Peringatan Keamanan

There is no information regarding the acute toxicity (LD50) or overdose of arimoclomol.

Arimoclomol

DB05025

small molecule approved investigational

Deskripsi

Arimoclomol is a hydroxylamine derivative A264414 and a heat-shock protein-70 (HSP70) co-inducer.L51384 Arimoclomol was approved by the FDA on September 20, 2024, making it the first treatment for Niemann-Pick disease, type C (NPC).L51389 It is also being investigated in amyotrophic lateral sclerosis (ALS) A264414, A264429 and inclusion body myositis.A264419

Struktur Molekul 2D

Berat 313.78
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of arimoclomol is approximately four hours.[L51384]
Volume Distribusi The mean apparent volume of distribution (VZ/F) of arimoclomol at steady-state in healthy adult subjects is 211 L. A dose-dependent increase in arimoclomol cerebral spinal fluid concentrations was seen at steady state.[L51384]
Klirens (Clearance) The mean apparent clearance of arimoclomol (CL/F) at steady state is 34 L/hr in healthy adult subjects.[L51384]

Absorpsi

Following the oral administration of 248 mg arimoclomol three times a day in healthy subjects, the geometric mean (CV%) AUC0-8 hours at day one (first dose) and day six (steady-state) were 5317 (17%) hr x ng/mL and 7207 (19%) hr x ng/mL, respectively. The geometric mean (CV%) Cmax at day one (first dose) and day six (steady-state) were 1749 (49%) ng/mL and 2090 (23%) ng/mL, respectively. The median Tmax was approximately 0.5 hours. The absolute bioavailability of arimoclomol following oral administration has not been determined.L51384 No clinically significant difference in arimoclomol pharmacokinetics was observed following the administration of a high-fat, 1000-calorie, 60% fat meal to healthy subjects.L51384

Metabolisme

Arimoclomol is predominantly metabolized through glutathionation, O-glucuronidation and NO-oxime cleavage.L51384

Rute Eliminasi

Following a single dose of radiolabeled arimoclomol 100 mg to healthy male subjects under fasted conditions, approximately 12% of the dose was recovered in feces and 77.5% in urine (42% unchanged).L51384

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food has negligible effects on the pharmacokinetics of arimoclomol.

