Tesamorelin peptide is a growth hormone releasing hormone (GHRH) analogue consisting of standard GHRH to which an additional trans-3-hexanoic acid group has been added. Produced by Theratechnologies of Canada, Tesamorelin became the newest drug to be approved by the FDA for use in HIV-associated lipodystrophy in 2010. The peptide has also been investigated for its ability to improve peripheral nerve regeneration and as a potential intervention for mild cognitive impairment (MCI), the precursor to dementia.
Sequence (Single Letter): Unk-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-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu
Molecular Formula: C223H370N72O69S
Molecular Weight: 5195.908 g/mol
PubChem CID: 44147413
CAS Number: 901758-09-6
As a GHRH analogue, tesamorelin has all of the same effects as GHRH and GHRH analogues like sermorelin, GRF (1-29), CJC-1295, etc. The addition of trans-3-hexanoic acid to tesamorelin makes it more stable in human plasma and thus increases its half-life. Despite this increase in half-life, tesamorelin, like CJC-1295, preserves the physiological action of GHRH and thus has fewer side effects than similar molecules that obliterate normal pulsatile growth hormone (GH) release.
Tesamorelin Peptide and Lypodystrophy
The primary use for tesamorelin peptide is in the treatment of HIV-associated lipodystrophy, which arises both as a consequence of HIV infection and as a side effect of antiretroviral therapy. In lipodystrophy, fat accumulates excessively both in the abdomen and in other areas of the body. The physiologic mechanism responsible for this is not clearly understood, but it is thought that commonly used protease inhibitors play a large role in the pathogenesis of lipodystrophy.
Patients suffering from lipodystrophy initially had diet, exercise, and a handful of ineffective medications to rely on for treatment. If those did not work, surgery was a last-ditch, often ineffective, and frequently complicated solution. In 2010, however, the FDA approved tesamorelin specifically for the treatment of HIV-associated lipodystrophy. The drug has been found to reduce adiposity by nearly 20% in this population. Research suggests that tesamorelin peptide is approximately 4 times more effective in reducing adiposity than all of the other available therapies combined.