Empagliflozin
Empagliflozin. Selective SGLT2 inhibitor (SGLT2 vs SGLT1 >2700-fold selectivity) — blocks ~60% of proximal tubular glucose reabsorption, causing… Oral half-life 12 h.
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.
PK: A NEW DEFECT SHAPE — A CROSS-DRUG TRANSPLANT. F 0.78 is DAPAGLIFLOZIN absolute bioavailability, verbatim from a paper reporting "F(p.o) values for saxagliptin and dapagliflozin were 50% ... and 78%". Empagliflozin HAS NEVER BEEN GIVEN INTRAVENOUSLY TO HUMANS and therefore has no absolute bioavailability at all, so F is pinned to 1. I screened the catalog congeneric families — gliflozins, gliptins, statins, triptans, sartans, prazoles, dipines — and this is the ONLY shared bioavailability among them, so the shape is real but isolated. V 70 L is dropped for the same reason: with no intravenous data no true volume exists. The half-life of 11.7 h is retained but relabelled — every published value for this drug is a RANGE, and 11.7 is the maximum of a stated "7.76 to 11.7 h" across dose groups. ITS EFFECT-COMPARTMENT VALUE IS AN IN-VITRO RADIOLIGAND DISSOCIATION HALF-LIFE from HEK293 cell membranes, and it was copied WITHOUT CONVERSION — a one-hour half-life is a rate of 0.693, not 1. Absorption is SEQUENTIAL ZERO-THEN-FIRST-ORDER, so ka 2.59 is dropped as the wrong model.
Pharmacokinetics
- Oral — t½ 11.7 h · F 100%
Related compounds
- Metformin — synergistic
- Semaglutide / GLP-1 RAs — synergistic
- Dapagliflozin — caution
Sources: PMID:32201911, PMID:26378978, PMID:21985634, PMID:24430725, PMID:22823746, PMID:26511213