Drug intelligence / Profile preview

probenecid

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Probenecid is a small molecule uricosuric agent primarily used to treat chronic gout and gouty arthritis by increasing the excretion of uric acid through the kidneys, thereby lowering serum urate levels. It acts as a renal tubular blocking agent, inhibiting the reabsorption of urate at the proximal convoluted tubule. This mechanism not only helps prevent gout attacks but also promotes resorption of existing urate deposits. Additionally, probenecid inhibits the secretion of various weak organic acids (including penicillins and some cephalosporins), which can increase plasma concentrations and efficacy of these antibiotics when co-administered. Probenecid has also been shown to inhibit pannexin 1 channels, which may play a role in ATP release from cells[1][2][3][4][5][6].

Brand names
BenemidProbalan
Other names
probenecid
02

Targets

OAT1 (Organic anion transporter 1)PANX1 (Pannexin-1)SLC22A8 (Organic anion transporter 3)URAT1 (Uric Acid Transporter 1)OAT4 (Solute carrier family 22 member 11)

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