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词条 Rimeporide
释义

  1. Mechanism of action

  2. History

  3. See also

     Other drugs for Duchenne muscular dystrophy 

  4. References

{{Infobox drug
| IUPAC_name = N-(2-methyl-4,5-bis(methylsulfonyl)benzoyl)guanidine
| image = Rimeporide skeletal.svg
| alt =
| caption =
| tradename =
| Drugs.com =
| MedlinePlus =
| pregnancy_AU =
| pregnancy_AU_comment =
| pregnancy_US =
| pregnancy_category=
| legal_AU =
| legal_AU_comment =
| legal_CA =
| legal_NZ =
| legal_UK =
| legal_US =
| legal_UN =
| legal_status = Experimental
| routes_of_administration =
| bioavailability =
| protein_bound =
| metabolism =
| metabolites =
| onset =
| elimination_half-life =
| duration_of_action =
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| CAS_number = 187870-78-6
| ATCvet =
| ATC_prefix = none
| ATC_suffix =
| PubChem = 9799487
| ChemSpiderID = 7975252
| DrugBank =
| ChEMBL = 2107802
| UNII = QH6B4V5743
| C=11 | H=15 | N=3 | O=5 | S=2
| smiles = Cc1cc(c(cc1C(=O)NC(=N)N)S(=O)(=O)C)S(=O)(=O)C
| StdInChI=1S/C11H15N3O5S2/c1-6-4-8(20(2,16)17)9(21(3,18)19)5-7(6)10(15)14-11(12)13/h4-5H,1-3H3,(H4,12,13,14,15)
| StdInChIKey = GROMEQPXDKRRIE-UHFFFAOYSA-N
}}Rimeporide is an experimental drug for the treatment of Duchenne muscular dystrophy, being developed by the EspeRare foundation. it has been granted orphan drug status by the European Medicines Agency.[2]

Mechanism of action

The substance blocks an ion pump called sodium–hydrogen antiporter 1 (NHE-1). While the exact mechanism is unknown, it is speculated that inhibition of this pump reduces sodium and calcium overload in cells of Duchenne patients.

History

Rimeporide was designed as a treatment for chronic heart failure. It was unsuccessful in Phase I clinical trials, but was tolerated well by volunteers. Subsequently, the drug was sold to EspeRare, a Swiss nonprofit organisation[4] that aims at developing drugs for rare diseases. {{as of|2015|5}}, the substance is in preclinical development for Duchenne.

See also

Other drugs for Duchenne muscular dystrophy

  • Ataluren
  • Biostrophin (experimental)
  • Idebenone (experimental)

References

1. ^{{cite web|url=http://esperare.org/en/our-mission-and-vision|title=Our mission and vision|publisher=EspeRare|accessdate=23 July 2015}}
2. ^{{cite news|url=http://esperare.org/en/news/esperares-rimeporide-receives-orphan-drug-designation-duchenne-muscular-dystrophy|title=EspeRare’s Rimeporide receives Orphan Drug Designation in Duchenne Muscular Dystrophy|publisher=EspeRare|date=4 May 2015}}
[1][2]
}}

4 : Muscular dystrophy|Orphan drugs|Acylguanidines|Sulfones

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