Tabimorelin

Tabimorelin

Skeletal structure of Tabimorelin

Tabimorelin is a synthetic growth hormone secretagogue that was developed for its potential to stimulate the secretion of growth hormone (GH) in humans. It belongs to a class of compounds known as ghrelin mimetics, which act on the growth hormone secretagogue receptor (GHS-R) to promote the release of growth hormone from the pituitary gland.

Mechanism of Action

Tabimorelin functions by binding to the growth hormone secretagogue receptor (GHS-R1a), which is a G-protein coupled receptor located primarily in the pituitary gland and the hypothalamus. Upon binding to this receptor, Tabimorelin mimics the action of the endogenous hormone ghrelin, leading to the activation of intracellular signaling pathways that result in the release of growth hormone into the bloodstream.

Clinical Applications

The primary clinical application of Tabimorelin was intended to be the treatment of growth hormone deficiency in adults. By stimulating the release of endogenous growth hormone, Tabimorelin could potentially improve body composition, increase muscle mass, and enhance overall physical performance in individuals with insufficient growth hormone levels.

Development and Research

Tabimorelin was developed by Pharmacia and underwent various stages of clinical trials to assess its efficacy and safety. However, despite its promising mechanism of action, the development of Tabimorelin was eventually discontinued. The reasons for discontinuation included suboptimal efficacy in clinical trials and the emergence of side effects that outweighed the potential benefits.

Pharmacokinetics

Tabimorelin is administered orally and is absorbed through the gastrointestinal tract. It undergoes hepatic metabolism and is excreted primarily via the kidneys. The pharmacokinetic profile of Tabimorelin includes a relatively short half-life, which necessitates frequent dosing to maintain therapeutic levels of growth hormone stimulation.

Side Effects

Common side effects associated with Tabimorelin include nausea, headache, and dizziness. More serious adverse effects can include edema, arthralgia, and hyperglycemia. The risk of side effects was a significant factor in the decision to halt further development of the drug.

Related Pages

• Growth hormone secretagogue
• Ghrelin
• Growth hormone deficiency
• Pituitary gland