Tesamorelin (acetate)
Tesamorelin (acetate) CAS：901758-09-6 is a synthetic, stabilized 44‑amino‑acid peptide analog of human growth hormone‑releasing hormone (GHRH), marketed under the brand name Egrifta (including Egrifta SV and Egrifta WR). It is the only FDA‑approved GHRH analog for clinical use, primarily indicated for reducing excess abdominal fat in adults with HIV‑associated lipodystrophy.
Description
Tesamorelin acetate is derived from the full‑length human GHRH(1‑44) sequence, with a trans‑3‑hexenoyl moiety covalently attached to the N‑terminal tyrosine residue. This modification protects the peptide from rapid degradation by dipeptidyl peptidase‑4 (DPP‑4), extending its half‑life to 26–38 minutes and preserving its biological activity. As an acetate salt, it offers improved solubility, stability, and consistency for pharmaceutical formulation.
Mechanistically, tesamorelin binds to pituitary GHRH receptors to stimulate pulsatile release of endogenous growth hormone (GH), which in turn elevates insulin‑like growth factor‑1 (IGF‑1) levels. This cascade promotes targeted reduction of visceral adipose tissue (VAT), improves lipid profiles, and supports metabolic homeostasis—without disrupting natural GH feedback loops.
Key Features
- FDA‑Approved Clinical Peptide: Rigorously evaluated in Phase III trials; approved in 2010 for HIV‑associated lipodystrophy.
- Stabilized GHRH Analog: N‑terminal modification confers DPP‑4 resistance and extended half‑life.
- Visceral Fat Targeting: Selectively reduces abdominal VAT while preserving lean mass.
- Metabolic Benefits: Improves triglyceride levels and supports glucose homeostasis.
- Pulsatile GH Release: Mimics natural GH secretion, minimizing risks of GH excess.
- Stable Acetate Formulation: Ensures consistent bioavailability and ease of administration.
AxisPharm offers 5000+ PEG Linkers with high purity. Different kinds of PEG Reagents may be available by custom synthesis.
