Macimorelin

Orally active ghrelin (GHSR1a) agonist and growth-hormone secretagogue, FDA-approved as a diagnostic test for adult growth hormone deficiency.

Overview

Macimorelin is a small peptidomimetic mimic of ghrelin that binds the growth-hormone secretagogue receptor type 1a (GHSR1a). Given as a single weight-based oral dose, it produces a robust, transient rise in serum growth hormone (GH) that can distinguish patients with adult GH deficiency (AGHD) from healthy individuals.

Historically, the insulin tolerance test (ITT) was the gold standard for diagnosing AGHD, but it is cumbersome, requires induced hypoglycaemia, and is contraindicated in patients with cardiac disease or seizure disorders. The pivotal phase 3 validation study demonstrated that the oral macimorelin test achieved sensitivity and specificity comparable to the ITT while being far better tolerated (Garcia 2018).

Macimorelin is administered after an overnight fast; GH is sampled at defined intervals (typically 30, 45, 60 and 90 minutes), and a peak GH below the validated cut-off is consistent with GH deficiency. It has also been investigated for diagnosis of childhood-onset GH deficiency and, at repeated doses, explored in cancer cachexia.

Mechanism of Action

As a ghrelin mimetic, macimorelin engages the same G-protein-coupled receptor as endogenous ghrelin, driving Gq/phospholipase-C signalling and calcium-dependent GH release. Because oral bioavailability is sufficient to reach the pituitary, a single oral dose evokes a GH peak in individuals with intact somatotroph function; a blunted peak indicates GH deficiency.

Reconstitution Calculator

Reconstitution Calculator

Calculate your peptide dosing

Draw Volume
0.100mL
Syringe Units
10units
Concentration
2,500mcg/mL
Doses / Vial
20doses
Vial Total
5mg
Waste / Vial
0mcg
Syringe Cap.
100units · 1mL
How to reconstitute
Gather & prepare
1/6Gather & prepare

Set up a clean workspace with all supplies ready.

1.Wash hands thoroughly, put on disposable gloves
2.Your 5mg peptide vial (lyophilized powder)
3.Bacteriostatic water (you'll need 2mL)
4.A 3–5mL syringe with 21–25 gauge needle for reconstitution
5.Alcohol swabs (70% isopropyl)
Use bacteriostatic water (0.9% benzyl alcohol) for multi-dose vials. Sterile water is only safe for single-use.
Supply Planner

7x / week for weeks

·
40%
2vials
28 doses20 days/vial12 leftover
Cost Breakdown
Vial price
$0.00per dose
$0.00 /week$0 /month
Store 2-8°C30 day shelf lifeSwirl gentlyFor research purposes only

This calculator is provided for informational and educational purposes only. It is not intended as medical advice, diagnosis, or treatment guidance. Always consult a qualified healthcare professional before preparing or administering any substance. PepGuide assumes no liability for decisions made based on these calculations.

References (2)

  1. [1]
    Garcia JM, Biller BMK, Korbonits M, et al. Macimorelin as a Diagnostic Test for Adult GH Deficiency Journal of Clinical Endocrinology & Metabolism (2018)

    In a phase 3 crossover trial the single oral 0.5 mg/kg macimorelin test showed 92% sensitivity and 96% specificity versus the insulin tolerance test for adult GH deficiency.

  2. [2]
    Piccoli F, Degen L, et al. The macimorelin-stimulated growth hormone test for adult growth hormone deficiency diagnosis Expert Review of Endocrinology & Metabolism (2014)

    Reviews macimorelin as an orally available ghrelin mimetic that acutely raises GH via the GHSR1a receptor with good diagnostic accuracy and a favourable safety profile.

Updated 2026-07-07Reviewed by ai-enrich-2026-07-contentSources: https://pubmed.ncbi.nlm.nih.gov/29860330/, https://pubmed.ncbi.nlm.nih.gov/24834478/

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