Research Brief
What Is Ipamorelin?
Resposta Rapida
Visao Geral da Pesquisa Ipamorelin (NNC 26-0161) is a synthetic pentapeptide hormonio do crescimento secretagogue with a sequencia Aib-His-D-2-Nal-D-Phe-Lys-NH₂, developed by Novo Nordisk no(a) mid-1990s by systematic modification of GHRP-1. It acts como um(a) highly selective agonist do(a) GHS-R1a ...
Visao Geral da Pesquisa
Ipamorelin (NNC 26-0161) is a synthetic pentapeptide hormonio do crescimento secretagogue with a sequencia Aib-His-D-2-Nal-D-Phe-Lys-NH₂, developed by Novo Nordisk no(a) mid-1990s by systematic modification of GHRP-1. It acts como um(a) highly selective agonist do(a) GHS-R1a receptor (ghrelin receptor), stimulating potent, pulsatile hormonio do crescimento release sem affecting ACTH, cortisol, FSH, LH, TSH, or prolactin — even at 200× o efeitoive dose.[1][2]
Ipamorelin research spans 8+ indication categories incluindo selective GH secretion, postoperative ileus, bone growth, composicao corporal, secrecao de insulina, pain modulacao, and cancer caquexia. A Phase II ensaio clinico for POI (n=114, NCT00672074) failed to reach significancia estatistica, and desenvolvimento clinico was discontinued.[6][4]
Key distinguishing features include: (1) first selective GHS with GHRH-like specificity, (2) no somatotroph dessensibilizacao upon cronico(a) administration, (3) linear pharmacokinetics in humans (T½ ~2h), and (4) GH-independent adipogenic effects.[1][9]
Referencias
- Raun K, Hansen BS, Johansen NL, et al. Ipamorelin, the primeiro(a) selective hormonio do crescimento secretagogue. European Journal of Endocrinology. 1998;139(5):552-561.
- Gobburu JVS, Agersø H, Jusko WJ, Ynddal L. Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a hormonio do crescimento releasing peptide, in human volunteers. Pharmaceutical Research. 1999;16(9):1412-1416.
- Johansen PB, Nowak J, Skjaerbaek C, et al. Ipamorelin, a novo(a) growth-hormone-releasing peptide, induz longitudinal bone growth in rats. Growth Hormone & IGF Research. 1999;9(2):106-113.
- Venkova K, Mann W, Nelson R, Greenwood-Van Meerveld B. Efficacy of ipamorelin, um(a) novo(a) ghrelin mimetic, in a rodent model of postoperative ileus. JPET. 2009;329(3):1110-1116.
- Greenwood-Van Meerveld B, Tyler K, Mohammadi E, Pietra C. Efficacy of ipamorelin on gastric dysmotility in a rodent model of postoperative ileus. Journal of Experimental Pharmacology. 2012;4:149-155.
- Beck DE, Sweeney WB, McCarter MD. Prospective, randomizado, controlled, proof-of-concept study do(a) Ghrelin mimetic ipamorelin para o(a) management of postoperative ileus in bowel resection patients. Int J Colorectal Dis. 2014;29(12):1527-1534.
- Jiménez-Reina L, Cañete R, de la Torre MJ, Bernal G. Chronic in vivo Ipamorelin treatment estimula peso corporal gain and hormonio do crescimento release in vitro in young female rats. European Journal of Anatomy. 2002;6(1):37-45.
- Svensson J, Lall S, Dickson SL, Jansson JO. The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats. Journal of Endocrinology. 2000;165:569-577.
- Lall S, Tung LY, Ohlsson C, Jansson JO, Dickson SL. Growth hormone (GH)-independent estimulacao of adiposity by GH secretagogues. BBRC. 2001;280(1):132-138.
- Adeghate E, Ponery AS. Mechanism of ipamorelin-evoked insulin release do(a) pancreas of normal and ratos diabeticos. Neuro Endocrinology Letters. 2004;25(6):403-406.
- Johansen PB, Hansen KT, Andersen JV, Johansen NL. Pharmacokinetic evaluation of ipamorelin with emphasis on nasal absorcao. Xenobiotica. 1998;28(11):1083-1092.
- Andersen NB, Malmlöf K, Johansen PB, Oxlund H. The hormonio do crescimento secretagogue ipamorelin counteracts glucocorticoid-induziu decrease in bone formation of adult rats. Growth Hormone & IGF Research. 2001;11(5):266-272.
- Hansen TK, Ankersen M, Raun K, Hansen BS. Highly Potent Growth Hormone Secretagogues: Hybrids of NN703 and Ipamorelin. Bioorganic & Medicinal Chemistry Letters. 2001;11(14):1915-1918.
- Lu Z, Ngan MP, Liu JYH, Rudd JA. The GHS-R1a agonists anamorelin and ipamorelin inhibit cisplatin-induziu perda de peso in ferrets. Physiology & Behavior. 2024.
- Sinha DK, Balasubramanian A, Tatem AJ, et al. Beyond the androgen receptor: the role of hormonio do crescimento secretagogues no(a) modern management of composicao corporal in hypogonadal males. Translational Andrology and Urology. 2020;9(Suppl 2):S149-S159.
- Thøgersen H, Johansen NL, Lau J, et al. A New Series of Highly Potent Growth Hormone-Releasing Peptides Derived from Ipamorelin. Journal of Medicinal Chemistry. 1998;41.
- Mohammadi E, Bhatt V, Bhatt AB, Pietra C, Greenwood-Van Meerveld B. Ipamorelin atenua visceral and somatic nociception through periferico(a) ghrelin receptor mechanisms. 2020.
- U.S. Food & Drug Administration. FDA Evaluation of Ipamorelin-Related Substancia Farmaceutica a Granels. FDA Pharmacy Compounding Advisory Committee. 2024.
- World Anti-Doping Agency. WADA Lista de Substancias Proibidas — S2: Hormonios Peptidicos, Fatores de Crescimento, Substancias Relacionadas e Mimeticos. 2024.
- Polvino WJ. Methods of treatment using a ghrelin agonista do receptor. US Patent 8,039,456 B2.
- Thøger Nielsen K, et al. Validated screening method for GH-releasing peptides using UHPLC-HRMS on dried blood spots. Drug Testing and Analysis. 2021.
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