Ipamorelin: Safety Profile & Research Summary
21 PubMed CitationsExpert ReviewedGMP CertifiedLast Reviewed: February 2026
Preclinical Research Summary
Key Preclinical Studies
| Study | Model | Key Findings | Ref |
|---|---|---|---|
| Raun et al. (1998) | Rats/Swine — IV bolus | ED₅₀ = 80 nmol/kg (rats), 2.3 nmol/kg (swine); NO ACTH/cortisol even at >200× ED₅₀; first selective GHS | [1] |
| Johansen et al. (1999) | Adult female rats — 18–450 µg/day SC × 15d | Longitudinal bone growth 42→52 µm/day (p<0.0001); dose-dependent | [3] |
| Andersen et al. (2001) | Rats — GC-induced catabolism — 100 µg/kg SC TID × 3mo | Periosteal bone formation rate increased 4-fold; increased maximum tetanic muscle tension | [12] |
| Venkova et al. (2009) | Rats with POI — 0.014–1.0 mg/kg IV | Gastric retention reduced to <25% (vs 78% vehicle, p<0.05); accelerated colonic transit | [4] |
| Svensson et al. (2000) | Female rats — 0.5 mg/kg/day SC × 12 wk | Increased tibial and vertebral BMC; bone dimensions increased (not density) | [8] |
| Jiménez-Reina et al. (2002) | Female Wistar rats — 100 µg/kg SC × 21d | 67% increase in basal GH release; NO somatotroph desensitization; significant weight gain | [7] |
| Lall et al. (2001) | GH-deficient (lit/lit) mice — 250 µg/kg SC BID × 2–9 wk | Body weight +15–17%; increased adiposity via GH-independent mechanism | [9] |
| Adeghate & Ponery (2004) | Normal/diabetic rat tissue — 10⁻¹² to 10⁻⁶ M in vitro | Significant insulin release (p<0.04); via calcium channels and adrenergic pathways | [10] |
| Mohammadi et al. (2020) | Rat visceral hypersensitivity — 0.01–1.0 mg/kg IV | Dose-dependent reduction in visceromotor response; blocked by ghrelin receptor antagonist | [17] |
| Lu et al. (2024) | Ferrets — cisplatin-induced wasting | Inhibited cisplatin-induced weight loss; confirmed non-rodent cachexia model | [14] |
Clinical Trials
| Trial | Population | Intervention | Key Results | Ref |
|---|---|---|---|---|
| Phase I PK/PD | n=48 healthy males | 5 dose levels (4.21–140.45 nmol/kg IV × 15 min) | Linear kinetics; T½ ~2h; SC₅₀ = 214 nmol/L; episodic GH burst peaking at 0.67h; no adverse events | [2] |
| Phase II POI (NCT00672074) | n=114 bowel resection patients | 0.03 mg/kg IV BID × 7 days | Median meal tolerance: 25.3h vs 32.6h placebo — NOT significant (p=0.15); hypokalemia 12.5%, hyperglycemia 14.3%; 2 fatal SAEs in treatment group; TRIAL FAILED | [6] |
Safety Summary
| Parameter | Finding |
|---|---|
| Selectivity | No ACTH, cortisol, FSH, LH, PRL, or TSH stimulation — even at 200× ED₅₀ |
| Phase I (n=48) | No adverse events in healthy volunteers |
| Phase II (n=114) | Hypokalemia 12.5% vs 3.4% placebo; insomnia 10.7% vs 5.2%; hyperglycemia 14.3% vs 8.6%; 2 fatal SAEs |
| Reproductive | Class-wide concern: ghrelin receptor agonists may negatively impact fertilization/embryofetal development (mouse models) |
| Drug Interactions | Reverses morphine-induced GI slowing; blocked by GHS receptor antagonists; not affected by GHRH antagonists |
| Pharmacokinetics | Intranasal ~20% bioavailability; oral <1%; 60–80% excreted unchanged in urine |
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References
- Raun K, Hansen BS, Johansen NL, et al. Ipamorelin, the first selective growth hormone secretagogue. European Journal of Endocrinology. 1998;139(5):552-561.
- Gobburu JVS, Agersø H, Jusko WJ, Ynddal L. Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. Pharmaceutical Research. 1999;16(9):1412-1416.
- Johansen PB, Nowak J, Skjaerbaek C, et al. Ipamorelin, a new growth-hormone-releasing peptide, induces 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, a novel 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, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the 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 stimulates body weight gain and growth hormone 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 stimulation of adiposity by GH secretagogues. BBRC. 2001;280(1):132-138.
- Adeghate E, Ponery AS. Mechanism of ipamorelin-evoked insulin release from the pancreas of normal and diabetic rats. Neuro Endocrinology Letters. 2004;25(6):403-406.
- Johansen PB, Hansen KT, Andersen JV, Johansen NL. Pharmacokinetic evaluation of ipamorelin with emphasis on nasal absorption. Xenobiotica. 1998;28(11):1083-1092.
- Andersen NB, Malmlöf K, Johansen PB, Oxlund H. The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced 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-induced weight loss in ferrets. Physiology & Behavior. 2024.
- Sinha DK, Balasubramanian A, Tatem AJ, et al. Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition 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 attenuates visceral and somatic nociception through peripheral ghrelin receptor mechanisms. 2020.
- U.S. Food & Drug Administration. FDA Evaluation of Ipamorelin-Related Bulk Drug Substances. FDA Pharmacy Compounding Advisory Committee. 2024.
- World Anti-Doping Agency. WADA Prohibited List — S2: Peptide Hormones, Growth Factors, Related Substances, and Mimetics. 2024.
- Polvino WJ. Methods of treatment using a ghrelin receptor agonist. 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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