Pronunciation:
de-sye-ta-been/sed-az-ure-i-deen
Trade Name(s)
Ther. Class.
Pharm. Class.
antimetabolites
cytidine deaminase inhibitors
Treatment of various myelodysplastic syndromes (MDS).
Decitabine: inhibits DNA methyltransferase, causing apoptosis; has more effect on rapidly replicating cells. Cedazuridine: acts as a cytidine deaminase inhibitor, preventing the degradation of decitabine in the GI tract and liver; leads to an increase in systemic exposure of decitabine.
Therapeutic Effect(s):
Decreased progression of disease and improved rate of conversion from bring transfusion dependent to independent of red blood cell and platelet transfusions.
Absorption: Cedazuridine increases the oral bioavailability of decitabine.
Distribution: Widely distributed to extravascular tissues.
Metabolism and Excretion: Decitabine: degraded by cytidine deaminase and undergoes physicochemical degradation; Cedazuridine: undergoes physicochemical degradation; 27% excreted unchanged in feces, 21% excreted unchanged in urine.
Half-life: Decitabine: 1.5 hr; Cedazuridine: 6.7 hr.
TIME/ACTION PROFILE (plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
PO | unknown | 1 hr (decitabine); 3 hr (cedazuridine) | unknown |
Contraindicated in:
Use Cautiously in:
CV: arrhythmias, edema, hypotension
Derm: rash
Endo: hyperglycemia, hypoglycemia
F and E: hypocalcemia, hyponatremia
GI: ↑ liver enzymes, abdominal pain, constipation, diarrhea, hypoalbuminemia, mucositis, nausea, vomiting
GU: renal impairment, ↓ fertility (males)
Hemat: ANEMIA, BLEEDING, NEUTROPENIA, THROMBOCYTOPENIA
Metabolic: ↓ appetite, ↓ weight
MS: arthralgia, myalgia
Neuro: dizziness, falls, headache, insomnia, peripheral neuropathy
Resp: cough, dyspnea
Misc: fatigue, fever, INFECTION
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Drug-Drug
None reported.
Do not substitute IV decitabine for decitabine/cedazuridine.
PO (Adults): One tablet (decitabine 35 mg/cedazuridine 100 mg) once daily on Days 1–5 of each 28–day cycle; continue for a minimum of four cycles until disease progression or unacceptable toxicity.
Tablets: decitabine 35 mg/cedazuridine 100 mg
Monitor for signs and symptoms of infection (fever, chills, sore throat) during therapy. If active or uncontrolled infection occurs, delay next cycle and resume at same or reduced dose when resolved.
Lab Test Considerations:
Verify negative pregnancy test before starting therapy.
Obtain CBC prior to each cycle and as clinically indicated. Administer growth factors and anti-infectives for treatment or prophylaxis. If ANC <1,000/mm3 and platelets <50,000/mm3 in the absence of active disease, delay next cycle. Monitor CBC until recovery (ANC ≥1,000/mm3 and platelets ≥50,000/mm3 ). If recovery occurs within 2 wks of achieving remission, continue at same dose. If recovery does not occur within 2 wks, delay cycle for up to 2 additional wks and resume at reduced dose on Days 1–4. May require further dose reductions.
Advise patient to notify health care professional promptly is signs and symptoms of low blood cell counts (fever, chills, body aches, bruising more easily than usual) occur.
Decreased progression of disease and improved rate of conversion from bring transfusion dependent to independent of red blood cell and platelet transfusions.