Tesamorelin

Halmos G, Szabo Z, Dobos N, Juhasz E, Schally AV

Reviews in endocrine & metabolic disorders

A 2025 structural and molecular-biology review characterizes the pituitary growth-hormone-releasing-hormone receptor (GHRH-R) as a seven-transmembrane G-protein-coupled receptor, detailing its splice variants (including the cAMP-signaling, proliferation-linked SV1 variant), receptor activation and regulatory mechanisms, and downstream signaling pathways across pituitary and extrapituitary tissue -- establishing the receptor-pharmacology framework relevant to GHRH-receptor agonists such as tesamorelin.

Granata R, Trovato L, Gallo MP, Destefanis S, Settanni F, Scarlatti F, et al.

Cardiovascular research

In adult rat ventricular myocytes and the H9c2 rat cardiac cell line, activation of the GHRH receptor triggered ERK1/2 and PI3K/Akt signaling that blocked serum-starvation- and isoproterenol-induced apoptosis; a GHRH-receptor antagonist reversed the effect, and in Langendorff-perfused rat hearts GHRH-receptor activation reduced infarct size after ischemia-reperfusion, indicating a receptor-mediated cytoprotective signaling pathway.

Ferdinandi ES, Brazeau P, High K, Procter B, Fennell S, Dubreuil P

Basic & clinical pharmacology & toxicology

Preclinical evaluation of TH9507 (tesamorelin) in rat, dog, and pig models found that N-terminal modification with a trans-3-hexenoyl group conferred resistance to dipeptidyl-peptidase-IV degradation, prolonging plasma persistence relative to native GHRH(1-44) and producing sustained increases in plasma growth hormone and IGF-1 after repeated subcutaneous or intravenous administration in animals; sub-chronic toxicology characterized exposure-related body-weight and organ findings at supraphysiological levels.

Jansen M, Darby I, Abribat T, Dubreuil P, Ferdinandi ES, Hardy JG

International journal of pharmaceutics

In beagle dogs, intratracheal dry-powder delivery of TH9507 (tesamorelin) achieved roughly 41% bioavailability relative to subcutaneous injection with a comparable terminal half-life, characterizing pulmonary absorption kinetics for this GHRH(1-44) peptide analog as an alternative administration route in an animal pharmacokinetic model.