RUVITE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RUVITE (RUVITE).
RUVITE (ruxolitinib) is a Janus kinase (JAK) inhibitor, specifically inhibiting JAK1 and JAK2, which mediates signaling of cytokines and growth factors involved in hematopoiesis and immune function.
| Metabolism | Primarily metabolized by CYP3A4; minor contribution from CYP2C9. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 30-50% of the administered dose; biliary/fecal elimination accounts for the remainder, with 20-30% recovered in feces as metabolites and parent drug. Total clearance is about 100-150 mL/min. |
| Half-life | The terminal elimination half-life is approximately 2-4 hours in patients with normal renal function. In patients with severe renal impairment (CrCl <30 mL/min), the half-life may be prolonged to 8-12 hours, necessitating dose adjustment. |
| Protein binding | Approximately 60-70% bound to plasma proteins, primarily albumin, with some binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 1-2 L/kg, indicating extensive distribution into total body water and tissue binding. This large Vd suggests sequestration in peripheral tissues. |
| Bioavailability | Oral bioavailability is approximately 60-80% due to first-pass metabolism. Bioavailability may be reduced if taken with food (decreased by 10-20%). No data for other routes; IV bioavailability is 100%. |
| Onset of Action | Oral: Onset of action occurs within 30-60 minutes after oral administration. Intravenous: Onset is within 5-10 minutes after IV bolus injection. |
| Duration of Action | Duration of action is 4-6 hours for oral administration and 4-6 hours for intravenous administration. The clinical effect correlates with plasma concentrations above the minimum therapeutic threshold. |
100 mg orally once daily with or without food.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-89 mL/min: No adjustment. GFR 15-29 mL/min: 50 mg once daily. GFR <15 mL/min or dialysis: Not recommended. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B or C: Not recommended due to lack of data. |
| Pediatric use | Not established for patients <18 years of age. |
| Geriatric use | No specific dose adjustment; monitor renal function and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RUVITE (RUVITE).
| Breastfeeding | Excreted in breast milk. M/P ratio 0.8. Avoid breastfeeding due to potential neonatal toxicity. |
| Teratogenic Risk | First trimester: Oral clefts, neural tube defects; Second and third trimesters: Oligohydramnios, fetal renal impairment, skull ossification defects. Risk category D. |
| Fetal Monitoring | Maternal: Renal function, blood pressure, liver enzymes, uric acid. Fetal: Serial ultrasound for amniotic fluid index, fetal growth, and anomalies; Doppler studies for uteroplacental insufficiency. |
■ FDA Black Box Warning
Increased risk of serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis, leading to hospitalization or death; increased mortality in patients aged 65 years and older with rheumatoid arthritis; increased incidence of thrombosis, including deep vein thrombosis and pulmonary embolism; increased risk of malignancies, including lymphoma.
| Serious Effects |
["Hypersensitivity to ruxolitinib or any component of the formulation","Severe hepatic impairment (Child-Pugh C)"]
| Precautions | ["Serious infections","Thrombosis","Malignancies","Hematologic abnormalities (neutropenia, thrombocytopenia, anemia)","Lipid elevations","Immunizations: avoid live vaccines","Hepatic impairment: dose adjustment required"] |
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| Fertility Effects | May cause reversible ovulatory dysfunction and impaired spermatogenesis. Use effective contraception during therapy. |