Tesamorelin — FDA-Referenced Growth Hormone-Releasing Hormone Analog Research Peptide | Klene Peptides
For Research Use Only | Not for Human or Veterinary Administration
Tesamorelin is a synthetic analog of endogenous growth hormone-releasing hormone (GHRH), comprising the full 44-amino acid GHRH sequence modified at the N-terminus with a trans-3-hexenoic acid group to enhance biological stability against DPP-IV enzyme degradation. Approved by the FDA in 2010 under the trade name Egrifta® for the reduction of excess abdominal fat (lipodystrophy) in HIV-infected patients on antiretroviral therapy, tesamorelin is among the most clinically validated GHRH analogs in the research literature. Its mechanism — stimulating pulsatile GH release from anterior pituitary somatotroph cells, increasing IGF-1, and driving selective visceral adipose reduction — has generated significant research interest beyond its approved indication, including investigations into general lipodystrophy, cardiovascular risk reduction, cognitive function, and GH restoration in aging-associated metabolic decline. Klene Peptides supplies tesamorelin to USA research institutions with verified purity and same-day fulfillment.
Every vial from Klene Peptides includes:
- ≥99%+ purity — verified by HPLC (High-Performance Liquid Chromatography)
- HPLC-MS (High-Performance Liquid Chromatography - Mass Spectrometry)
- Same-day shipping for all USA orders
Chemical Identity & Structural Profile
| Parameter | Value |
|---|---|
Full Name | Tesamorelin |
INN | Tesamorelin |
Brand Name | Egrifta® (FDA-approved) |
Sequence Basis | Full GHRH(1-44) amino acid sequence |
N-terminal Modification | Trans-3-hexenoic acid conjugated to Tyr¹ |
Amino Acid Count | 44 amino acids |
Molecular Weight | ~5,135 Da |
CAS Number | 218949-48-5 |
FDA Approval | 2010 — HIV-associated lipodystrophy (visceral adiposity) |
Appearance | White lyophilized powder |
Solubility | Water, saline |
Storage | Lyophilized: −20°C; Reconstituted: 4°C, use same day or within 24 hours |
The trans-3-hexenoic acid N-terminal modification substantially enhances tesamorelin’s stability relative to native GHRH by protecting the Ala² position against DPP-IV cleavage — the primary route of native GHRH inactivation in plasma. This modification extends functional half-life while maintaining full, high-affinity GHRH receptor agonist activity.
Mechanism of Action
GHRH Receptor Signaling
| Step | Mechanism | Effect |
|---|---|---|
GHRHR binding | High-affinity agonism at pituitary GHRH receptor | Somatotroph cell activation |
Gs/cAMP pathway | Adenylate cyclase → cAMP → PKA activation | GH gene transcription + secretory vesicle exocytosis |
GH pulse release | Pulsatile secretion from anterior pituitary | Systemic GH elevation |
IGF-1 induction | Hepatic GH receptor → IGF-1 synthesis and secretion | Downstream anabolic and metabolic signaling |
Downstream Metabolic Effects
| Effect | Mechanism | Research Context |
|---|---|---|
Visceral adipose reduction | GH → lipolysis in visceral adipocytes; lipogenesis inhibition | Primary FDA-approved endpoint |
Triglyceride reduction | GH/IGF-1-driven lipid metabolism normalization | Cardiometabolic risk research |
LDL reduction | Secondary to visceral fat reduction and lipid metabolism | Cardiovascular biomarker research |
Lean body mass maintenance | IGF-1 anabolic signaling | Body composition endpoint studies |
Glucose/insulin modulation | GH-induced insulin resistance (dose-dependent) | Metabolic safety monitoring in research protocols |
Pharmacokinetic & ADME Profile
| Parameter | Value | Notes |
|---|---|---|
Molecular Weight | ~5,135 Da | SC delivery; IM not standard |
Route (Research / Approved) | SC | Single daily injection in approved clinical use |
Bioavailability (SC) | ~4.5% (absolute bioavailability, HIV patient data) | N-terminal modification extends vs. native GHRH |
Tmax | ~15–30 minutes (SC) | Rapid GH peak post-administration |
Half-life (t½) | ~26–38 minutes | Significantly extended vs. native GHRH (~7 minutes) |
Duration of GH Elevation | ~3–5 hours post-dose | Outlasts plasma half-life due to receptor signaling kinetics |
