Dapagliflozin
Dapagliflozin. Selective SGLT2 inhibitor — first-in-class (approved EU 2012, US 2014). Mechanism + glucosuric output comparable to empagliflozin… Oral half-life 13 h.
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.
PK: MY TRANSPLANT PRIOR IS REFUTED AND THE THEFT RAN THE OTHER WAY — AND WAS ALREADY FIXED. "F(p.o) values for saxagliptin and dapagliflozin were 50% (48, 53%) and 78% (73, 83%), respectively": the stored bioavailability is dapagliflozin OWN, verbatim and correctly attributed. It was EMPAGLIFLOZIN that took it, and that record notes show the theft was caught in an earlier pass and pinned back. DO NOT TOUCH THIS BIOAVAILABILITY. The absorption rate is removed: it was derived from a peak time of 0.9 h that is EXACTLY THE MIDPOINT of a verbatim "time to maximum plasma concentration of 0.5-1.3 h" — the second independent failure of that authoring script header claim. Two further values are unsupported by anything cited and are logged rather than patched: the only abstract-verifiable half-life for this drug is seventeen hours, not the label 12.9 that is stored, and the volume could not be located in any source at all. THE CmaxOVER-AUC IDENTITY FAILS DECISIVELY AND IN BOTH DIRECTIONS AT ONCE — the record under-predicts the peak 2.4x while over-predicting exposure 2.06x, which is the floor-violation signature — and adopting the verbatim seventeen-hour half-life would DEEPEN it. That is the honest signal that this drug needs the two-compartment slot rather than a better scalar. Seven abstracts were chased and not one states an absolute peak or exposure, which is itself the label-only signature.
Pharmacokinetics
- Oral — t½ 12.9 h · F 78% · Vd 112 L
Related compounds
- Empagliflozin — caution
- Metformin — synergistic
Sources: PMID:32201911, PMID:31535829, PMID:21226818, PMID:19129748