Drug intelligence / Profile preview

empagliflozin + probenecid

Development stage
Preclinical
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

**empagliflozin + probenecid** is a combination of two small molecule drugs: empagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, and probenecid, an inhibitor of organic anion transporters (primarily OAT3) and uridine diphosphate glucuronosyltransferases (UGTs). Empagliflozin works by blocking SGLT2 in the renal proximal tubules, promoting urinary glucose excretion and lowering blood glucose levels, primarily indicated in type 2 diabetes mellitus for glycemic control and reduction of cardiovascular risk. Probenecid inhibits OAT3-mediated renal secretion, increasing the systemic exposure to drugs excreted by this mechanism; it is classically used to manage gout by increasing renal uric acid excretion and to alter elimination of other drugs. The pharmacokinetic interaction between probenecid and empagliflozin leads to an increased plasma concentration of empagliflozin (approximately 1.5-fold increase) due to reduced renal clearance, but studies indicate this does not require empagliflozin dose adjustment for most patients[1][2]. Coadministration may necessitate caution due to possible increased risk of adverse events such as diabetic ketoacidosis[2]. No marketed product currently exists under this combination; information references experimental or off-label coadministration.

02

Targets

SLC22A8 (Organic anion transporter 3)SGLT2 (Sodium-glucose cotransporter protein subunit 2)UGT (UDP-glucuronosyltransferase family)

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