Edoxaban
Edoxaban. Selective, reversible direct inhibitor of activated factor X (FXa) — blocks prothrombinase activity and thrombin generation without… Oral half-life 11 h.
Selective, reversible direct inhibitor of activated factor X (FXa) — blocks prothrombinase activity and thrombin generation without requiring antithrombin III. Once-daily dosing is supported by ~10–14 h terminal t½ plus tight target binding. ~50% renal clearance makes renal function a labelled dose-adjustment trigger. Substrate of P-gp (not CYP3A4-heavy); DDI profile dominated by strong P-gp inhibitors. Andexanet alfa provides off-label reversal.
ABSORPTION-RATE PROVENANCE: this value was derived by inverting the one-compartment peak-time relation in 2026-05-26-wave25-ka-from-tmax.ts, whose header claimed every peak time was verbatim from a primary human study. ALL FORTY-FOUR ENTRIES HAVE NOW BEEN CHECKED AND TWENTY-EIGHT FAIL. This one fails because the midpoint of a verbatim "peak plasma concentrations within 1.0-2.0 h". It is DISCLOSED RATHER THAN DELETED: a midpoint of a narrow range is usually inside the true spread, and removing it would fall back on the solver default of 1.0 per hour, which is worse for most of these records. PK: A TEN-FOLD ERROR THAT NO CITATION CHECK COULD EVER HAVE FOUND, BECAUSE THE FIELD WAS ABSENT RATHER THAN WRONG. With no volume the solver silently substitutes half a litre per kilogram, and at this half-life that asserts a clearance of 2.21 L/h against a verbatim "total clearance is approximately 22 L/h". STORING THE OTHER VERBATIM NUMBER IN THE SAME SENTENCE DOES NOT FIX IT: "the steady-state volume of distribution is approximately 107 L" still leaves the model three-fold slow, because a steady-state volume is not the quantity a one-compartment exposure model consumes. The value stored is that verbatim clearance divided by the rate the stored half-life implies. The bioavailability was verbatim but MISATTRIBUTED — its stated source reports "relative bioavailability (F 1) was estimated as 67.2 %", a different quantity and a different number — so the citation moves to the paper that actually says 62 percent. The half-life itself is an interior pick from ranges that no source states as a point, and the absorption rate remains a disclosed back-derivation from a range midpoint, both left as they are and declared.
Pharmacokinetics
- Oral — t½ 11 h · F 62% · ka 2.52 h⁻¹ · Vd 349 L
Related compounds
Sources: PMID:25186833, PMID:15911722, PMID:26620048