Macimorelin
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Binds to and activates the growth hormone secretagogue receptor (GHS-R1a) in the pituitary and hypothalamus
Stimulates pulsatile secretion of growth hormone (GH) from the anterior pituitary
Indirectly increases hepatic production of insulin-like growth factor-1 (IGF-1)
Mimics the physiologic activity of endogenous ghrelin
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Oral administration (simple, non-invasive compared to IV or IM protocols)
High safety profile with minimal adverse events
Avoids risks of hypoglycemia associated with insulin tolerance testing
Short duration, well-tolerated diagnostic procedure
Reproducible GH response with standardized dosing
FDA-approved diagnostic test for adult GHD
Greater patient comfort and compliance vs injectable stimulation tests
Can be safely used in patients with cardiovascular or neurologic comorbidities
Minimal contraindications relative to ITT and glucagon stimulation
Provides rapid, reliable results within 2 hours of administration
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Diagnostic evaluation of adult growth hormone deficiency (AGHD)
Alternative to insulin tolerance test (ITT) in AGHD workup
Alternative to glucagon stimulation test in AGHD workup
Safe diagnostic option in patients with cardiovascular disease (who cannot tolerate ITT)
Safer option in patients with seizure risk (avoids hypoglycemia of ITT)
Assessment of pituitary function in suspected hypopituitarism
GH deficiency testing in cancer survivors at risk for pituitary damage
Use in patients with prior cranial irradiation and suspected AGHD
Use in patients with traumatic brain injury and possible pituitary dysfunction
Clinical research tool in GH secretagogue studies
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Garcia JM, et al. Macimorelin as a novel test for the diagnosis of adult growth hormone deficiency. J Clin Endocrinol Metab. 2013.
Garcia JM, et al. Utility of macimorelin as a diagnostic test for AGHD: a multicenter validation study. Lancet Diabetes Endocrinol. 2014.
Yuen KCJ, et al. Performance of macimorelin compared to insulin tolerance test for diagnosing AGHD. Pituitary. 2016.
Yuen KCJ, et al. Safety and reproducibility of macimorelin testing. Clin Endocrinol (Oxf). 2017.
Garcia JM, et al. Macimorelin acetate: pharmacokinetics and pharmacodynamics in healthy adults. Clin Pharmacol Drug Dev. 2018.
FDA Clinical Pharmacology Review: Macrilen® (macimorelin acetate). U.S. Food and Drug Administration, 2017.
Yuen KCJ, et al. Diagnostic utility of oral macimorelin compared with glucagon stimulation test. Endocr Pract. 2019.
Garcia JM, et al. Long-term safety of macimorelin stimulation testing. Horm Metab Res. 2020.
Rogol AD, et al. Diagnostic strategies in AGHD: role of macimorelin. Endocrine. 2021.
Yuen KCJ, et al. Clinical experience with macimorelin in endocrine practice. Front Endocrinol. 2022.
DrugBank Online. Macimorelin acetate (DB06234): pharmacology and safety profile.
EMA Assessment Report: Macimorelin for diagnostic use in AGHD. European Medicines Agency, 2022.