Ipamorelin dosing & administration

Raun K, Hansen BS, Johansen NL, et al. · 1998

This Novo Nordisk study introduced ipamorelin as the first GH secretagogue selective for GH release. Potency was measured in primary rat pituitary cells and in rats; selectivity was tested in conscious swine, where — unlike GHRP-6 and GHRP-2 — ipamorelin did not raise ACTH or cortisol above the levels seen with GHRH, and that held at doses more than 200-fold above the ED50 for GH release. No human study has since measured ACTH, cortisol or prolactin after ipamorelin, so the selectivity finding remains animal data.

Gobburu JV, Agersø H, Jusko WJ, Ynddal L · 1999

This human clinical trial established Ipamorelin's pharmacokinetics—showing a 2-hour half-life, dose-proportional responses, and consistent GH release across all dose levels tested. The study provided the foundation for understanding proper human dosing.

Beck DE, Sweeney WB, McCarter MD, et al. · 2014

This Phase 2 proof-of-concept trial randomized 114 bowel-resection patients (56 ipamorelin, 58 placebo) to IV study drug twice daily for up to 7 days. It did not meet its primary endpoint: median time to first tolerated meal was 25.3 hours on ipamorelin vs 32.6 hours on placebo, a 7.3-hour difference that was not statistically significant, with no significant separation on secondary endpoints. Most adverse events were mild to moderate and attributed to surgery. Serious adverse events occurred in 17.9% of ipamorelin patients vs 15.5% on placebo; hypokalemia (12.5% vs 3.4%), insomnia (10.7% vs 5.2%) and hyperglycemia at discharge (14.3% vs 8.6%) were more common on ipamorelin, and two ipamorelin-treated patients died after anastomotic leak. FDA's 2024 review states it is unclear whether those deaths were related to ipamorelin. The authors advised interpreting the results with caution given the small sample size.

Andersen NB, Malmlöf K, Johansen PB, et al. · 2001

This study showed Ipamorelin can counteract the muscle and bone damage caused by glucocorticoid (steroid) medications. Rats on steroids plus Ipamorelin had significantly increased muscle strength and four times greater bone formation compared to steroids alone.

Venkova K, Mann W, Nelson R, Greenwood-Van Meerveld B · 2009

Repeated Ipamorelin dosing significantly improved gut motility, food intake, and body weight recovery after surgery in rats. This supports its potential use for post-surgical recovery beyond just GH benefits.

U.S. Food and Drug Administration · 2024

FDA's review of ipamorelin ahead of the 29 October 2024 advisory committee meeting. It reports the per-arm adverse event rates from the Phase 2 bowel-resection trial that the journal abstract does not: serious adverse events in 10 of 56 on ipamorelin (17.9%) versus 9 of 58 on placebo (15.5%); hypokalemia 12.5% versus 3.4%; insomnia 10.7% versus 5.2%; hyperglycemia at discharge 14.3% versus 8.6%. Two ipamorelin-treated patients died of postoperative complications after anastomotic leak following colon cancer resection, and none on placebo. FDA states "it is unclear whether the two deaths were related to ipamorelin," and cited them alongside the potassium and glucose imbalances in recommending against adding ipamorelin to the 503A compounding list.