Enarodustat

Hypoxia-inducible factor prolyl hydroxylase inhibitor

{{Drugbox | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-[(4-chlorophenyl)methyl]phenyl]methyl]-1-[(2S)-2-hydroxy-2-phenylethyl]-2,3-dihydro-1H-imidazo[4,5-b]pyridin-2-yl]ethanone | image = Enarodustat.svg | width = 250 | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 1262132-82-0 | ATC_prefix = | ATC_suffix = | PubChem = 49846519 | DrugBank = | ChemSpiderID = 28535835 | UNII = | KEGG = | ChEBI = | ChEMBL = 2103870 | synonyms = JTZ-951 | C=24 | H=22 | Cl=1 | N=3 | O=2 | smiles = C1=CC=C(C=C1)C(C2=CC=C(C=C2)CC3=NC4=C(N3CC(C5=CC=CC=C5)O)N=CC=C4)=O | StdInChI = 1S/C24H22ClN3O2/c25-18-10-8-17(9-11-18)14-19-6-4-16(5-7-19)13-22-27-23-20(12-15-26-24(23)28-22)21(29)24(30)31-24/h4-12,24,30H,13-15H2 | StdInChIKey = }}

Enarodustat is a hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI) used in the treatment of anemia associated with chronic kidney disease (CKD). It works by stabilizing the hypoxia-inducible factor (HIF), which in turn stimulates the production of erythropoietin and enhances erythropoiesis.

Mechanism of Action

Enarodustat inhibits the activity of prolyl hydroxylase, an enzyme responsible for the degradation of HIF under normal oxygen conditions. By inhibiting this enzyme, enarodustat allows HIF to accumulate and activate the transcription of genes involved in erythropoiesis, iron metabolism, and oxygen transport.

Clinical Use

Enarodustat is primarily indicated for the treatment of anemia in patients with chronic kidney disease. It offers an alternative to traditional erythropoiesis-stimulating agents (ESAs) and may provide benefits in terms of reducing the need for intravenous iron supplementation.

Pharmacokinetics

The pharmacokinetic profile of enarodustat includes oral bioavailability, protein binding, metabolism, and elimination half-life. Detailed pharmacokinetic data are essential for understanding the dosing regimen and potential drug interactions.

Side Effects

Common side effects of enarodustat may include hypertension, nausea, and diarrhea. Monitoring for adverse effects is crucial, especially in patients with underlying cardiovascular conditions.

Related Pages

• Anemia
• Chronic kidney disease
• Erythropoiesis
• Hypoxia-inducible factor
• Prolyl hydroxylase