Arimoclomol

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Arimoclomol
File:Arimoclomol.svg
Systematic (IUPAC) name
N-{[(2R)-2-hydroxy-3-piperidin-1-ylpropyl]oxy}pyridine-3-carboximidoyl chloride 1-oxide
Clinical data
Legal status
  • Investigational
Routes of
administration		 Oral
Identifiers
CAS Number 289893-25-0 YesY
ATC code none
PubChem CID: 208924
ChemSpider 21106260 YesY
UNII EUT3557RT5 YesY
ChEMBL CHEMBL2107726 N
Chemical data
Formula C14H20ClN3O3
Molecular mass 313.78 g/mol
  • O[C@H](CN1CCCCC1)CO\N=C(\Cl)c2ccc[n+]([O-])c2
  • InChI=1S/C14H20ClN3O3/c15-14(12-5-4-8-18(20)9-12)16-21-11-13(19)10-17-6-2-1-3-7-17/h4-5,8-9,13,19H,1-3,6-7,10-11H2/b16-14+/t13-/m1/s1 YesY
  • Key:SGEIEGAXKLMUIZ-ZPTIMJQQSA-N YesY
 NYesY (what is this?)  (verify)

Arimoclomol (INN; originally codenamed BRX-345, which is a citrate salt formulation of BRX-220) is an experimental drug developed by CytRx Corporation, a biopharmaceutical company based in Los Angeles, California. The orally administered drug is intended to treat amyotrophic lateral sclerosis (ALS).[1][2]

Mechanism of action

Arimoclomol is believed to function by stimulating a normal cellular protein repair pathway through the activation of molecular chaperones. Since damaged proteins, called aggregates, are thought to play a role in many diseases, CytRx believes that arimoclomol could treat a broad range of diseases.

Arimoclomol activates the heat shock response.[3][4][5][6][7][8] It is believed to act at Hsp70.[9]

History

Arimoclomol has been shown to extend life in an animal model of ALS[10] and was well tolerated in healthy human volunteers in a Phase I study. CytRx is currently conducting a Phase II clinical trial.[11]

Arimoclomol also has been shown to be an effective treatment in an animal model of Spinal Bulbar Muscular Atrophy (SBMA, also known as Kennedy's Disease). [12]

Arimoclomol was discovered by Hungarian researchers, as a drug candidate to treat insulin resistance[13][14] and diabetic complications such as retinopathy, neuropathy and nephropathy. Later, the compound, along with other small molecules, was screened for further development by Hungarian firm Biorex, which was sold to CytRx Corporation, who developed it toward a different direction from 2003.

References

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