Daprodustat

Daprodustat is a reversible inhibitor of HIF-PH1, PH2 and PH3 (IC 50 in the low nM range). This activity results in the stabilization and nuclear accumulation of HIF-1α and HIF-2α transcription factors, leading to increased transcription of the HIF-responsive genes, including erythropoietin.

• JESDUVROQ is indicated for the treatment of anemia due to chronic kidney disease (CKD) in adults who have been receiving dialysis for at least four months. Limitations of Use JESDUVROQ has not been shown to improve quality of life, fatigue, or patient well-being.ICD-10: D64.9, N18.9

• JESDUVROQ is contraindicated in patients: • Receiving a strong CYP2C8 inhibitor such as gemfibrozil [see Drug Interactions ( 7.1 ), Clinical Pharmacology ( 12.3 )] . • With uncontrolled hypertension [see Warnings and Precautions ( 5.3 )] .contraindicated

• Administer orally once daily, with or without food. ( 2.2 , 2.3 ) • See Full Prescribing Information for starting dosage based on hemoglobin level, liver function and concomitant medications, and for dose titration and monitoring recommendations. ( 2.3 , 2.4 , 2.5 , 2.6 ) 2.1 Pre-Treatment and On-Treatment Evaluations of Anemia, Iron Stores, and Liver Tests Evaluation of Anemia and Iron Stores Correct and exclude other causes of anemia (e.g., vitamin deficiency, metabolic or chronic inflammatory conditions, bleeding) before initiating JESDUVROQ. Evaluate the iron status in all patients before and during treatment with JESDUVROQ. Administer supplemental iron therapy when serum ferritin is less than 100 ng/ml or when serum transferrin saturation is less than 20%. The majority of patients with CKD will require supplemental iron during the course of therapy. Liver Testing Assess serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase, and total bilirubin prior to initiation of JESDUVROQ. Repeat the liver tests if the patient develops signs or symptoms that could be consistent with liver disease during treatment with JESDUVROQ. 2.2 Important Dosing Information Individualize dosing and use the lowest dose of JESDUVROQ sufficient to reduce the need for red blood cell transfusions. Do not target a hemoglobin higher than 11 g/dL. JESDUVROQ can be taken with or without food, and without regard to concomitant administration of iron or phosphate binders [see Clinical Pharmacology ( 12.3 )] . JESDUVROQ should be swallowed whole.

• Risk of Hospitalization for Heart Failure: Increased in patients with a history of heart failure. ( 5.2 ) • Hypertension: Worsening hypertension, including hypertensive crisis may occur. Monitor blood pressure. Adjust anti-hypertensive therapy as needed. ( 5.3 ) • Gastrointestinal Erosion: Gastric or esophageal erosions and gastrointestinal bleeding have been reported. ( 5.4 ) • Not indicated for treatment of anemia of CKD in patients who are not dialysis-dependent ( 5.5 ) • Malignancy: May have unfavorable effects on cancer growth. Not recommended if active malignancy. ( 5.6 ) 5.1 Increased Risk of Death, Myocardial Infarction, Stroke, Venous Thromboembolism, and Thrombosis of Vascular Access JESDUVROQ increases the risk of arterial and venous thrombotic events, that may be fatal, including myocardial infarction, stroke, venous thromboembolism and vascular access thrombosis [see Boxed Warning, Adverse Reactions ( 6.1 )] . Patients with cardiovascular or cerebrovascular disease are at increased risk of these events. Avoid use in patients with a history of myocardial infarction, cerebrovascular event, or acute coronary syndrome within the 3 months prior to starting JESDUVROQ. A rate of hemoglobin rise of greater than 1 g/dL over 2 weeks may contribute to these risks. Targeting a hemoglobin level of greater than 11 g/dL is expected to further increase the risk of death and arterial and venous thrombotic events, as occurs with ESAs, which also increase erythropoietin levels.

The following clinically significant adverse reactions are described elsewhere in the labeling: • Increased Risk of Death, Myocardial Infarction, Stroke, Venous Thromboembolism, and Thrombosis of Vascular Access [see Boxed Warning, Warnings and Precautions ( 5.1 )] . • Risk of Hospitalization for Heart Failure [see Warnings and Precautions ( 5.2 )] . • Hypertension [see Warnings and Precautions ( 5.3 )] . • Gastrointestinal Erosion [see Warnings and Precautions ( 5.4 )] . Most common adverse reactions (incidence ≥10%) are hypertension, thrombotic vascular events, and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact GlaxoSmithKline at 1-888-825-5249 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of JESDUVROQ was evaluated in adults with dialysis-dependent chronic kidney disease with anemia in the ASCEND-D trial based on an on-study analysis (on and off treatment) [see Clinical Studies ( 14.1 )] . Patients were randomized to JESDUVROQ or rhEPO (epoetin alfa for patients on hemodialysis; darbepoetin alfa for patients on peritoneal dialysis). Of the 2,964 patients randomized in the trial, 1,487 were randomized to JESDUVROQ, 1,316 (88.5%) of whom were on hemodialysis and 171 (11.5%) of whom were on peritoneal dialysis.

• Pregnancy: May cause fetal harm. ( 8.1 ) • Lactation: Breastfeeding not recommended until one week after the final dose. ( 8.2 ) • Hepatic Impairment: Reduce the starting dose in patients with moderate hepatic impairment (Child-Pugh Class B). JESDUVROQ not recommended in severe hepatic impairment (Child-Pugh Class C). ( 8.6 ) 8.1 Pregnancy Risk Summary Available data with JESDUVROQ use in pregnant women are insufficient to establish a drug associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. There are risks to the mother and the fetus associated with CKD ( see Clinical Considerations ) . Daprodustat administered orally to pregnant rats and rabbits during the period of organogenesis was associated with adverse fetal outcomes, including embryonic and fetal loss and reduced fetal weight, at doses that caused maternal toxicity and polycythemia ( see Data ). Advise pregnant women of the potential risk to the fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

Daprodustat exposure generally increases in a dose-proportional manner over the range of approved doses. Steady-state concentrations are achieved within 24-hours of dosing.

