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Azacitidine

(US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: 5-Azacytidine; Azacitidina; Ladakamycin; NSC-102816; U-18496
USAN: Azacitidine
INN: Azacitidine [rINN (en)]
INN: Azacitidina [rINN (es)]
INN: Azacitidine [rINN (fr)]
INN: Azacitidinum [rINN (la)]
INN: Азацитидин [rINN (ru)]
Chemical name: 4-Amino-1-β-d-ribofuranosyl-1,3,5-triazin-2(1H)-one
Molecular formula: C8H12N4O5 =244.2
CAS: 320-67-2

Adverse Effects and Precautions

The adverse effects of azacitidine are generally similar to those seen with cytarabine. Hypokalaemia, dyspnoea, and bruising are common.

Pharmacokinetics

Azacitidine is rapidly absorbed after subcutaneous use; the bioavailability relative to intravenous use is about 89%. The mean plasma half-life after subcutaneous injection is about 40 minutes. Azacitidine and its metabolites are excreted primarily in the urine; about 50% and 85% is recovered after subcutaneous and intravenous dosing, respectively. The mean elimination half-life is about 4 hours after subcutaneous or intravenous use.

Uses and Administration

Azacitidine is an antimetabolite antineoplastic with general properties similar to those of cytarabine. It also inhibits cellular pyrimidine synthesis. Azacitidine is used in myelodys-plastic syndromes; it has also been used in the treatment of acute myeloid leukaemia.

For the treatment of myelodysplastic syndromes, azacitidine is given subcutaneously or intravenously in a dose of 75 mg/m daily for 7 days, in 4-week cycles. If there is no benefit after 2 cycles, and no toxicity other than nausea and vomiting has occurred, the dose may be increased to 100 mg/m daily. Treatment for at least 4 cycles is usually needed.

Azacitidine should be used with caution in renal impairment and doses adjusted accordingly (see below).

Administration in renal impairment. Adverse renal effects of azacitidine include abnormalities in renal-function tests, renal tubular acidosis, renal failure, and death. US licensed product information recommends that if serum-bicarbonate concentrations fall to below 20 mEq/litre, the dose of azacitidine should be halved for the next course. If there are rises in serum concentrations of urea or creatinine, the next cycle of azacitidine should be delayed until these return to normal or baseline, and the dose should be halved on the next treatment course.

Proprietary Preparations

USA: Vidaza

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