Daprodustat
Generic Name: daprodustat
Brand Names:
Jesduvroq
11 DESCRIPTION JESDUVROQ contains daprodustat, an inhibitor of hypoxia inducible factor (HIF), prolyl 4-hydroxylases (PH)1, PH2 and PH3. The chemical name of daprodustat is N‑[(1,3‑dicyclohexylhexahydro-2,4,6-trioxopyrimidin-5-yl) carbonyl]glycine. The molecular formula of daprodustat is C 19 H 27 N 3 O 6 , and its molecular mass is 393.43. The structural formula is shown below. Daprodustat is a white to off-white powder that is poorly soluble in water.
Overview
11 DESCRIPTION JESDUVROQ contains daprodustat, an inhibitor of hypoxia inducible factor (HIF), prolyl 4-hydroxylases (PH)1, PH2 and PH3. The chemical name of daprodustat is N‑[(1,3‑dicyclohexylhexahydro-2,4,6-trioxopyrimidin-5-yl) carbonyl]glycine. The molecular formula of daprodustat is C 19 H 27 N 3 O 6 , and its molecular mass is 393.43. The structural formula is shown below. Daprodustat is a white to off-white powder that is poorly soluble in water.
Uses
1 INDICATIONS AND USAGE 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. JESDUVROQ is not indicated for use: • As a substitute for red blood cell transfusions in patients who require immediate correction of anemia. • For treatment of anemia of chronic kidney disease in patients who are not on dialysis. JESDUVROQ is a hypoxia-inducible factor prolyl hydroxylase (HIF PH) inhibitor indicated for the treatment of anemia due to chronic kidney disease in adults who have been receiving dialysis for at least four months.
Dosage
2 DOSAGE AND ADMINISTRATION • 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.
Side Effects
6 ADVERSE REACTIONS 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.
Interactions
7 DRUG INTERACTIONS • Moderate CYP2C8 Inhibitors: Reduce starting dose. ( 7.1 ) • CYP2C8 Inducers: Monitor hemoglobin and adjust the dose of JESDUVROQ as appropriate. ( 7.2 ) 7.1 CYP2C8 Inhibitors Concomitant administration of strong CYP2C8 inhibitors (e.g., gemfibrozil) with JESDUVROQ is contraindicated due to a marked increase in daprodustat exposure [see Contraindications ( 4 ), Clinical Pharmacology ( 12.3 )] . Concomitant administration of moderate CYP2C8 inhibitors (e.g., clopidogrel) increases daprodustat exposure [see Clinical Pharmacology ( 12.3 )] . Reduce the starting dose of JESDUVROQ by half when initiating treatment in patients on clopidogrel or a moderate CYP2C8 inhibitor except in patients whose starting dose is already 1 mg.
Warnings
WARNING: INCREASED RISK OF DEATH, MYOCARDIAL INFARCTION, STROKE, VENOUS THROMBOEMBOLISM, and THROMBOSIS OF VASCULAR ACCESS JESDUVROQ increases the risk of thrombotic vascular events, including major adverse cardiovascular events (MACE) [see Warnings and Precautions ( 5.1 )] . 5 WARNINGS AND PRECAUTIONS • 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. 4 CONTRAINDICATIONS 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 )] . • Strong cytochrome P450 2C8 (CYP2C8) inhibitors such as gemfibrozil. ( 4 ) • Uncontrolled hypertension. ( 4 )
Pregnancy
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 ).
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied JESDUVROQ tablets contain 1 mg, 2 mg, 4 mg, 6 mg or 8 mg of daprodustat. Tablet Strength Package Configuration and NDC Number Tablet Description and Markings 1 mg 30 count bottle (NDC 0173-0897-13) Round, gray, biconvex, film-coated tablets debossed with “GS KF” on one side 100 count blister pack (NDC 0173-0897-56) 2 mg 30 count bottle (NDC 0173-09...
Frequently Asked Questions
What is Daprodustat used for?▼
1 INDICATIONS AND USAGE 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. JESDUVROQ is not indicated for use: • As a substitute for red blood cell transfusions in patients who require immediate correction of anemia. • For treatment of anemia of chronic kidney disease in patients who are not on dialysis. JESDUVROQ is a hypoxia-inducible factor prolyl hydroxylase (HIF PH) inhibitor indicated for the treatment of anemia due to chronic kidney disease in adults who have been receiving dialysis for at least four months.
What are the side effects of Daprodustat?▼
6 ADVERSE REACTIONS 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.
Can I take Daprodustat during pregnancy?▼
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 ).
What are the important warnings for Daprodustat?▼
WARNING: INCREASED RISK OF DEATH, MYOCARDIAL INFARCTION, STROKE, VENOUS THROMBOEMBOLISM, and THROMBOSIS OF VASCULAR ACCESS JESDUVROQ increases the risk of thrombotic vascular events, including major adverse cardiovascular events (MACE) [see Warnings and Precautions ( 5.1 )] . 5 WARNINGS AND PRECAUTIONS • 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. 4 CONTRAINDICATIONS 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 )] . • Strong cytochrome P450 2C8 (CYP2C8) inhibitors such as gemfibrozil. ( 4 ) • Uncontrolled hypertension. ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.