Roxadustat
Roxadustat. An orally available reversible inhibitor of HIF prolyl-hydroxylase, which stabilises HIF-1alpha and HIF-2alpha and so raises… Oral half-life 13 h.
An orally available reversible inhibitor of HIF prolyl-hydroxylase, which stabilises HIF-1alpha and HIF-2alpha and so raises endogenous erythropoietin. PMID:32487538 verbatim (roxadustat the subject): "In cells, roxadustat increased both HIF-1alpha and HIF-2alpha proteins, leading to an increase in EPO production, even in the presence of EPO-suppressing inflammatory cytokines", and it "significantly decreased hepatic expression of hepcidin ... and increased expression of two genes involved in duodenal iron absorption: divalent metal transporter 1 and duodenal cytochrome b." Approved for anaemia of chronic kidney disease and prohibited in sport as a blood-doping agent. NO NUMERIC IC50 IS PUBLISHED IN ANY ABSTRACT OR LABEL REACHED — see the GAPS row — so no occupancy row is authored.
PubChem CID 11256664 (C19H16N2O5, 352.3), re-queried 2026-09-26. NO SALT FORM EXISTS — PubChem returns PUGREST.NotFound for "roxadustat sodium" — so every dose is the free acid and no dose_moiety_fraction is needed. NO US LABEL EXISTS: DailyMed SPL v2 returns zero records for both `roxadustat` and `evrenzo`, so unlike daprodustat and vadadustat there is no label route to a volume or a binding figure. APPARENT CLEARANCE, RECORDED BUT NOT STORED: PMID:33486718 (popPK, 8209 samples, 2855 CKD patients) gives "apparent clearance of 1.1 (0.0223) L/h in NDD subjects, and apparent central and peripheral volumes of distribution of 14.9 (0.0278) L and 9.5 (0.0872) L". The CL/F is a patient, steady-state, titrated-dose figure and is not mixed with the healthy single-dose t1/2; the volumes are a two-compartment Vc and Vp, and R15 forbids both using a Vc in a one-compartment slot and summing Vc+Vp. HALF-LIVES BY POPULATION, so nobody reconciles them: 12.8 h normal hepatic function single-dose; 17.7 h Child-Pugh B; and "elimination half-life ranged from 14.7 to 19.4 hours" across two ESRD-haemodialysis dose cohorts (PMID:32603526) — a range across cohorts, never to be midpointed. A REVIEW USED ONLY AS A SANITY CHECK, NOT CITED FOR A VALUE: PMID:34905154 aggregates "apparent volume of distribution after oral administration of 22-57 L, apparent clearance of 1.2-2.65 L/h ... the elimination half-life is 9.6-16 h" — secondary literature and all ranges, but it brackets the primary values above.
Pharmacokinetics
- Oral — t½ 12.8 h · F 100%
Sources: PMID:27352308, PMID:32487538, PMID:33486718, PMID:32603526