Empagliflozin

Category: pharmacological

Aliases: Jardiance, BI 10773

Pharmacological Mechanism

Selective SGLT2 inhibitor (SGLT2 vs SGLT1 >2700-fold selectivity) — blocks ~60% of proximal tubular glucose reabsorption, causing glucosuria 60–90 g/day. Non-insulin-dependent glucose lowering (no hypoglycaemia as monotherapy). Cardioprotective mechanism disputed — proposed osmotic diuresis, natriuresis, improved myocardial energetics (ketone shift), reduced sympathetic tone. EMPA-REG OUTCOME demonstrated MACE + all-cause mortality reduction in T2D with established CVD.

Half-Life (t½)

PO: 11.7h

Dosing Guidelines

PO: Typical 10 mg (Range: 10–10 mg)

Target Organ Systems

cardiovascular
endocrine
digestive
renal

Interactions

Metformin (synergistic): Standard dual-therapy pairing in T2D; complementary mechanisms, no PK interaction.
Semaglutide / GLP-1 RAs (synergistic): Complementary — GLP-1 targets β-cell + appetite; SGLT2i targets renal glucose reabsorption + CV/renal outcomes.
Dapagliflozin (caution): Same class; not combined. Pick one SGLT2i.

Pathways It Modulates

AMPK energy sensor (activator) — AMPK (SGLT2i)
Atherosclerosis plaque pathology (inhibitor) — CV mortality reduction (EMPA-REG) — multifactorial beyond glycemia
Insulin signaling + glucose homeostasis (inhibitor) — SGLT2
Mineralocorticoid receptor (inhibitor) — MR axis (indirect)
NAFLD / MASH (inhibitor) — SGLT2 → weight loss + ↓steatosis (E-LIFT signal)
Renal tubular transport (inhibitor) — SGLT2 (proximal tubule)

Chemical Identifiers

PubChem CID: 11949646
Formula: C23H27ClO7
Molecular weight: 450.91 g/mol
InChIKey: OBWASQILIWPZMG-QZMOQZSNSA-N
SMILES: C1COC[C@H]1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)Cl