Disease relevance of Ipamorelin

• In +/lit and lit/lit mice ipamorelin induced a small (15%) increase in body weight by 2 weeks, that was not further augmented by 9 weeks [1].

High impact information on Ipamorelin

• NNC 26-0235 demonstrated a 10% oral bioavailability in dogs, and NNC 26-0235 and ipamorelin were able to increase basal GH level by more than 10-fold after oral administration of a dose of 1.8 and 2.7 mg/kg, respectively [2].
• This stomach-specific expression of ghrelin in seabream is subject to regulation, as administration of growth hormone or ipamorelin to the fish in vivo was demonstrated to enhance its expression [3].
• Here we compared the effects of twice daily s.c. treatment of GH and the GHS, ipamorelin, on body fat in GH-deficient (lit/lit) and in GH-intact (+/lit and +/+) mice [1].
• The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats [4].
• CONCLUSIONS: The proposed PK/PD model provides a useful characterization of ipamorelin disposition and GH responses across a range of doses [5].

Biological context of Ipamorelin

• PURPOSE: To examine the pharmacokinetics (PK) and pharmacodynamics (PD) of ipamorelin, a growth hormone (GH) releasing peptide, in healthy volunteers [5].
• With the objective of investigating the effects on longitudinal bone growth rate (LGR), body weight (BW), and GH release, ipamorelin in different doses (0, 18, 90 and 450 microg/day) was injected s.c. three times daily for 15 days to adult female rats [6].
• The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats [7].

Anatomical context of Ipamorelin

• The ability of the growth hormone secretagogue (GHS) Ipamorelin to counteract the catabolic effects of glucocorticoid (GC) on skeletal muscles and bone was investigated in vivo in an adult rat model [7].
• Mechanism of ipamorelin-evoked insulin release from the pancreas of normal and diabetic rats [8].

Associations of Ipamorelin with other chemical compounds

• Very surprisingly, ipamorelin did not release ACTH or cortisol in levels significantly different from those observed following GHRH stimulation [9].

Gene context of Ipamorelin

• Basal intracellular GH content in somatotroph cells over 4 hours was lower in the Ipamorelin group and the GHRH group than in the saline group [10].
• Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro [10].
• Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers [5].
• The development and pharmacology of a new potent growth hormone (GH) secretagogue, ipamorelin, is described [9].
• NN703 is a novel orally active GH secretagogue (GHS) derived from ipamorelin [11].

Analytical, diagnostic and therapeutic context of Ipamorelin

• 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 [12].

References