Drug intelligence / Profile preview

roxadustat + sacubitril + valsartan

Development stage
Unknown
Lead developer
FibroGen
Modality
Small Molecules
Administration
Oral
01

Overview

Roxadustat + sacubitril + valsartan is a combination of three small molecule drugs, each with distinct mechanisms of action. Roxadustat is a hypoxia-inducible factor prolyl hydroxylase inhibitor that stimulates endogenous erythropoietin production and improves iron metabolism, primarily used for the treatment of anemia in chronic kidney disease. Sacubitril is a neprilysin inhibitor (prodrug), which increases levels of vasoactive peptides by preventing their degradation; it is combined with valsartan, an angiotensin II receptor blocker (ARB) that inhibits the effects of angiotensin II on blood vessels and aldosterone secretion. The sacubitril/valsartan combination (marketed as Entresto) is approved for heart failure and works synergistically to reduce cardiovascular events by enhancing natriuretic peptide activity while blocking the renin-angiotensin-aldosterone system. The triple combination has been investigated in clinical trials for cardiorenal anemia syndrome but does not have an established brand name or regulatory approval as a fixed-dose product[2][1][3][6].

02

Targets

PHD1 (Prolyl hydroxylase domain-containing protein 1)NEP (Neutral Endopeptidase)AGTR1 (Angiotensin II Type-1 receptor)

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