Peringatan Keamanan

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 have not been conducted FDA Label.

Macimorelin

DB13074

small molecule approved investigational

Deskripsi

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 A31481. 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 A31484. Risk factors of AGHD include a history of childhood-onset GH deficiency or with hypothalamic/pituitary disease, surgery, or irradiation to these areas, head trauma, or evidence of other pituitary hormone deficiencies A31481. While there are various therapies available such as GH replacement therapy, the absence of panhypopituitarism and low serum IGF-I levels with nonspecific clinical symptoms pose challenges to the detection and diagnosis of AGHD. The diagnosis of AGHD requires biochemical confirmation with at least 1 GH stimulation test A31481. Macimorelin is clinically useful since it displays good stability and oral bioavailability with comparable affinity to ghrelin receptor as its endogenous ligand. In clinical studies involving healthy subjects, macimorelin stimulated GH release in a dose-dependent manner with good tolerability A31481.

Macimorelin, developed by Aeterna Zentaris, was approved by the FDA in December 2017 under the market name Macrilen for oral solution.

Struktur Molekul 2D

Berat 474.565
Wujud -

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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].
Volume Distribusi 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 [A31482].
Klirens (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 [A31482].

Absorpsi

Macimorelin is a novel, synthetic ghrelin agonist, which is readily absorbed from the gastrointestinal tract A31482. The maximum plasma concentration (Cmax) was observed between 0.5 and 1.5 hours following oral administration of 0.5mg/kg macimorelin to patients with AGHD under fasting for at least 8 hours. Higher doses of drug demonstrate a dose-proportional increase in plasma concentrations A31482. A liquid meal decreased the macimorelin Cmax and AUC by 55% and 49%, respectively FDA Label.

Metabolisme

Macimorelin predominantly undergoes CYP3A4-mediated metabolism according to an *in vitro* human liver microsomes study FDA Label.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. This herb induces the CYP3A metabolism of macimorelin and may reduce its serum concentration, which may cause a false-positive test result.
  • 2. Take on an empty stomach. Fast for at least eight hours before taking macimorelin.

