P Palthera
Hormone Analogues

Ipamorelin

NNC-26-0161

Ipamorelin is a synthetic pentapeptide ghrelin (GHS-R1a) developed at Novo Nordisk in the late 1990s as a selective growth hormone secretagogue. Published work includes early-phase human pharmacokinetic studies and a body of rodent literature. Ipamorelin is not approved as a medicine and is not for human use outside of regulated research settings.

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Hormone Analogues
Classification
Selective ghrelin / GHS-R1a receptor agonist (GHRP)
Research stage
Early-phase clinical pharmacokinetic research and preclinical animal literature
Sequence
Aib-His-D-2-Nal-D-Phe-Lys-NH2
Molecular weight
711.86 Da

Snapshot

Key takeaways

A three-bullet snapshot before reading the full dossier.

  1. 01

    Synthetic pentapeptide ghrelin- with reported selectivity for GH release over /cortisol/prolactin.

  2. 02

    Primary peer-reviewed evidence comprises a small Phase I human PK study and rodent work.

  3. 03

    Not approved as a medicine by the FDA, MHRA, or EMA at the time of writing.

Dossier overview

4

research areas

3

references

3

handling notes

01

Mechanism of action

Ipamorelin binds the growth hormone secretagogue (GHS-R1a), the ghrelin receptor, to induce pulsatile growth hormone release. Early pharmacology characterised it as more selective than first-generation GHRPs.

02

Research applications

  • Ghrelin / GHS-R1a pharmacology
  • Rodent bone-growth and growth-hormone axis research
  • Pharmacokinetic / pharmacodynamic modelling
  • Comparative growth hormone secretagogue research

Evidence at a glance

What's behind this profile

3 citations · 1998–1999

Human
1

Studies in human volunteers or patients (incl. early-phase trials).

Animal
2

Studies in rodents or other animal models.

Publication years

  1. 98
  2. 99
19981999

Counts are derived from the cited studies below. A study covering both in vivo and in vitro work is counted by its primary model. Sample size is reported in 1 of 3 citations. Findings remain model-specific and are not extrapolated to therapeutic use.

03

Study references

Each profile cites a minimum of two peer-reviewed sources, with model type and reported sample size where the source provides it. Findings are model-specific and must not be extrapolated to therapeutic use.

Ipamorelin, the first selective growth hormone secretagogue

1998

Raun K et al. · European Journal of Endocrinology

Model
Preclinical pharmacology (in vitro receptor binding + in vivo rat and swine GH-release studies)
Sample
Not reported in abstract

Reported selective GH release versus , cortisol, and prolactin in animal models — establishing the selective-secretagogue profile that defined the compound.

PMID 9849822 DOI 10.1530/eje.0.1390552

Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats

1999

Johansen PB et al. · Growth Hormone & IGF Research

Model
In vivo — rats (15-day dose-ranging study)
Sample
Not reported in abstract

Dose-dependent increases in longitudinal bone growth and body weight in rats over 15 days of administration.

PMID 10373343 DOI 10.1054/ghir.1999.9998

Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers

1999

Gobburu JV et al. · Pharmaceutical Research

Model
Phase I dose-escalation pharmacokinetic study in healthy male volunteers
Sample
n=40

Reported dose-proportional with a ~2-hour and episodic GH release after intravenous administration in healthy adult men.

PMID 10496658 DOI 10.1023/a:1018955126402

Evidence caveats

  • Ipamorelin is not approved as a medicine; the published human evidence is limited to early-phase pharmacokinetic studies (small cohorts, short duration).
  • Subsequent development was discontinued at Phase II; long-term safety and efficacy in humans have not been established in peer-reviewed literature.

04

Storage and handling

Store under controlled laboratory conditions with batch and preparation details recorded.

  • Maintain batch and supplier documentation for comparison studies.
  • Record conditions and avoid repeated cycles where not protocol-supported.
  • Research-only inventory must be clearly separated from any clinical material.

Common questions

Ipamorelin FAQ

Plain-English answers backed by the citations on this profile — what it is, what's been studied, regulatory status, evidence limits.

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