Tabimorelin
Encyclopedia
Tabimorelin is a drug which acts as a potent, orally active growth hormone
secretagogue, mimicking the effects of the endogenous peptide agonist ghrelin
as a stimulator of growth hormone release. It was one of the first GH secretagogues developed and is largely a modified polypeptide, but it is nevertheless orally active in vivo. Tabimorelin produced sustained increases in levels of growth hormone and IGF-1, along with smaller transient increases in levels of other hormones such as ACTH, cortisol and prolactin. However actual clinical effects on growth-hormone deficient adults were limited, with only the most severely GH-deficient patients showing significant benefit, and tabimorelin was also found to act as a CYP3A4
inhibitor which could cause it to have undesirable interactions with other drugs.
Growth hormone
Growth hormone is a peptide hormone that stimulates growth, cell reproduction and regeneration in humans and other animals. Growth hormone is a 191-amino acid, single-chain polypeptide that is synthesized, stored, and secreted by the somatotroph cells within the lateral wings of the anterior...
secretagogue, mimicking the effects of the endogenous peptide agonist ghrelin
Ghrelin
Ghrelin is a 28 amino acid peptide and hormone that is produced mainly by P/D1 cells lining the fundus of the human stomach and epsilon cells of the pancreas that stimulates hunger. Ghrelin levels increase before meals and decrease after meals. It is considered the counterpart of the hormone...
as a stimulator of growth hormone release. It was one of the first GH secretagogues developed and is largely a modified polypeptide, but it is nevertheless orally active in vivo. Tabimorelin produced sustained increases in levels of growth hormone and IGF-1, along with smaller transient increases in levels of other hormones such as ACTH, cortisol and prolactin. However actual clinical effects on growth-hormone deficient adults were limited, with only the most severely GH-deficient patients showing significant benefit, and tabimorelin was also found to act as a CYP3A4
CYP3A4
Cytochrome P450 3A4 , a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. CYP3A4 is involved in the oxidation of the largest range of substrates of all the CYPs. As a result, CYP3A4 is present in...
inhibitor which could cause it to have undesirable interactions with other drugs.