Metabolism | DPP-IV resistant (N-terminal protection); downstream proteolytic | Substantially reduced first-pass DPP-IV inactivation |
Excretion | Renal | Metabolite clearance |
Research Applications
HIV-Associated Lipodystrophy (Clinical Reference Context)
Tesamorelin’s FDA approval is grounded in Phase III clinical data:
| Clinical Endpoint | Result |
|---|---|
Visceral adipose tissue (VAT) | ~15–20% reduction vs. placebo at 26 weeks |
Triglycerides | Significant reduction |
Trunk fat ratio | Improved body composition parameters |
IGF-1 | Dose-dependent elevation |
Glucose / HbA1c | Modest increase — monitored as safety parameter |
Source: Falutz J, et al., NEJM 2007; Dhillon S, Drugs 2011
Visceral Adiposity Research (Non-HIV Context)
Research has expanded tesamorelin investigation into broader metabolic contexts:
- Age-associated abdominal adiposity (somatopause-related VAT accumulation)
- Metabolic syndrome and cardiovascular risk factor modeling
- Comparative effectiveness vs. other GHRH analogs and GH secretagogues
- Non-alcoholic fatty liver disease (NAFLD) — hepatic fat quantification studies
Cognitive Function Research
Emerging research has investigated tesamorelin’s neurocognitive effects based on:
- GH and IGF-1 support of hippocampal neuroplasticity
- Tesamorelin clinical trials measuring cognitive composite scores as secondary endpoints
- IGF-1 elevation as a mediator of neuroprotective effects in aging populations
Cardiovascular & Cardiometabolic Research
| Parameter | Direction | Mechanism |
|---|---|---|
Carotid intima-media thickness (cIMT) | Reduction in some published studies | Lipid normalization, reduced visceral inflammation |
LDL-C and triglycerides | Reduction | GH-mediated lipid metabolism |
Visceral adipose mass | Reduction | Direct anti-lipogenic and lipolytic effect |
Inflammatory markers | Under investigation | Secondary to metabolic parameter improvement |
Research Dosing Reference
For scientific reference only — not prescriptive recommendations
| Research Context | Reported Dose | Route | Duration |
|---|---|---|---|
FDA-approved clinical reference | 2 mg once daily | SC | 26–52 weeks |
Preclinical GH pulse studies | 100–300 mcg/kg | SC | Acute or repeated |
Metabolic research (rodent) | 1–2 mg/kg/day (scaled) | SC | 4–12 weeks |
In vitro receptor binding | 1–100 nM | Cell culture | Per experiment |
Egrifta® clinical dose provided as reference context only.
Reconstitution Reference
| Lyophilized Amount | Sterile Water | Concentration |
|---|---|---|
2 mg | 1.0 mL | 2.0 mg/mL |
5 mg | 2.5 mL | 2.0 mg/mL |
10 mg | 5.0 mL | 2.0 mg/mL |
Klene Peptides Quality Standards
Certificate of Analysis — Standard Parameters
Every batch supplied by Klene Peptides is verified against the following analytical benchmarks:
| Test | Specification | Method |
|---|---|---|
Purity | ≥99% | HPLC (High-Performance Liquid Chromatography) |
Molecular Identification | Confirmed | HPLC-MS (High-Performance Liquid Chromatography – Mass Spectrometry) |
Water Content | <1.5% | — |
What Every Klene Peptides Order Includes
- Lot-specific Certificate of Analysis traceable to synthesis batch
- Verified cold-chain shipping — all orders dispatched with appropriate cold-pack packaging
- Same-day fulfillment — orders placed before cutoff ship the same business day
Ordering Tesamorelin for Your Research Program
Important Research Compliance Notice
Scientific References
- Falutz J, et al. "Metabolic effects of a growth hormone-releasing factor in patients with HIV." N Engl J Med. 2007;357(23):2359-2370.
- Falutz J, et al. "Effects of tesamorelin (TH9507), a growth hormone-releasing factor analog, in HIV-infected patients with abdominal fat accumulation." J Acquir Immune Defic Syndr. 2010;53(3):311-322.
- Dhillon S. "Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy." Drugs. 2011;71(8):1071-1091.
- Stanley TL, et al. "Effects of tesamorelin on non-alcoholic fatty liver disease in HIV-infected patients." AIDS. 2019.
- Sigalos JT, Pastuszak AW. "The Safety and Efficacy of Growth Hormone Secretagogues." Sex Med Rev. 2018;6(1):45-53.
- FDA. Egrifta® (tesamorelin for injection) Prescribing Information. 2010.
- PubChem. Tesamorelin. CID: 16130415. https://pubchem.ncbi.nlm.nih.gov