Enarodustat

Prolyl Hydroxylase Domain (PHD) Inhibitor / HIF Prolyl Hydroxylase InhibitorRx: PrescriptionCompound: Approved

Also known as: Enarod, Enarodustat, JTZ-951

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Enarodustat (JTZ-951) is an oral HIF prolyl hydroxylase inhibitor developed by Japan Tobacco and Torii Pharmaceutical for the treatment of renal anemia in patients with chronic kidney disease (CKD), both on and not on dialysis. It is approved in Japan and stimulates endogenous erythropoietin synthesis without the need for injectable erythropoiesis-stimulating agents (ESAs).

Mechanism of Action

Inhibits hypoxia-inducible factor prolyl hydroxylase (HIF-PH) enzymes, stabilizing HIF-alpha subunits and upregulating endogenous erythropoietin production, thereby stimulating erythropoiesis and increasing hemoglobin levels.

Routes of Administration

Oral

Goals & Uses

  • Reduction of ESA injectionsPatient Convenience / Treatment OptimizationHigh
  • Hemoglobin stabilization in non-dialysis CKDNephrologyHigh
  • Iron utilization improvementIron MetabolismModerate
  • Treatment of renal anemiaHematology / NephrologyHigh

Contraindications

  • Active malignancyOncologyModerateUse caution or avoid depending on agent and context
  • PregnancyPopulationHighPotential fetal risk or insufficient safety data
  • Known hypersensitivity to enarodustatAllergyHigh
  • Uncontrolled hypertensionCardiovascularModerate

Adverse Effects

  • HypertensionCardiovascularCommonHigh blood pressure
  • NasopharyngitisInfectiousCommon
  • HeadacheNeurologicCommonPain in the head or upper neck
  • Liver enzyme elevation (ALT/AST)HepaticUncommon
  • Shunt thrombosis (dialysis access)VascularUncommon
  • ThromboembolismCardiovascularUncommon

Drug Interactions

  • Antihypertensive agentsModerate
  • CYP enzymes / drug transportersLow
  • Iron supplementsLow

Population Constraints

  • Patients with active or recent malignancyOncologicRelative
  • Pediatric patientsAgeRelative
  • Patients with severe hepatic impairmentHepaticRelative
  • Pregnant womenReproductiveAbsolute

Regulatory Status

  • European UnionUnapprovedNot approved by the EMA as of the current knowledge cutoff.
  • United StatesUnapprovedNot approved by the FDA as of the current knowledge cutoff; not in late-stage US clinical development.
  • United KingdomUnapprovedNot approved by the MHRA as of the current knowledge cutoff.

Approved in Japan (2022) for renal anemia associated with CKD. Not approved by the FDA or EMA as of the current knowledge cutoff. It is a small molecule, not a peptide in the classical sense, but functions in the erythropoiesis-stimulating pathway.

Evidence & Sources

No sources recorded yet.

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