Jesduvroq Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Tabs—30
Manufacturer
Generic Availability
NO
Mechanism of Action
Daprodustat is a reversible inhibitor of hypoxia inducible factor (HIF), prolyl 4-hydroxylases (PH)1, PH2 and PH3. 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 Indications
Indications
Anemia due to chronic kidney disease (CKD) in adults who have been receiving dialysis for ≥4mos.
Limitations of Use
Not been shown to improve quality of life, fatigue, or patient well-being. Not indicated for red blood cell transfusion substitute in patients who require immediate correction of anemia. Not for anemia of CKD in patients not on dialysis.
Jesduvroq Dosage and Administration
Adult
Use lowest effective dose. Individualize. Swallow whole. Not being treated with ESA: Pre-treatment Hgb (<9g/dL): 4mg once daily; (9–10g/dL): 2mg once daily; (>10g/dL): 1mg once daily. Switching from ESA (eg, epoetin alfa, darbepoetin alfa, methoxy PEG-epoetin beta): see full labeling. Max Hgb target: 11g/dL. Max treatment: 24 weeks. Moderate hepatic impairment or concomitant moderate CYP2C8 inhibitors: reduce initial dose by ½, unless already taking 1mg.
Children
Not established.
Jesduvroq Contraindications
Contraindications
Concomitant strong CYP2C8 inhibitor (eg, gemfibrozil). Uncontrolled hypertension.
Jesduvroq Boxed Warnings
Boxed Warning
Increased risk of death, myocardial infarction, stroke, venous thromboembolism, thrombosis of vascular access.
Jesduvroq Warnings/Precautions
Warnings/Precautions
Increased risk for thrombotic vascular events (may be fatal), including myocardial infarction (MI), stroke, venous thromboembolism, vascular access thrombosis; evaluate if occurs. History of MI, cerebrovascular event, or acute coronary syndrome within 3mos prior to initiation; not recommended. Preexisting history of heart failure increases risk for hospitalization. Monitor BP periodically. History of GI erosions, peptic ulcer disease, concomitant medications that increase risk of GI erosion, tobacco smokers, use of alcohol. Active malignancies: not recommended. Correct and exclude other causes of anemia (eg, vitamin deficiency, metabolic or chronic inflammatory conditions, bleeding) prior to initiation. Evaluate iron levels prior to and during treatment; give supplemental iron when serum ferritin <100mcg/mL or serum transferrin saturation <20%. Assess ALT, AST, ALP, total bilirubin prior to initiation; repeat tests if signs of liver disease develop. Monitor Hgb every 2 weeks for the first month, then every 4 weeks thereafter, following therapy initiation and after each dose adjustment. Moderate hepatic impairment: reduce initial dose. Severe hepatic impairment: not recommended. Pregnancy. Nursing mothers: not recommended (during and for 1 week after the last dose).
Jesduvroq Pharmacokinetics
Absorption
Following oral administration, median time to peak concentration (Tmax): range from 1–4 hours. Absolute bioavailability: 65%.
Distribution
Following IV dosing, the volume of distribution at steady-state: 14.3 L. Plasma protein bound: >99%.
Elimination
Fecal (74%), renal (21%). Half-life: 1–4 hours.
Jesduvroq Interactions
Interactions
See Contraindications. Potentiated by moderate CYP2C8 inhibitors (eg, clopidogrel); monitor Hgb and adjust daprodustat dose. Antagonized by CYP2C8 inducers (eg, rifampin); monitor Hgb and adjust daprodustat dose.
Jesduvroq Adverse Reactions
Adverse Reactions
Hypertension, thrombotic vascular events, abdominal pain; MI, stroke, VTE, thrombosis of vascular access, GI erosion.
Jesduvroq Clinical Trials
Jesduvroq Note
Not Applicable
Jesduvroq Patient Counseling
See Literature
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