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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''.〔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〕 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.〔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〕〔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〕 However actual clinical effects in adults with growth hormone deficiency were limited, with only the most severely GH-deficient patients showing significant benefit,〔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〕 and tabimorelin was also found to act as a CYP3A4 inhibitor which could cause it to have undesirable interactions with other drugs.〔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〕 ==See also== * Anamorelin * Capromorelin * Examorelin (hexarelin) * GHRP-6 (SKF-110679) * Ibutamoren (MK-677) * Ipamorelin * Macimorelin * Pralmorelin (GHRP-2) * Relamorelin * SM-130,686 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Tabimorelin」の詳細全文を読む スポンサード リンク
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