Drug intelligence / Profile preview

empagliflozin + rifampicin

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

Overview

Empagliflozin + rifampicin is a combination of two small molecule oral drugs. Empagliflozin is a selective and reversible inhibitor of sodium-glucose cotransporter 2 (SGLT2), decreasing renal glucose reabsorption and increasing urinary glucose excretion, thereby lowering blood glucose levels in patients with type 2 diabetes mellitus. Rifampicin is an antibiotic of the rifamycin class that inhibits bacterial DNA-dependent RNA polymerase, used primarily to treat tuberculosis and other bacterial infections. Pharmacokinetic studies show coadministration of rifampicin with empagliflozin increases empagliflozin exposure by about 35%, but this is not considered clinically meaningful and no dose adjustment of empagliflozin is recommended. Rifampicin’s effect is due to transporter inhibition (OATP1B1/1B3), but empagliflozin exposure is affected less than 2-fold, with good tolerability observed in healthy subjects[1][2][3]. There is no evidence this drug combination is approved or marketed as a fixed-dose product; the combination refers to the coadministration of these two drugs.

02

Targets

SLCO1B3 (Organic anion transporting polypeptide 1B3)SGLT2 (Sodium-glucose cotransporter protein subunit 2)OATP1B1 (Organic anion transporting polypeptide 1B1)ABCG2 (Breast cancer resistance protein)

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