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Pharmaceuticals

Pharmaceuticals -> Listed in ZINC15

175.13 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

176 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

Danger

H301 (98.1%): Toxic if swallowed [Danger Acute toxicity, oral]

P203, P264, P270, P273, P280, P301+P316, P318, P321, P330, P391, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 54 reports by companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Liver test abnormalities have been reported to occur rarely during benzbromarone therapy, in only 0.1% of patients in clinical trials. Furthermore, it was used widely for many years without reports of hepatotoxicity until the late 1980s, after which several cases of acute liver injury and acute liver failure during benzbromarone therapy were published. Hepatic injury arises after 1 to 6 months of therapy presenting with jaundice and fatigue, usually with a hepatocellular pattern of enzyme elevations. Immunoallergic symptoms (rash, fever) are uncommon. Low levels of autoantibodies have been reported in some cases with liver histology demonstrating chronic active hepatitis, particularly if benzbromarone is not stopped promptly. Upon stopping therapy, resolution is typically within 1 to 3 months. The hepatic injury from benzbromarone is similar to that reported with benzarone, a structurally related drug that was used for peripheral vascular disease, but also withdrawn also because of concerns over hepatotoxicity.

Drug Induced Liver Injury Rank (DILIrank 2.0)

Benzbromarone

vMost-DILI-concern

8

Withdrawn

DOI:10.1016/j.drudis.2016.02.015

M - Musculo-skeletal system

QM - Musculo-skeletal system