Dapagliflozin

Category: pharmacological

Aliases: Farxiga, Forxiga, BMS-512148

Pharmacological Mechanism

Selective SGLT2 inhibitor — first-in-class (approved EU 2012, US 2014). Mechanism + glucosuric output comparable to empagliflozin; slightly lower SGLT2:SGLT1 selectivity (~1400-fold). DAPA-HF established HFrEF benefit independent of diabetes status; DAPA-CKD established CKD progression reduction.

Half-Life (t½)

PO: 12.9h

Dosing Guidelines

• PO: Typical 6.67 mg (Range: 5–10 mg)

Target Organ Systems

• endocrine
• digestive
• renal

Interactions

• Empagliflozin (caution): Same class; not combined. Pick one SGLT2i.
• Metformin (synergistic): Standard dual-therapy pairing.

Pathways It Modulates

• AMPK energy sensor (activator) — AMPK (similar SGLT2i mechanism)
• Insulin signaling + glucose homeostasis (inhibitor) — SGLT2
• Mineralocorticoid receptor (inhibitor) — MR axis (indirect — ↓aldosterone; synergy with MRA in DKD)
• NAFLD / MASH (inhibitor) — SGLT2 → similar pattern
• Notch signaling (inhibitor) — Notch (preclinical fibrosis models)
• Renal tubular transport (inhibitor) — SGLT2

Chemical Identifiers

• PubChem CID: 9887712
• Formula: C21H25ClO6
• Molecular weight: 408.87 g/mol
• InChIKey: JVHXJTBJCFBINQ-ADAARDCZSA-N
• SMILES: CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)Cl

References

• PMID 32201911
• PMID 31535829
• PMID 21226818