Description

Simple

A medication used to treat adults with low levels of growth hormone.

Clinical

A medication used to treat adult growth hormone deficiency.

Overview

Macimorelin, a novel and orally active ghrelin mimetic that stimulates GH secretion, is used in the diagnosis of adult GH deficiency (AGHD). More specifically, macimorelin is a peptidomimetic growth hormone secretagogue (GHS) that acts as an agonist of GH secretagogue receptor, or ghrelin receptor (GHS-R1a) to dose-dependently increase GH levels [3]. Growth hormone secretagogues (GHS) represent a new class of pharmacological agents which have the potential to be used in numerous clinical applications. They include treatment for growth retardation in children and cachexia associated with chronic disease such as AIDS and cancer.

Growth hormone (GH) is classically linked with linear growth during childhood. In deficiency of this hormone, AGHD is commonly associated with increased fat mass (particularly in the abdominal region), decreased lean body mass, osteopenia, dyslipidemia, insulin resistance, and/or glucose intolerance overtime. In addition, individuals with may be susceptible to cardiovascular complications from altered structures and function [Read more

Pharmacology

Indication

Indicated for the diagnosis of adult growth hormone deficiency (AGHD) [FDA Label].

Pharmacodynamic

Maximum GH levels from stimulation are observed between 30 to 90 minutes after administration of macimorelin [FDA Label]. Increase in the QTcF interval may be observed from macimorelin administration [FDA Label].

Mechanism of action

Ghrelin is an endogenous ligand for the GH secretagogue receptor that is also called the ghrelin receptor (GHS-R1a). Upon activation of the receptor, ghrelin serves to increase growth hormone (GH) secretion. Macimorelin mimics the actions of ghrelin by stimulating GH release. As a synthetic agonist,... Read more

Absorption

Macimorelin is a novel, synthetic ghrelin agonist, which is readily absorbed from the gastrointestinal tract [ Read more

Protein binding

Information currently not available.

Volume of distribution

Following a single oral dose of 0.5 mg/kg macimorelin, the mean volume of distribution of the central compartment is 5,733.4 ± 565.7L [ Read more

Clearance

Following a single oral dose of 0.5 mg/kg macimorelin, the mean clearance over the fraction absorbed (Cl/F) was 37,411.0 ± 4,554.6 mL/min [ Read more

Half life

The mean terminal half-life (T1/2) is 4.1 hours following administration of a single oral dose of 0.5 mg macimorelin/kg body weight in healthy subjects [FDA Label].

Route of elimination

Information currently not available.

Toxicity

Macimorelin has not shown to demonstrate mutagenic properties according to bacterial assays. It also did not induce any mutations or clastogenic effects in mouse lymphoma cells with or without metabolic activation. Studies assessing the carcinogenic potential or effect on fertility of macimorelin ha... Read more

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Abexinostat
The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Macimorelin.
Acebutolol
The risk or severity of QTc prolongation can be increased when Acebutolol is combined with Macimorelin.
Aceclofenac
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Aceclofenac.
Acemetacin
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Acemetacin.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Aceprometazine is combined with Macimorelin.
Acetyldigoxin
The risk or severity of QTc prolongation can be increased when Acetyldigoxin is combined with Macimorelin.
Acetylsalicylic acid
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Acetylsalicylic acid.
Aclidinium
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Aclidinium.
Acrivastine
The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Macimorelin.
Adenosine
The risk or severity of QTc prolongation can be increased when Adenosine is combined with Macimorelin.
Ajmaline
The risk or severity of QTc prolongation can be increased when Ajmaline is combined with Macimorelin.
Albusomatropin
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Albusomatropin.
Alclofenac
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Alclofenac.
Alfuzosin
The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Macimorelin.
Alimemazine
The risk or severity of QTc prolongation can be increased when Alimemazine is combined with Macimorelin.
Alminoprofen
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Alminoprofen.
Amantadine
The risk or severity of QTc prolongation can be increased when Amantadine is combined with Macimorelin.
Amifampridine
The risk or severity of QTc prolongation can be increased when Amifampridine is combined with Macimorelin.
Aminophenazone
The therapeutic efficacy of Macimorelin can be decreased when used in combination with Aminophenazone.
Amiodarone
The risk or severity of QTc prolongation can be increased when Amiodarone is combined with Macimorelin.
5 References
  1. 1 . Guerlavais V, Boeglin D, Mousseaux D, Oiry C, Heitz A, Deghenghi R, Locatelli V, Torsello A, Ghe C, Catapano F, Muccioli G, Galleyrand JC, Fehrentz JA, Martinez J: New active series of growth hormone secretagogues. J Med Chem. 2003 Mar 27;46(7):1191-203.PubMed: 12646029
  2. 2 . Broglio F, Boutignon F, Benso A, Gottero C, Prodam F, Arvat E, Ghe C, Catapano F, Torsello A, Locatelli V, Muccioli G, Boeglin D, Guerlavais V, Fehrentz JA, Martinez J, Ghigo E, Deghenghi R: EP1572: a novel peptido-mimetic GH secretagogue with potent and selective GH-releasing activity in man. J Endocrinol Invest. 2002 Sep;25(8):RC26-8.PubMed: 12240910
  3. 3 . Garcia JM, Swerdloff R, Wang C, Kyle M, Kipnes M, Biller BM, Cook D, Yuen KC, Bonert V, Dobs A, Molitch ME, Merriam GR: Macimorelin (AEZS-130)-stimulated growth hormone (GH) test: validation of a novel oral stimulation test for the diagnosis of adult GH deficiency. J Clin Endocrinol Metab. 2013 Jun;98(6):2422-9. doi: 10.1210/jc.2013-1157. Epub 2013 Apr 4.PubMed: 23559086
  4. 4 . Piccoli F, Degen L, MacLean C, Peter S, Baselgia L, Larsen F, Beglinger C, Drewe J: Pharmacokinetics and pharmacodynamic effects of an oral ghrelin agonist in healthy subjects. J Clin Endocrinol Metab. 2007 May;92(5):1814-20. doi: 10.1210/jc.2006-2160. Epub 2007 Feb 6.PubMed: 17284637
  5. 5 . Fukuda I, Hizuka N, Muraoka T, Ichihara A: Adult growth hormone deficiency: current concepts. Neurol Med Chir (Tokyo). 2014;54(8):599-605. Epub 2014 Jul 28.PubMed: 25070016