Interaksi Obat

25 Data
Choline The serum concentration of Choline can be increased when it is combined with Arimoclomol.
Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Arimoclomol.
Reserpine The serum concentration of Reserpine can be increased when it is combined with Arimoclomol.
Metformin The serum concentration of Metformin can be increased when it is combined with Arimoclomol.
Norepinephrine The serum concentration of Norepinephrine can be increased when it is combined with Arimoclomol.
Pramipexole The serum concentration of Pramipexole can be increased when it is combined with Arimoclomol.
Prazosin The serum concentration of Prazosin can be increased when it is combined with Arimoclomol.
Cisplatin The serum concentration of Cisplatin can be increased when it is combined with Arimoclomol.
Oxaliplatin The serum concentration of Oxaliplatin can be increased when it is combined with Arimoclomol.
Epinephrine The serum concentration of Epinephrine can be increased when it is combined with Arimoclomol.
Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Arimoclomol.
Gentamicin The serum concentration of Gentamicin can be increased when it is combined with Arimoclomol.
Ranitidine The serum concentration of Ranitidine can be increased when it is combined with Arimoclomol.
Amantadine The serum concentration of Amantadine can be increased when it is combined with Arimoclomol.
Dopamine The serum concentration of Dopamine can be increased when it is combined with Arimoclomol.
Memantine The serum concentration of Memantine can be increased when it is combined with Arimoclomol.
Varenicline The serum concentration of Varenicline can be increased when it is combined with Arimoclomol.
Histamine The serum concentration of Histamine can be increased when it is combined with Arimoclomol.
Dalfampridine The serum concentration of Dalfampridine can be increased when it is combined with Arimoclomol.
Tetraethylammonium The serum concentration of Tetraethylammonium can be increased when it is combined with Arimoclomol.
Agmatine The serum concentration of Agmatine can be increased when it is combined with Arimoclomol.
Linagliptin The serum concentration of Linagliptin can be increased when it is combined with Arimoclomol.
Nafamostat The serum concentration of Nafamostat can be increased when it is combined with Arimoclomol.
Choline salicylate The serum concentration of Choline salicylate can be increased when it is combined with Arimoclomol.
Solriamfetol The serum concentration of Solriamfetol can be increased when it is combined with Arimoclomol.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27605553
    Kirkegaard T, Gray J, Priestman DA, Wallom KL, Atkins J, Olsen OD, Klein A, Drndarski S, Petersen NH, Ingemann L, Smith DA, Morris L, Bornaes C, Jorgensen SH, Williams I, Hinsby A, Arenz C, Begley D, Jaattela M, Platt FM: Heat shock protein-based therapy as a potential candidate for treating the sphingolipidoses. Sci Transl Med. 2016 Sep 7;8(355):355ra118. doi: 10.1126/scitranslmed.aad9823.
  • PMID: 34418116
    Mengel E, Patterson MC, Da Riol RM, Del Toro M, Deodato F, Gautschi M, Grunewald S, Gronborg S, Harmatz P, Heron B, Maier EM, Roubertie A, Santra S, Tylki-Szymanska A, Day S, Andreasen AK, Geist MA, Havnsoe Torp Petersen N, Ingemann L, Hansen T, Blaettler T, Kirkegaard T, I Dali C: Efficacy and safety of arimoclomol in Niemann-Pick disease type C: Results from a double-blind, randomised, placebo-controlled, multinational phase 2/3 trial of a novel treatment. J Inherit Metab Dis. 2021 Nov;44(6):1463-1480. doi: 10.1002/jimd.12428. Epub 2021 Sep 7.
  • PMID: 38782015
    Benatar M, Hansen T, Rom D, Geist MA, Blaettler T, Camu W, Kuzma-Kozakiewicz M, van den Berg LH, Morales RJ, Chio A, Andersen PM, Pradat PF, Lange D, Van Damme P, Mora G, Grudniak M, Elliott M, Petri S, Olney N, Ladha S, Goyal NA, Meyer T, Hanna MG, Quinn C, Genge A, Zinman L, Jabari D, Shoesmith C, Ludolph AC, Neuwirth C, Nations S, Shefner JM, Turner MR, Wuu J, Bennett R, Dang H, Sundgreen C: Safety and efficacy of arimoclomol in patients with early amyotrophic lateral sclerosis (ORARIALS-01): a randomised, double-blind, placebo-controlled, multicentre, phase 3 trial. Lancet Neurol. 2024 Jul;23(7):687-699. doi: 10.1016/S1474-4422(24)00134-0. Epub 2024 May 20.
  • PMID: 37739573
    Machado PM, McDermott MP, Blaettler T, Sundgreen C, Amato AA, Ciafaloni E, Freimer M, Gibson SB, Jones SM, Levine TD, Lloyd TE, Mozaffar T, Shaibani AI, Wicklund M, Rosholm A, Carstensen TD, Bonefeld K, Jorgensen AN, Phonekeo K, Heim AJ, Herbelin L, Barohn RJ, Hanna MG, Dimachkie MM: Safety and efficacy of arimoclomol for inclusion body myositis: a multicentre, randomised, double-blind, placebo-controlled trial. Lancet Neurol. 2023 Oct;22(10):900-911. doi: 10.1016/S1474-4422(23)00275-2.
  • PMID: 20525256
    Vanier MT: Niemann-Pick disease type C. Orphanet J Rare Dis. 2010 Jun 3;5:16. doi: 10.1186/1750-1172-5-16.
  • PMID: 29367439
    Benatar M, Wuu J, Andersen PM, Atassi N, David W, Cudkowicz M, Schoenfeld D: Randomized, double-blind, placebo-controlled trial of arimoclomol in rapidly progressive SOD1 ALS. Neurology. 2018 Feb 13;90(7):e565-e574. doi: 10.1212/WNL.0000000000004960. Epub 2018 Jan 24.

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