Tabimorelin: Difference between revisions

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'''Tabimorelin''' is a [[growth hormone secretagogue]] and [[ghrelin]] mimetic that is currently under investigation for its potential therapeutic uses. It was developed by [[Theratechnologies]], a Canadian biopharmaceutical company, and is also known by its developmental code names TH9507 and EP1572.
== Tabimorelin ==


== Mechanism of Action ==
[[File:Tabimorelin_skeletal.svg|thumb|right|Skeletal structure of Tabimorelin]]
Tabimorelin works by mimicking the action of ghrelin, a hormone that stimulates the release of [[growth hormone]] from the [[pituitary gland]]. This action is mediated through the [[growth hormone secretagogue receptor]] (GHSR), which is found in various tissues throughout the body, including the pituitary gland and the hypothalamus.


== Clinical Trials ==
'''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]].
Several [[clinical trials]] have been conducted to evaluate the safety and efficacy of tabimorelin. These trials have primarily focused on its potential use in the treatment of [[HIV-associated lipodystrophy]], a condition characterized by abnormal fat distribution and metabolic complications in individuals with [[HIV]].


== Potential Therapeutic Uses ==
=== Mechanism of Action ===
In addition to HIV-associated lipodystrophy, tabimorelin may also have potential therapeutic uses in other conditions associated with growth hormone deficiency or dysfunction, such as [[cachexia]] associated with chronic diseases, [[aging]], and [[cancer]].


== Safety and Side Effects ==
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.
As with any drug, tabimorelin has the potential to cause side effects. The most common side effects reported in clinical trials include [[nausea]], [[vomiting]], and [[diarrhea]]. However, these side effects were generally mild and transient.


== Future Directions ==
=== Clinical Applications ===
While tabimorelin has shown promise in early clinical trials, further research is needed to fully understand its potential therapeutic uses and long-term safety profile.


[[Category:Drugs]]
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.
[[Category:Growth hormones]]
 
[[Category:Experimental drugs]]
=== Development and Research ===
{{Pharma-stub}}
 
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]]
 
[[Category:Growth hormone secretagogues]]
[[Category:Pharmacology]]

Latest revision as of 11:34, 15 February 2025

Tabimorelin[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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[edit]