K4 Elite
K4 Elite
Ipamorelin is a synthetic pentapeptide growth hormone secretagogue (ghrelin-receptor agonist) originally developed by Novo Nordisk and characterised in rat, swine and in-vitro models (Raun et al., 1998). Human evidence is thin: a single-dose intravenous pharmacokinetic/pharmacodynamic study in 40 healthy male volunteers (Gobburu et al., 1999) and one Phase 2 proof-of-concept RCT of intravenous ipamorelin for postoperative ileus after bowel resection (n=117; Beck et al., 2014), which found no significant efficacy difference from placebo. Development was not pursued and ipamorelin is not approved anywhere; there are no published human data on subcutaneous, repeated or long-term use, nor on body composition or 'anti-ageing' end points.
Each row records what a published study did: who it enrolled, the regimen it administered to those subjects, and what it reported. These are historical study descriptions, not protocols to follow.
| Study | Population | Regimen as reported | Primary findings |
|---|---|---|---|
| Gobburu et al., Pharm Res 1999 (Phase 1 PK/PD, healthy volunteers) | Healthy male volunteers (eight subjects at each of five dose levels) | Subjects received ipamorelin as a 15-minute intravenous infusion at one of five rates (4.21, 14.02, 42.13, 84.27 or 140.45 nmol/kg) in a dose-escalation design. | Pharmacokinetics were dose-proportional with a terminal half-life of about 2 hours, clearance 0.078 L/h/kg and steady-state volume of distribution 0.22 L/kg; each dose produced a single episode of GH release peaking at 0.67 hours, with an SC50 of 214 nmol/L. |
| Beck et al., Int J Colorectal Dis 2014 (Phase 2 proof-of-concept RCT, postoperative ileus) Registry: NCT00672074
|
Adults undergoing small- or large-bowel resection by open or laparoscopic surgery (117 enrolled; 114 in safety and modified intent-to-treat populations; multicentre) | Patients received intravenous infusions of ipamorelin 0.03 mg/kg or placebo twice daily from postoperative day 1 to day 7 or hospital discharge. | Median time to first tolerated solid meal was 25.3 h with ipamorelin versus 32.6 h with placebo (p=0.15); there were no significant differences in key or secondary efficacy analyses. |
| Raun et al., Eur J Endocrinol 1998 (animal / in-vitro pharmacology) | Primary rat pituitary cells; pentobarbital-anaesthetised rats; conscious swine | In anaesthetised rats ipamorelin was given intravenously (ED50 80 nmol/kg for GH release); in conscious swine it was given intravenously (ED50 2.3 nmol/kg), with doses up to more than 200-fold the GH ED50 examined for ACTH and cortisol effects. | Ipamorelin released GH with potency and efficacy comparable to GHRP-6, did not affect FSH, LH, prolactin or TSH in swine, and unlike GHRP-6 and GHRP-2 did not raise ACTH or cortisol beyond levels seen with GHRH. |
| Johansen et al., Growth Horm IGF Res 1999 (rat bone-growth model) | Adult female rats | Ipamorelin 0, 18, 90 or 450 µg/day was injected subcutaneously three times daily for 15 days. | Longitudinal bone growth rate rose dose-dependently from 42 to 44, 50 and 52 µm/day with a dose-dependent increase in body-weight gain; total IGF-I, IGFBPs and bone-turnover markers were unchanged, and the pituitary GH response to a provocative ipamorelin dose was marginally reduced. |
| Venkova et al., J Pharmacol Exp Ther 2009 (rat postoperative ileus model) | Fasted male rats subjected to laparotomy and intestinal manipulation | Ipamorelin 0.01-1 mg/kg, GHRP-6 20 µg/kg or saline was given by intravenous bolus as a single dose or four times daily for 2 days. | A single 1 mg/kg dose shortened time to first bowel movement; repeated dosing at 0.1 or 1 mg/kg increased cumulative faecal output, food intake and body-weight gain over 48 h. |
Effects recorded in the cited reports. Frequencies are those the source reported, in the population that source studied.
| Effect | Frequency / context | Source |
|---|---|---|
| Treatment-emergent adverse events (any) | 87.5% in the ipamorelin group vs 94.8% with placebo among postoperative bowel-resection patients receiving 0.03 mg/kg IV twice daily for up to 7 days; the authors described the regimen as well tolerated (Beck et al., 2014). Individual event frequencies are not given in the abstract. | Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients ↗ |
| GH release (pharmacodynamic effect) | Single episode of GH release at all five intravenous dose levels in healthy male volunteers, peaking at 0.67 h and declining to negligible levels (Gobburu et al., 1999). | Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers ↗ |
| ACTH / cortisol release (animal data) | Not observed in swine at doses >200-fold the GH ED50, in contrast to GHRP-2 and GHRP-6; no effect on FSH, LH, prolactin or TSH (Raun et al., 1998; swine model). | Ipamorelin, the first selective growth hormone secretagogue ↗ |
| Increased body-weight gain and food intake (animal data) | Dose-dependent body-weight gain in adult female rats given 18-450 µg/day subcutaneously for 15 days (Johansen et al., 1999); increased food intake and weight gain with repeated IV dosing in a rat ileus model (Venkova et al., 2009). | Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats ↗ |
No interactions with a verifiable citation have been indexed for this compound.
Exclusions and label contraindications recorded in the cited sources.