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diacerein

Small moleculeexperimental

Diacerein (INN), also known as diacetylrhein, is a slow-acting medicine of the class anthraquinone used to treat joint diseases such as osteoarthritis. It works by inhibiting interleukin-1 beta. An updated 2014 Cochrane review found diacerein had a small beneficial effect on pain. Diacerein-containing medications are registered in some European Union and Asian countries and included as a treatment option on several international therapeutic guidelines. — Wikipedia

Clinical trial activity

34 trials · 32 clinical orgs · 0 marketing orgs

Phase 1
6
Phase 2
17
Phase 3
7
Phase 4
8

Earliest trial started Mar 1, 1993 (NCT00451360)

Timeline

1990s

  1. Jan 1, 1993

    Earliest Phase 3 Sponsor(trial)

2010s

  1. Jan 1, 2010

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2017

    Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

  • Interleukin-1 receptorANTAGONIST

    IL1R1 antagonist

  • Unspecified targetOTHER

    Unknown

    Diacerein is a prodrug that is metabolized to rhein. It is a symptomatic slow-acting drug in osteoarthritis (SYSADOA) with anti-inflammatory, anti-catabolic and pro-anabolic properties on cartilage and synovial membrane. It has also been shown to have protective effects against subchondral bone remodelling. The principal mechanism of action of diacerein is to inhibit the interleukin-1 beta (IL-1beta) system and related downstream signalling. Diacerein has been shown to impact the activation of IL-1beta via a reduced production of IL-1 converting enzyme, as well as to affect the sensitivity to IL-1 by decreasing IL-1 receptor levels on the cell surface of chondrocytes and by indirectly increasing IL-1 receptor antagonist production.

  • Unspecified targetUnclear

    unclear

    Diacerein is a prodrug that is metabolized to rhein. It is a symptomatic slow-acting drug in osteoarthritis (SYSADOA) with anti-inflammatory, anti-catabolic and pro-anabolic properties on cartilage and synovial membrane. It has also been shown to have protective effects against subchondral bone remodelling. The principal mechanism of action of diacerein is to inhibit the interleukin-1 beta (IL-1beta) system and related downstream signalling. Diacerein has been shown to impact the activation of IL-1beta via a reduced production of IL-1 converting enzyme, as well as to affect the sensitivity to IL-1 by decreasing IL-1 receptor levels on the cell surface of chondrocytes and by indirectly increasing IL-1 receptor antagonist production.

Chemistry & pharmacology

Loading structure…

SMILES

CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O
Mol. weight
368.3 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 2-anthracenecarboxylic acid, 4,5-bis(acetyloxy)-9,10-dihydro-9,10-dioxo-
  • art 50
  • art 50
  • art brand of diacetylrhein
  • artrodar
  • diacerein
  • diacerein
  • diacerein
  • diacerein
  • diacerein
  • diacerein
  • diacerein
  • diacerein
  • diacerhein
  • diacerhein
  • diacetylrhein
  • diacetylrhein
  • diacetyl-rhein
  • fisiodar
  • fisiodar
  • fisiodar
  • negma brand of diacetylrhein
  • niverpharm brand of diacetylrhein
  • zondar

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07199933N/AOct 1, 2025Nanjing University of Traditional Chinese Medicine
NCT06308068Phase 1Jul 30, 2024Mahidol University
NCT06912035Phase 2/Phase 3 (Phase 3)Jun 21, 2024Universitas Sriwijaya
NCT06073132Phase 2/Phase 3 (Phase 3)Dec 31, 2023TWi Biotechnology, Inc.
NCT05226754Phase 2Apr 1, 2022Fundação de Amparo à Pesquisa do Estado de São Paulo, University of Campinas
NCT04917679Phase 2Sep 1, 2020Shandong University
NCT04318041Phase 3Apr 30, 2020TRB Chemedica
NCT03754634Phase 2Jun 1, 2019Anhui Medical University, China Medical University, Dalian Medical University, People's Liberation Army of China, Shandong University, Zhejiang Chinese Medical University
NCT03472287Phase 1May 10, 2018Castle Creek Pharmaceuticals
NCT03468322Phase 2Apr 30, 2018TWi Biotechnology, Inc.
NCT03404479Phase 4Jan 25, 2018Catholic University of Korea, Korea University
NCT03472547Phase 1Jan 15, 2018Castle Creek Pharmaceuticals
NCT03472534Phase 1Jan 9, 2018Castle Creek Pharmaceuticals
NCT03473197Phase 1Jan 8, 2018Castle Creek Pharmaceuticals
NCT03473184Phase 1Dec 12, 2017Castle Creek Pharmaceuticals
NCT03389308Phase 2Dec 1, 2017Castle Creek Pharmaceuticals
NCT03286582Phase 2Sep 5, 2017TWi Biotechnology, Inc.
NCT03154333Phase 2May 31, 2017Castle Creek Pharmaceuticals
NCT02688400Phase 3May 1, 2016ArthroLab Inc., TRB Chemedica, University of Montreal
NCT02470689Phase 2Jun 1, 2015Ichilov Medical Center, Tel Aviv University
Showing 20 of 34 trials
Page 1 / 2

Organizations

Research & Development (32)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Castle Creek PharmaceuticalsFor profit7722017
Laboratoires NEGMAFor profit4421993
TRB ChemedicaFor profit3322010
TWi Biotechnology, Inc.For profit3322017
University of CampinasAcademic/Hospital3212013
ANS PharmaFor profit2112013
Conselho Nacional de Desenvolvimento Científico e TecnológicoGovernment2012013
Mahidol UniversityAcademic/Hospital2222013
Shandong UniversityAcademic/Hospital2212019
University of MontrealAcademic/Hospital2022007
Anhui Medical UniversityAcademic/Hospital1012019
ArthroLab Inc.For profit1012016
Catholic University of KoreaAcademic/Hospital1112018
China Medical UniversityAcademic/Hospital1012019
Dalian Medical UniversityAcademic/Hospital1012019
Federal University of Rio de JaneiroAcademic/Hospital1112014
Fundação de Amparo à Pesquisa do Estado de São PauloAcademic/Hospital1012022
GMC AmritsarAcademic/Hospital1012007
Government Medical College, AmritsarAcademic/Hospital1112007
Government of MexicoGovernment1112011
32 organizations
Page 1 / 2