Tabimorelin Research

Lange T, Thomas A, Görgens C, Bidlingmaier M, Schilbach K, Fichant E et al.

Analytical methods to determine the potential misuse of the ghrelin mimetics capromorelin (CP-424,391), macimorelin (macrilen, EP-01572) and tabimorelin (NN703) in sports were developed. Therefore, different extraction strategies, i.e. solid-phase extraction, protein precipitation, as well as a "...

Shimatsu A

Holm AM, Johansen PB, Ahnfelt-Rønne I, Rømer J

The aim was to investigate the possible interactions of the two peripheral hormones, leptin and ghrelin, that regulate the energy balance in opposite directions.Leptin-receptor mutated Zucker diabetic fatty (ZDF) and lean control rats were treated with the ghrelin-receptor ligand, tabimorelin (50...

Svensson J, Monson JP, Vetter T, Hansen TK, Savine R, Kann P et al.

Little is known of the usefulness of GH secretagogues (GHSs) in GH-deficient (GHD) adults. The objective of this study was to determine the number of responders to treatment with NN703 in GHD adults.A multicentre, randomized, double-blind, and placebo-controlled study.Ninety-seven GHD adults were...

Zdravkovic M, Olsen AK, Christiansen T, Schulz R, Taub ME, Thomsen MS et al.

NN703 (tabimorelin) is an orally active growth hormone (GH) secretagogue intended for use as an alternative to daily injections of GH. In vitro studies in human liver microsomes have indicated that NN703 is a mechanism-based inhibitor of CYP3A4. The aim of the present study was to investigate in ...

Nielsen KK, Buddington KK, Raun K, Hansen TK, Buddington RK

Pharmacokinetics for one growth hormone secretogogue (NNC 26-0722), but not for another (NN703), differ between dogs in estrus or anestrus. We examined if the differences could be mimicked by administering estradiol during anestrus and if there was a relationship with rates of small intestine abs...

Peschke B, Ankersen M, Bauer M, Hansen TK, Hansen BS, Nielsen KK et al.

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidin...

Malmlöf K, Bauer MK, Johansen PB, Ankersen M, Veldhuis JD

Repeated administration of growth hormone secretagogues (GHSs) has proven to be a delicate matter owing to development of tolerance. The aim of the present study was to define conditions during which the responsiveness to the orally active NN703 was maintained over several days. Growing pigs were...

Nagamine J, Nagata R, Seki H, Nomura-Akimaru N, Ueki Y, Kumagai K et al.

SM-130686, an oxindole derivative, is a novel orally active GH secretagogue (GHS) which is structurally distinct from previously reported GHSs such as MK-677, NN703 and hexarelin. SM-130686 stimulates GH release from cultured rat pituitary cells in a dose-dependent manner. Half-maximum stimulatio...

Hansen TK, Ankersen M, Raun K, Hansen BS

A series of NN703 analogues with lysine mimetics combined with naphthyl- or biphenylalanine in the core has been prepared and tested in vitro in a rat pituitary cell based assay and subsequently in vivo in pigs in a single dose at 50 nmol/kg. Re-introduction of certain pharmacophores in the C-ter...

Zdravkovic M, Christiansen T, Eliot L, Agersoe H, Thomsen MS, Falch JF et al.

The aim of the present study was to assess the safety, pharmacokinetics and pharmacodynamics (including specificity) of NN703 (tabimorelin), a growth hormone (GH) secretagogue, in healthy male subjects following treatment for 7 days once-daily. This was a randomized, double-blind and placebo-cont...

Ahnfelt-Rønne I, Nowak J, Olsen UB

NN703 is an orally active and selective growth hormone secretagogue (GHS) that was derived from growth hormone-releasing peptide-1(GHRP-1) via ipamorelin by a peptidomimetic approach and has now entered into phase II clinical trials. When the disposition in rats of NN703 and GHRP-6 was studied us...

Agersø H, Ynddal L, Søgaard B, Zdravkovic M

The objective of this study was to describe the pharmacokinetics and pharmacodynamics of NN703, a growth hormone (GH)-releasing secretagogue, after po administration to healthy human male subjects. The study was designed as a randomized, placebo-controlled, double-blind, dose-escalating, single-d...

Zdravkovic M, Christiansen T, Grosch K, Ilondo MM

Zdravkovic M, Søgaard B, Ynddal L, Christiansen T, Agersø H, Thomsen MS et al.

The aim of the present study was to investigate the pharmacodynamics, pharmacokinetics, safety and tolerability of a single dose of NN703 (tabimorelin), a growth hormone secretagogue in healthy male subjects. The study design was double blind, randomized and placebo-controlled, with eight escalat...

Peschke B, Ankersen M, Hansen TK, Hansen BS, Lau J, Nielsen KK et al.

Based on NN703, low molecular weight growth hormone secretagouges (GHSs) with a reduced number of hydrogen binding sites were designed by removal of the C-terminal amide group. The compounds were highly potent in combination with high efficacy in a rat pituitary cell assay, being characterized wi...

Ankersen M, Kramer Nielsen K, Kruse Hansen T, Raun K, Sehested Hansen B

A series of GH secretagogues based on modifications in the C-terminal of NN703 is reported. The C-terminal N-methyl amide of NN703 has been replaced with alkylated hydrazides in order to decrease the volume of distribution and identify GH secretagogues with shorter duration of action. Most of the...

Hansen BS, Raun K, Nielsen KK, Johansen PB, Hansen TK, Peschke B et al.

NN703 is a novel orally active GH secretagogue (GHS) derived from ipamorelin. NN703 stimulates GH release from rat pituitary cells in a dose-dependent manner with a potency and efficacy similar to that of GHRP-6. The effect is inhibited by known GHS antagonists, but not by a GH-releasing hormone ...

Peschke B, Hansen BS

The C-terminal the orally active growth hormone secretagogue NN703 was changed to prepare analogues with inverse sulfonamides and inverse amides. The compounds showed high activity in a in vitro rat pituitary model.

Johansen PB, Hansen KT, Andersen JV, Johansen NL

1. The pharmacokinetics of three new peptidyl growth hormone secretagogues, ipamorelin (NNC 26-0161), NNC 26-0194 and NNC 26-0235, were compared with two well-known hexapeptides, GHRP-2 and GHRP-6, in the male rat following different routes of administration. 2. Following i.v. bolus injection, pl...