Headache and gastrointestinal adverse reactions (e.g., nausea) may be seen with acute overdose with JESDUVROQ. There is no specific antidote. Hemodialysis will not substantially remove daprodustat because it is highly protein bound.

• Feb 1, 2023NDANDA216951Glaxosmithkline

1. 1Hospitalisation25815%
2. 2Off Label Use1408.0%
3. 3Product Use Issue1387.9%
4. 4Death1076.1%
5. 5Haemoglobin Decreased905.1%
6. 6Cardiac Failure864.9%
7. 7Renal Impairment864.9%
8. 8Haemoglobin Increased714.0%
9. 9Dysphagia683.9%
10. 10Nephrogenic Anaemia623.5%
11. 11Marasmus593.4%
12. 12Cerebral Infarction573.2%
13. 13Fall512.9%
14. 14Pneumonia432.4%
15. 15Condition Aggravated402.3%

The 10 most recently updated of 38 ClinicalTrials.gov registrations naming Daprodustat as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• REDCURE Registry for Chronic Kidney Disease (CKD) Anemia
  Not yet recruiting · Observational · 384 enrolled · Nabiqasim Industries (Pvt) Ltd
  NCT07346547updated 2026-01-20
• A Study to Evaluate Efficacy and Safety of QLG1218(Daprodustat) in Chinese Hemodialysis (HD)-Dependent Subjects With Anemia Associated With Chronic Kidney Disease (CKD)
  Not yet recruiting · Phase 3 · Interventional · 100 enrolled · Qilu Pharmaceutical Co., Ltd.
  NCT07300111updated 2025-12-23
• Anemia Studies in CKD: Erythropoiesis Via a Novel PHI Daprodustat - Pediatric (ASCEND-P)
  Completed · Phase 3 · Interventional · 4 enrolled · GlaxoSmithKline
  NCT05682326updated 2025-11-10
• Comparison of Daprodustat Formulations Produced by Two Methods of Manufacture for Bioequivalence and Dissolution in Healthy Participants
  Completed · Phase 1 · Interventional · 259 enrolled · GlaxoSmithKline
  NCT04640311updated 2025-04-10
• A Prospective Interventional Study Assessing the Clinical and Operational Effectiveness of Transitioning From Mircera to Daprodustat for the Treatment of Anemia in End Stage Kidney Disease
  Completed · Phase 4 · Interventional · 161 enrolled · USRC Kidney Research
  NCT05951192updated 2024-05-24
• Anemia Studies in Chronic Kidney Disease: Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor Daprodustat-Non-Dialysis (ASCEND-ND)
  Completed · Phase 3 · Interventional · 3,872 enrolled · GlaxoSmithKline
  NCT02876835updated 2024-04-02
• Anemia Studies in Chronic Kidney Disease (CKD): Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat in Non-Dialysis Subjects Evaluating Hemoglobin (Hgb) and Quality of Life (ASCEND-NHQ)
  Completed · Phase 3 · Interventional · 614 enrolled · GlaxoSmithKline
  NCT03409107updated 2024-04-02
• Anemia Studies in CKD: Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat- Iron (ASCEND: Fe)
  Completed · Phase 2 · Interventional · 15 enrolled · GlaxoSmithKline
  NCT03457701updated 2024-03-27
• Anemia Study in Chronic Kidney Disease (CKD) : Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat -Forearm Blood Flow (ASCEND-FBF)
  Terminated · Phase 2 · Interventional · 6 enrolled · GlaxoSmithKline
  NCT03446612updated 2024-03-27
• Anemia Studies in Chronic Kidney Disease: Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor Daprodustat-Dialysis (ASCEND-D)
  Completed · Phase 3 · Interventional · 2,964 enrolled · GlaxoSmithKline
  NCT02879305updated 2021-12-03

Frequently asked questions

How does Daprodustat work?

Daprodustat is a reversible inhibitor of HIF-PH1, PH2 and PH3 (IC 50 in the low nM range). This activity results in the stabilization and nuclear accumulation of HIF-1α and HIF-2α transcription factors, leading to increased transcription of the HIF-responsive genes, including erythropoietin.

What is Daprodustat used for?

According to FDA labeling, Daprodustat carries indications including: JESDUVROQ is indicated for the treatment of anemia due to chronic kidney disease (CKD) in adults who have been receiving dialysis for at least four months. Limitations of Use JESDUVROQ has not been shown to improve quality of life, fatigue, or patient well-being.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Daprodustat?

Daprodustat is classified as Other antianemic preparations, Hypoxia-inducible Factor Prolyl Hydroxylase Inhibitor, Cytochrome P450 2C8 Inhibitors, Hypoxia-inducible Factor Inhibitors, Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors, Increased Transcription to RNA.

What are the brand names for Daprodustat?

Daprodustat is marketed under brand names including Jesduvroq.

What are the contraindications for Daprodustat?

Daprodustat labeling lists contraindications including: JESDUVROQ is contraindicated in patients: • Receiving a strong CYP2C8 inhibitor such as gemfibrozil [see Drug Interactions ( 7.1 ), Clinical Pharmacology ( 12.3 )] . • With uncontrolled hypertension [see Warnings and Precautions ( 5.3 )] .. Always consult the full prescribing information and a clinician.