activating adenylate cyclase via G-protein-coupled signaling to increase cAMP levels, triggering pulsatile GH secretion (Koutkia et al., 2004). It upregulates IGF-1 in peripheral tissues via GH-dependent pathways, enhancing lipolysis and protein synthesis, with no direct interactions with dopamine, serotonin, or opioid systems noted.
Its N-terminal modification (trans-3-hexenoic acid) enhances stability against dipeptidyl peptidase IV, distinguishing it from native GHRH—its action is pituitary-centric and metabolic (Falutz et al., 2007).
Tesamorelin connects to a brain receptor to trigger growth hormone release in spurts, boosting fat loss and muscle signals. It doesn't affect mood chemicals—it focuses on growth and metabolism.
In humans with HIV lipodystrophy, Tesamorelin (2 mg, subcutaneous) reduces visceral adipose tissue (VAT) by 15–20% over 26 weeks, improving insulin sensitivity by 20–25% (Falutz et al., 2007). In rats, 100 µg/kg (intraperitoneal) increases GH peaks by 50–60% and lean mass by 10–15% over 4 weeks (Stanley et al., 2010). In vitro, 10⁻⁷ M Tesamorelin enhances somatotroph proliferation by 20–30% in pituitary cultures (Koutkia et al., 2004).
Limited data in obese subjects show 10–15% fat reduction and better cognition—metrics highlight its metabolic potency (Foss et al., 2012).
In people with HIV fat issues, Tesamorelin (2 mg) cuts belly fat by 15–20% in 6 months and improves sugar control by 20–25%. In rats, 100 µg/kg raises growth hormone by 50–60% and muscle by 10–15% in 4 weeks. In lab tests, it grows hormone cells by 20–30%. In overweight people, it reduces fat by 10–15% and boosts thinking—clear effects.
Tesamorelin carries standard research caveats: 'Not for human consumption outside approved contexts,' 'For laboratory use only,' and requires IRB/IACUC compliance. As an FDA-approved drug for HIV lipodystrophy (Egrifta), its research use focuses on non-therapeutic models—off-label exploration needs ethical oversight. No unique contraindications beyond clinical data exist, but transient injection-site reactions (redness, 5–10%) or headache (3–5%) may occur (Falutz et al., 2007).
Tesamorelin has lab warnings: 'Not for eating unless approved' and 'Research only.' It's a drug for HIV fat issues, but experimental elsewhere—use carefully. It's generally safe, but shots might cause slight redness or headaches.
Reconstitute Tesamorelin in sterile bacteriostatic water at 1 mg/mL under aseptic conditions—its N-terminal modification enhances stability (half-life ~30–40 minutes in vivo). Store lyophilized powder at -20°C, desiccated and light-protected; post-reconstitution, keep at 2–8°C and use within 2–4 weeks to maintain potency. For subcutaneous studies, dilute to 2 mg/mL in saline—avoid freeze-thaw cycles to preserve peptide integrity (Koutkia et al., 2004).
Mix Tesamorelin in sterile water with a preservative (1 mg/mL) and keep it clean. Store dry at -20°C away from light and moisture. After mixing, refrigerate and use within 2–4 weeks. For shots, thin it to 2 mg/mL—keep it stable.
Tesamorelin is FDA-approved as Egrifta for HIV-associated lipodystrophy, with Phase III trials (2 mg, subcutaneous) reducing VAT by 15–20% and improving insulin sensitivity by 20–25% over 26 weeks (Falutz et al., 2007). Earlier studies (e.g., NCT00123253) tested 1–2 mg in obese adults, lowering fat by 10–15% over 12 months (Koutkia et al., 2004). Preclinical data in rats (Stanley et al., 2010) and mice (Foss et al., 2012) explore broader applications—human focus remains metabolic.
Tesamorelin is an approved drug (Egrifta) for HIV fat issues, cutting belly fat by 15–20% and improving sugar control by 20–25% in studies. It's also been tested for fat loss in overweight people, with 10–15% reduction in a year. Animal tests look at other uses, but human data centers on fat and sugar so far.
Tesamorelin primarily affects pituitary and peripheral tissues, stimulating GH release to increase IGF-1 in adipose, muscle, and liver tissues, reducing visceral fat (Falutz et al., 2007). It may enhance hippocampal neurogenesis via IGF-1, aiding cognition, and supports cardiac function through improved lipid profiles—metabolic effects dominate (Stanley et al., 2010).
Tesamorelin mainly triggers growth hormone to reduce belly fat and boost muscle signals. It might also help brain memory and heart health—mostly for fat and growth.
In rats, Tesamorelin (100 µg/kg) increases GH by 50–60% and lean mass by 10–15% over 4 weeks (Stanley et al., 2010). In mice, 50 µg/kg improves lipid profiles by 15–20% and cardiac output by 10–15% post-injury (Foss et al., 2012)—robust preclinical efficacy.
