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:
- Application site reactions such as redness and pain.
- Blood count changes such as anemia, thrombocytopenia, leukopenia / neutropenia.
- Gastrointestinal disturbances such as nausea, vomiting, diarrhea and constipation.