Interaksi Obat

686 Data
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Macimorelin.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Macimorelin.
Erythromycin The serum concentration of Macimorelin can be increased when it is combined with Erythromycin.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Macimorelin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Macimorelin.
Ranolazine The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Macimorelin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Macimorelin.
Methadone The risk or severity of QTc prolongation can be increased when Methadone is combined with Macimorelin.
Diltiazem The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Macimorelin.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Macimorelin.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Macimorelin.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Prochlorperazine is combined with Macimorelin.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Macimorelin.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Macimorelin.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Macimorelin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Macimorelin.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Macimorelin.
Cinnarizine The risk or severity of QTc prolongation can be increased when Cinnarizine is combined with Macimorelin.
Chloroquine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Macimorelin.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Macimorelin.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Macimorelin.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Macimorelin.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Carbinoxamine is combined with Macimorelin.
Dolasetron The risk or severity of QTc prolongation can be increased when Dolasetron is combined with Macimorelin.
Roxithromycin The risk or severity of QTc prolongation can be increased when Roxithromycin is combined with Macimorelin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Macimorelin.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Macimorelin.
Granisetron The risk or severity of QTc prolongation can be increased when Granisetron is combined with Macimorelin.
Ondansetron The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Macimorelin.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Macimorelin.
Mesoridazine The risk or severity of QTc prolongation can be increased when Mesoridazine is combined with Macimorelin.
Desloratadine The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Macimorelin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Lomefloxacin is combined with Macimorelin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Macimorelin.
Primaquine The risk or severity of QTc prolongation can be increased when Primaquine is combined with Macimorelin.
Papaverine The risk or severity of QTc prolongation can be increased when Papaverine is combined with Macimorelin.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Chlorpheniramine is combined with Macimorelin.
Nifedipine The risk or severity of QTc prolongation can be increased when Nifedipine is combined with Macimorelin.
Levofloxacin The risk or severity of QTc prolongation can be increased when Levofloxacin is combined with Macimorelin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Gemifloxacin is combined with Macimorelin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Ofloxacin is combined with Macimorelin.
Propafenone The risk or severity of QTc prolongation can be increased when Propafenone is combined with Macimorelin.
Flecainide The risk or severity of QTc prolongation can be increased when Flecainide is combined with Macimorelin.
Mibefradil The risk or severity of QTc prolongation can be increased when Mibefradil is combined with Macimorelin.
Probucol The risk or severity of QTc prolongation can be increased when Probucol is combined with Macimorelin.
Aceprometazine The risk or severity of QTc prolongation can be increased when Aceprometazine is combined with Macimorelin.
Terlipressin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Macimorelin.
Prenylamine The risk or severity of QTc prolongation can be increased when Prenylamine is combined with Macimorelin.
Fluspirilene The risk or severity of QTc prolongation can be increased when Fluspirilene is combined with Macimorelin.
Lofexidine The risk or severity of QTc prolongation can be increased when Lofexidine is combined with Macimorelin.
Azimilide The risk or severity of QTc prolongation can be increased when Azimilide is combined with Macimorelin.
Pracinostat The risk or severity of QTc prolongation can be increased when Pracinostat is combined with Macimorelin.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Technetium Tc-99m ciprofloxacin is combined with Macimorelin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Garenoxacin is combined with Macimorelin.
Tedisamil The risk or severity of QTc prolongation can be increased when Tedisamil is combined with Macimorelin.
Tucidinostat The risk or severity of QTc prolongation can be increased when Tucidinostat is combined with Macimorelin.
Telavancin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Macimorelin.
Pazopanib The risk or severity of QTc prolongation can be increased when Pazopanib is combined with Macimorelin.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Nemonoxacin is combined with Macimorelin.
Panobinostat The risk or severity of QTc prolongation can be increased when Panobinostat is combined with Macimorelin.
Nilvadipine The risk or severity of QTc prolongation can be increased when Nilvadipine is combined with Macimorelin.
Antazoline The risk or severity of QTc prolongation can be increased when Antazoline is combined with Macimorelin.
Crizotinib The risk or severity of QTc prolongation can be increased when Crizotinib is combined with Macimorelin.
Bedaquiline The risk or severity of QTc prolongation can be increased when Macimorelin is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Fendiline is combined with Macimorelin.
Eperisone The risk or severity of QTc prolongation can be increased when Eperisone is combined with Macimorelin.
Butriptyline The risk or severity of QTc prolongation can be increased when Butriptyline is combined with Macimorelin.
Ceritinib The risk or severity of QTc prolongation can be increased when Ceritinib is combined with Macimorelin.
Lenvatinib The risk or severity of QTc prolongation can be increased when Lenvatinib is combined with Macimorelin.
Melperone The risk or severity of QTc prolongation can be increased when Melperone is combined with Macimorelin.
Benidipine The risk or severity of QTc prolongation can be increased when Benidipine is combined with Macimorelin.
Dexchlorpheniramine maleate The risk or severity of QTc prolongation can be increased when Dexchlorpheniramine maleate is combined with Macimorelin.
Amifampridine The risk or severity of QTc prolongation can be increased when Amifampridine is combined with Macimorelin.
Mocetinostat The risk or severity of QTc prolongation can be increased when Mocetinostat is combined with Macimorelin.
Entinostat The risk or severity of QTc prolongation can be increased when Entinostat is combined with Macimorelin.
Gilteritinib The risk or severity of QTc prolongation can be increased when Gilteritinib is combined with Macimorelin.
CUDC-101 The risk or severity of QTc prolongation can be increased when CUDC-101 is combined with Macimorelin.
Simendan The risk or severity of QTc prolongation can be increased when Simendan is combined with Macimorelin.
Ricolinostat The risk or severity of QTc prolongation can be increased when Ricolinostat is combined with Macimorelin.
Mizolastine The risk or severity of QTc prolongation can be increased when Mizolastine is combined with Macimorelin.
Abexinostat The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Macimorelin.
Oxatomide The risk or severity of QTc prolongation can be increased when Oxatomide is combined with Macimorelin.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Sitafloxacin is combined with Macimorelin.
Sultopride The risk or severity of QTc prolongation can be increased when Sultopride is combined with Macimorelin.
Nizofenone The risk or severity of QTc prolongation can be increased when Nizofenone is combined with Macimorelin.
Bunaftine The risk or severity of QTc prolongation can be increased when Bunaftine is combined with Macimorelin.
Lorcainide The risk or severity of QTc prolongation can be increased when Lorcainide is combined with Macimorelin.
Dexchlorpheniramine The risk or severity of QTc prolongation can be increased when Dexchlorpheniramine is combined with Macimorelin.
Penfluridol The risk or severity of QTc prolongation can be increased when Penfluridol is combined with Macimorelin.
Dexverapamil The risk or severity of QTc prolongation can be increased when Dexverapamil is combined with Macimorelin.
Ivosidenib The risk or severity of QTc prolongation can be increased when Macimorelin is combined with Ivosidenib.
Levacetylmethadol The risk or severity of QTc prolongation can be increased when Levacetylmethadol is combined with Macimorelin.
Clomipramine The risk or severity of QTc prolongation can be increased when Clomipramine is combined with Macimorelin.
Encorafenib The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Macimorelin.
Emedastine The risk or severity of QTc prolongation can be increased when Emedastine is combined with Macimorelin.
Berotralstat The risk or severity of QTc prolongation can be increased when Berotralstat is combined with Macimorelin.
Oxytocin The risk or severity of QTc prolongation can be increased when Oxytocin is combined with Macimorelin.
Esmolol The risk or severity of QTc prolongation can be increased when Esmolol is combined with Macimorelin.
Bortezomib The risk or severity of QTc prolongation can be increased when Bortezomib is combined with Macimorelin.
Fluconazole The metabolism of Macimorelin can be decreased when combined with Fluconazole.

Target Protein

Growth hormone secretagogue receptor type 1 GHSR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12646029
    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.
  • PMID: 12240910
    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.
  • PMID: 23559086
    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.
  • PMID: 17284637
    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.
  • PMID: 25070016
    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.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Macimorelin Aeterna Zentaris
    Granule • 60 mg • Oral • EU • Approved
  • Macrilen
    Granule, for solution • 60 mg/1mg • Oral • US • Approved
  • Macrilen
    Granule, for solution • 60 mg/1mg • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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