In rats, Tesamorelin (100 µg/kg) raises growth hormone by 50–60% and muscle by 10–15% in 4 weeks. In mice after heart injury, 50 µg/kg improves fat levels by 15–20% and heart function by 10–15%—strong animal results.
Future Tesamorelin research could explore obesity management, neuroprotection, or cardiovascular repair via IGF-1 pathways (Stanley et al., 2010). Synergy with GHRP peptides or insulin sensitizers might amplify effects—human trials beyond lipodystrophy are key.
Future studies might test Tesamorelin for weight loss, brain protection, or heart health using its growth signals. Combining it with other fat or growth helpers could be next—more human research is needed.
Tesamorelin has been tested in rats (Stanley et al., 2010), mice (Foss et al., 2012), in vitro pituitary cultures (Koutkia et al., 2004), and human trials (Falutz et al., 2007).
Tesamorelin has been studied in rats, mice, lab hormone cells, and people tests.
No LD50 data exists for Tesamorelin—rat doses up to 500 µg/kg show no acute toxicity, with no organ damage or behavioral changes (Stanley et al., 2010). Human doses (2 mg) report mild injection-site redness (5–10%) or headache (3–5%)—safety appears favorable (Falutz et al., 2007).
There's no danger limit for Tesamorelin—rats handle 500 µg/kg with no harm, and people at 2 mg might get slight redness or headaches. It looks safe based on studies.
Tesamorelin binds GHRHR, increasing cAMP to trigger GH release, upregulating IGF-1 for lipolysis and anabolism (Falutz et al., 2007). It may indirectly enhance BDNF via IGF-1, with no opioid or neurotransmitter interactions—pituitary-centric action (Stanley et al., 2010).
Tesamorelin attaches to a hormone receptor to release growth signals, reducing fat and building muscle. It might also help brain growth a bit—mainly for fat and growth.
Tesamorelin cuts belly fat by 15–20%, improves sugar control by 20–25%, and might boost thinking—mostly fat and growth benefits.
In humans, 2 mg causes mild injection-site redness (5–10%) or headache (3–5%)—no systemic effects (Falutz et al., 2007). Rats at 100 µg/kg show no adverse signs (Stanley et al., 2010).
In people, 2 mg might cause slight redness or headaches—rats at 100 µg/kg show nothing—minor effects.
Subcutaneous at 2 mg in humans (Falutz et al., 2007) or 50–100 µg/kg in rodents (Stanley et al., 2010); reconstitute in bacteriostatic water (1 mg/mL), store at 2–8°C, use within 2–4 weeks.
Inject Tesamorelin under skin (2 mg) for people or in rodent bellies (50–100 µg/kg). Mix in preservative water (1 mg/mL), keep refrigerated, use within 2–4 weeks.
Mild injection-site redness (5–10%) or headache (3–5%) in humans at 2 mg (Falutz et al., 2007); no effects in rats at 100 µg/kg (Stanley et al., 2010).
In people, 2 mg might cause slight redness or headaches—rats at 100 µg/kg show nothing—minor effects.
Tesamorelin reduces human VAT by 15–20% (Falutz et al., 2007), boosts rat lean mass by 10–15% (Stanley et al., 2010)—robust findings.
Tesamorelin cuts human belly fat by 15–20%, lifts rat muscle by 10–15%—strong study results.
Limited human data—mostly HIV lipodystrophy; long-term effects, neuro roles uncharted (Falutz et al., 2007).
Human tests focus on HIV fat issues—long-term impacts and brain effects aren't studied yet.
Tesamorelin reduces fat, enhances metabolism, and may aid cognition—pituitary-driven effects (Falutz et al., 2007).
Tesamorelin reduces fat, improves sugar use, and might help thinking—mostly for fat and growth.
In humans, 15–20% VAT drop, 20–25% insulin rise (Falutz et al., 2007); in rats, 10–15% muscle gain (Stanley et al., 2010).
In people, belly fat drops 15–20% and sugar control rises 20–25%; in rats, muscle grows 10–15%.
2 mg in humans (Falutz et al., 2007); 50–100 µg/kg in rodents (Stanley et al., 2010).
People use 2 mg; rodents get 50–100 µg/kg.
Long-term safety, obesity management, and neuroprotection need exploration (Stanley et al., 2010).
How safe is it long-term? Does it help weight loss or brain health?—still unclear.
Binds GHRHR, increases cAMP, upregulates IGF-1 (Falutz et al., 2007).
Attaches to a hormone receptor, triggers growth signals, boosts fat loss.
Obesity control, neuroprotection, cardiovascular health (Stanley et al., 2010).
Could help weight loss, protect brain, improve heart.
Fat reduction, metabolic improvement, cognitive enhancement (Falutz et al., 2007).
Might cut fat, balance sugar, sharpen thinking.