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bufexamac
- Development stage
- Discontinued
- Modality
- Small Molecules
- Administration
- Topical, Rectal
01
Overview
Bufexamac is a non-steroidal anti-inflammatory drug (NSAID) primarily used topically for the treatment of inflammatory skin conditions such as eczema and dermatitis. It has also been used rectally in combination with other agents for haemorrhoids and anal fissures. The mechanism of action is thought to involve inhibition of cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis and thereby inflammation. Additionally, bufexamac has been identified as an inhibitor of class IIB histone deacetylases (HDAC6 and HDAC10), as well as leukotriene A4 hydrolase (LTA4H), which may contribute to its anti-inflammatory effects[1][2][5][6][8]. Due to a high risk of severe allergic contact dermatitis and insufficient evidence for efficacy, bufexamac has been withdrawn from markets in Europe, Australia, Canada, and the United States[1][4][5].
- Brand names
- ParadermParfenacDroxarylMalipuranBufalCalmadermFansamacMastu SParfenoideProctosan
- Other names
- bufexamac
02
Targets
PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)HDAC6 (Histone deacetylase 6)HDAC10 (Histone Deacetylase 10)LTA4H (Leukotriene A4 hydrolase)
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