Drug intelligence / Profile preview

dapagliflozin + roxadustat

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Dapagliflozin + roxadustat is a combination of two small molecule drugs: dapagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, and roxadustat, a hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Dapagliflozin reduces blood glucose by blocking renal glucose reabsorption, and has cytoprotective and cardiorenal benefits, partly by decreasing HIF-1α and activating HIF-2α. Roxadustat treats anemia in chronic kidney disease by inhibiting prolyl hydroxylase enzymes, stabilizing HIF-α subunits, and boosting erythropoietin and iron utilization through modulation of oxygen-sensing pathways. The combination has demonstrated synergistic protective effects on heart and kidney function in preclinical models and can restore podocyte-associated protein expression under diabetic conditions. This combination is being investigated for its ability to provide integrated cardio-renal protection, especially in the context of diabetes and chronic kidney disease[1][5][7].

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)PHD3 (Prolyl hydroxylase domain-containing protein 3)PHD1 (Prolyl hydroxylase domain-containing protein 1)SLCO1B3 (Organic anion transporting polypeptide 1B3)SGLT2 (Sodium-glucose cotransporter protein subunit 2)ABCG2 (Breast cancer resistance protein)EGLN1 (Prolyl hydroxylase domain-containing protein 2)

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