Tabimorelin

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Tabimorelin
File:Tabimorelin.png
Systematic (IUPAC) name
N-[(2E)-5-amino-5-methylhex-enoyl]-N-methyl-3-(2-naphthyl)alanyl-N,Nα-dimethyl-D-phenylalaninamide
Identifiers
ATC code none
PubChem CID 9810101
Synonyms ((2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide)
Chemical data
Formula C32H40N4O3
Molar mass 528.683 g/mol[[Script error: No such module "String".]]
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Tabimorelin (NN-703) 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.[1] 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.[2][3] However actual clinical effects on growth-hormone deficient adults were limited, with only the most severely GH-deficient patients showing significant benefit,[4] and tabimorelin was also found to act as a CYP3A4 inhibitor which could cause it to have undesirable interactions with other drugs.[5]

See also

References

  1. Jump up Hansen BS, Raun K, Nielsen KK, Johansen PB, Hansen TK, Peschke B, Lau J, Andersen PH, Ankersen M. Pharmacological characterisation of a new oral GH secretagogue, NN703. European Journal of Endocrinology. 1999 Aug;141(2):180-9. PMID 10427162
  2. Jump up Zdravkovic M, Søgaard B, Ynddal L, Christiansen T, Agersø H, Thomsen MS, Falch JE, Ilondo MM. The pharmacokinetics, pharmacodynamics, safety and tolerability of a single dose of NN703, a novel orally active growth hormone secretagogue in healthy male volunteers. Growth Hormone and IGF Research. 2000 Aug;10(4):193-8. PMID 11032702
  3. Jump up Zdravkovic M, Christiansen T, Eliot L, Agersoe H, Thomsen MS, Falch JF, Søgaard B, Ynddal L, Ilondo MM. The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects. Growth Hormone and IGF Research. 2001 Feb;11(1):41-8. PMID 11437473
  4. Jump up Svensson J, Monson JP, Vetter T, Hansen TK, Savine R, Kann P, Bex M, Reincke M, Hagen C, Beckers A, Ilondo MM, Zdravkovic M, Bengtsson BA, Korbonits M; NN703 Clinical Research Group. Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency. Clinical Endocrinology. 2003 May;58(5):572-80. PMID 12699438
  5. Jump up Zdravkovic M, Olsen AK, Christiansen T, Schulz R, Taub ME, Thomsen MS, Rasmussen MH, Ilondo MM. A clinical study investigating the pharmacokinetic interaction between NN703 (tabimorelin), a potential inhibitor of CYP3A4 activity, and midazolam, a CYP3A4 substrate. European Journal of Clinical Pharmacology. 2003 Feb;58(10):683-8. PMID 12610745