Drug intelligence / Profile preview

canagliflozin + rifampin

Development stage
Preclinical
Lead developer
OMJ Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two drugs: **canagliflozin**, a sodium-glucose co-transporter 2 (SGLT2) inhibitor used for the treatment of type 2 diabetes mellitus, and **rifampin** (also known as rifampicin), a rifamycin-class antibiotic commonly used to treat tuberculosis and atypical mycobacterial infections. Canagliflozin lowers blood glucose by inhibiting SGLT2 in the proximal renal tubules, reducing glucose reabsorption and increasing urinary glucose excretion. Rifampin is a potent inducer of several metabolic enzymes and drug transporters, leading to significant pharmacokinetic interactions. Coadministration of rifampin with canagliflozin markedly reduces plasma concentrations and systemic exposure of canagliflozin through induction of hepatic and extrahepatic UDP-glucuronosyltransferases (UGT1A9 and UGT2B4) and efflux drug transporters (notably P-glycoprotein and MRP2)[1][2][3]. The combination is not a marketed product but is relevant for clinical drug-drug interaction management.

02

Targets

CYP3A4 (Cytochrome P450 3A4)RNAP (Bacterial dna-dependent RNA polymerase)SGLT2 (Sodium-glucose cotransporter protein subunit 2)

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