Azacitidine

Products

Azacitidine is commercially available as a lyophilizate for the preparation of a suspension for injection (Vidaza, generic). It has been approved in many countries since 2006.

Structure and properties

Azacitidine (C8H12N4O5, Mr = 244.2 g/mol) is a derivative of the nucleoside cytidine found in nucleic acids. It belongs to the pyrimidine nucleoside analogues. Azacitidine exists as a white crystalline powder and is sparingly soluble in water. It is a prodrug of azacitidine triphosphate.

Effects

Azacitidine (ATC L01BC07) has cytotoxic and antiproliferative properties. On the one hand, the effects are due to the integration of the drug into RNA and DNA, which eventually leads to cell death. On the other hand, azacitidine at low doses also leads to hypomethylation of DNA through covalent binding and inhibition of DNA methyltransferases. This restores the expression of genes. The half-life is in the range of 0.7 hours.

Indications

For the treatment of patients who are not suitable for hematopoietic stem cell transplantation:

  • Myelodysplastic syndrome
  • Chronic myelomonocytic leukemia
  • Acute myeloid leukemia (AML)

Dosage

According to the professional information. The drug is injected subcutaneously after preparation.

Contraindications

  • Hypersensitivity
  • Severe liver disease
  • Pregnancy
  • Lactation

Full precautions can be found in the drug label.

Interactions

Azacitidine is not a substrate of CYP450 isozymes. Only incomplete information on drug-drug interactions is available.

Adverse effects

The most common possible adverse effects include: