Tabimorelin

Tabimorelin
Clinical data
ATC code none
Identifiers
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)
PubChem (CID) 9810101
ChemSpider 7985857
UNII L51CBE03KF YesY
Chemical and physical data
Formula C32H40N4O3
Molar mass 528.683 g/mol
3D model (Jmol) Interactive image
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Tabimorelin (INN) (developmental code name NN-703) is a drug which acts as a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue, mimicking the effects of the endogenous peptide agonist ghrelin as a stimulator of growth hormone (GH) 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 GH and insulin-like growth factor 1 (IGF-1), along with smaller transient increases in levels of other hormones such as adrenocorticotropic hormone (ACTH), cortisol, and prolactin.[2][3] However actual clinical effects in adults with growth hormone deficiency 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. ↑ 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. ↑ 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. ↑ 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. ↑ 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. ↑ 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



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