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Ghrelin receptor agonist (orally active peptidomimetic)

Tabimorelin

Tabimorelin (NN703) is a potent, orally active agonist of the ghrelin/growth hormone secretagogue receptor and one of the earliest GH secretagogues developed.

By The Peptides Codex Editorial TeamIndividual review date not recorded

Page data last changed: . Chemistry registry snapshot: . Registry refreshes and identity assessments are separate from scientific content review.

Length
n/a
Class
Ghrelin receptor agonist (orally active peptidomimetic)
Function
Growth hormone secretagogue receptor agonist
Context
Experimental oral GH secretagogue; never approved and not authorized by Health Canada

One of the earliest orally active GH secretagogues explored in development.

Also known as: NN703 · ghrelin receptor agonist

Part of the Growth hormone & IGF peptides cluster

Overview

Tabimorelin (NN703) is a potent, orally active agonist of the ghrelin/growth hormone secretagogue receptor and one of the earliest GH secretagogues developed. It remained an experimental compound, was never approved, and is not authorized by Health Canada. This page is educational and is not medical advice.

Source & context

Biological / chemical source: Synthetic orally active peptidomimetic

Primary research or clinical context: Experimental oral GH secretagogue; never approved and not authorized by Health Canada

Early secretagogue development

Tabimorelin helped establish that small orally active molecules could stimulate the growth hormone secretagogue receptor. It raised GH and IGF-1 levels, but clinical benefit in adults proved limited and development did not advance to approval.

Drug-interaction lesson

Tabimorelin was found to inhibit the CYP3A4 enzyme, highlighting a practical concern in secretagogue development: an oral compound must be evaluated for drug-metabolism interactions, not just receptor activity.

Structure & chemistry

Molecular identity & reference confidence

Source-supported reference

Reference values are taken from the cited molecular record or curated profile. A database match is not independent laboratory verification; modifications, counter-ions, and formulations can change the measured mass.

Molecular form
Tabimorelin (source record; form not independently established)
Species
Not established by this molecular identity audit
Termini (N / C)
Not specified / Not specified

Average reference mass

Reference policy updated: 2026-10-05

Molecular formula
C32H40N4O3
Average reference mass
≈ 528.7
Identifiers

Chemistry values: PubChem · fetched 2026-10-01.

Concentration math

Tabimorelin — reconstitution calculator

Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.

Reference form: Tabimorelin (source record; form not independently established)Average reference mass: 528.7 Da

Syringe graduation
Solution concentration
5 mg/mL5,000 mcg/mL
mcg

Enter an amount to see the volume it corresponds to.

Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.

Open the Tabimorelin calculator on its own page →

FAQ about Tabimorelin

What is Tabimorelin?+

Tabimorelin (NN703) is a potent, orally active agonist of the ghrelin/growth hormone secretagogue receptor and one of the earliest GH secretagogues developed. It remained an experimental compound, was never approved, and is not authorized by Health Canada. This page is educational and is not medical advice.

What Canadian product status is recorded for Tabimorelin?+

Canadian product status for Tabimorelin has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.

What is the typical length of Tabimorelin?+

Tabimorelin is not a classic amino-acid chain peptide in the same sense; see the profile for classification details.

Related peptides

PE-22-28
Research peptide
PE-22-28 is a synthetic heptapeptide derived from spadin, developed as a shortened analog that inhibits the TREK-1 potassium channel. It has been examined in rodent neuroscience studies and is not authorized as a medicine by Health Canada.
Cortexin
Polypeptide complex
Cortexin is a low-molecular-weight polypeptide complex extracted from cerebral cortex tissue, studied largely in Russian neuroscience literature. It is marketed as a drug in some countries but is not authorized by Health Canada.
Pinealon
Research peptide
Pinealon is the synthetic tripeptide Glu-Asp-Arg (EDR), one of the Khavinson short-peptide bioregulators. Its evidence is rodent, cell-culture and small uncontrolled Russian human observations reporting antioxidant and neuroprotective effects; no registered clinical trial exists and it is not an approved medicine in the US, Canada or the EU.
Teverelix
GnRH antagonist (decapeptide analog)
Teverelix is a synthetic decapeptide GnRH antagonist that binds competitively and reversibly to pituitary GnRH receptors, suppressing luteinizing hormone and follicle-stimulating hormone. It is an investigational compound studied in prostate disorders and is not authorized by Health Canada. This page is educational and is not medical advice.

References & further reading

  1. 1.Lange et al. (2021). Comprehensive insights into the formation of metabolites of the ghrelin mimetics capromorelin, macimorelin and tabimorelin as potential markers for doping control purposes. Biomed Chromatogr
  2. 2.Zdravkovic et al. (2003). A clinical study investigating the pharmacokinetic interaction between NN703 (tabimorelin), a potential inhibitor of CYP3A4 activity, and midazolam, a CYP3A4 substrate. Eur J Clin Pharmacol
  3. 3.Holm et al. (2004). Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin-signalling-deficient ZDF rats. Eur J Endocrinol
  4. 4.Hansen et al. (1999). Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur J Endocrinol
  5. 5.Svensson et al. (2003). Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency. Clin Endocrinol (Oxf)
  6. 6.Hansen et al. (2001). Highly potent growth hormone secretagogues: hybrids of NN703 and ipamorelin. Bioorg Med Chem Lett
  7. 7.Zdravkovic et al. (2000). The pharmacokinetics, pharmacodynamics, safety and tolerability of a single dose of NN703, a novel orally active growth hormone secretagogue in healthy male volunteers. Growth Horm IGF Res
  8. 8.Agersø et al. (2001). Pharmacokinetic and pharmacodynamic modeling of NN703, a growth hormone secretagogue, after a single po dose to human volunteers. J Clin Pharmacol
  9. 9.PubChem — compound summary for Tabimorelin (CID 9810101)
  10. 10.Wikipedia — Tabimorelin
Disclaimer: Educational content only. Not medical advice. Not instructions for human use. Research peptides and unapproved products may be restricted or illegal to market for human consumption in your jurisdiction. Consult qualified professionals and applicable law.
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