Diacerein

171.33 Ų [M+K]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]；170.4 Ų [M+H-H2O]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]；168.12 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]；169.49 Ų [M+Na]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

This chemical does not meet GHS hazard criteria for 3.3% (2 of 60) of reports.

Warning

H315 (96.7%): Causes skin irritation [Warning Skin corrosion/irritation]；H319 (96.7%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]；H335 (95%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure; Respiratory tract irritation]

P261, P264, P264+P265, P271, P280, P302+P352, P304+P340, P305+P351+P338, P319, P321, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 60 reports by companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.；Reported as not meeting GHS hazard criteria per 2 of 60 reports by companies.；There are 6 notifications provided by 58 of 60 reports by companies with hazard statement code(s).；Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. For more detailed information, please visit ECHA C&L website.

Status: Active Update: 27-03-2018 https://echa.europa.eu/registration-dossier/-/registered-dossier/23352

Status: Active Update: 30-07-2020 https://echa.europa.eu/registration-dossier/-/registered-dossier/31372

Skin Irrit. 2 (96.7%)；Eye Irrit. 2 (96.7%)；STOT SE 3 (95%)

Not Classified

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

Diacerein

DILI Positive

DOI:10.1016/j.drudis.2019.09.022

Status: Active Update: 27-03-2018 https://echa.europa.eu/registration-dossier/-/registered-dossier/23352

Status: Active Update: 30-07-2020 https://echa.europa.eu/registration-dossier/-/registered-dossier/31372

M - Musculo-skeletal system；M01 - Antiinflammatory and antirheumatic products；M01A - Antiinflammatory and antirheumatic products, non-steroids；M01AX - Other antiinflammatory and antirheumatic agents, non-steroids；M01AX21 - Diacerein

QM - Musculo-skeletal system；QM01 - Antiinflammatory and antirheumatic products；QM01A - Antiinflammatory and antirheumatic products, non-steroids；QM01AX - Other antiinflammatory and antirheumatic agents, non-steroids；QM01AX21 - Diacerein

99% of rhein is bound to plasma proteins.

Decreases inflammation and cartilage destruction and also corrects altered osteoblast acitivity.

Diacerein's active metabolite rhein [DB13174] reduces cartilage destruction by decreasing expression of matrix metalloproteinase (MMP)-1 and -3 as well as upregulating tissue inhibitor of matrix metalloproteinases which serve to reduce the activity of several MMPs. The anti-inflammatory action of rhein reduces the level of interleukin-1beta activity which plays a large role in reduction of extracellular matrix production, MMP activity, and continued inflammation. Rhein reduces abnormal osteoblast synthetic activity through an unknown mechanism.

4-10h.

Entirely converted to rhien [DB13174] through double deacetylation before reaching systemic circulation. Rhein [DB13174] is further metabolized to rhein glucuronide and rhein sulfate.

Substances that reduce or suppress INFLAMMATION.

Bioavailability of 50-60%. Entirely converted to the active metabolite rhein [DB13174] before reaching systemic circulation.

37% excreted in urine and 53% in feces as estimated in rats.

15-60L.

Total CL is 1.5L/h and renal CL is 0.1L/h.

Pharmaceuticals