azacitidine: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
azacitidine: clinical details
Prescribing considerations
- Initiate and supervise treatment through a clinician experienced in systemic anti-cancer therapy.
- Verify product name, formulation and route at every transition because oral and injectable azacitidine have different exposure and licensed roles.
- Assess baseline cytopenias, renal and hepatic function, infection and bleeding risk.
- Use caution with renal impairment, significant hepatic impairment, high tumour burden, or substantial cardiac or pulmonary disease.
- Counsel about differentiation syndrome, fertility preservation, contraception and prompt reporting of fever or bleeding.
Contraindications and cautions
- Hypersensitivity to azacitidine or formulation excipients
- Breastfeeding
- Advanced malignant hepatic tumours for injectable azacitidine
Monitoring
- Full blood count before treatment and regularly thereafter; increase surveillance when cytopenias or toxicity occur.
- For injectable treatment, monitor liver function, serum creatinine and bicarbonate before and during therapy.
- Monitor for infection, bleeding, gastrointestinal toxicity, renal or hepatic injury, tumour lysis and differentiation syndrome.
- Consider cardiopulmonary assessment in patients with relevant pre-existing disease.
Clinical pharmacology
Azacitidine is a pyrimidine analogue with cytotoxic and hypomethylating activity. It incorporates into RNA and DNA, inhibits DNA methyltransferase and alters gene expression and protein synthesis. Metabolism is mainly through spontaneous hydrolysis and cytidine-deaminase-mediated deamination rather than CYP pathways; oral systemic availability is substantially lower than after subcutaneous administration.
Formulation and product differences
- Oral tablets are licensed for AML maintenance after remission; injectable products have separate licences for specified MDS, CMML and AML populations.
- The formulations are not interchangeable because their exposure and clinical use differ.
- Tablets are swallowed whole and may be taken with or without food; injectable powder is reconstituted as a suspension for subcutaneous administration by healthcare professionals.
- Oral tablets contain lactose; injectable products contain mannitol.
azacitidine preparations and strengths
Tablet
Route: Oral
Strengths: 200 mg, 300 mg
Injection
Route: Parenteral
Strengths: 25 mg/mL
azacitidine interactions
Formal interaction studies are limited. The cancer team should review all prescribed, non-prescription and herbal products.
Other antineoplastic treatments
Use together requires caution and monitoring because additive, antagonistic or synergistic effects cannot be excluded.
Proton-pump inhibitors, including omeprazole
Omeprazole had little effect on oral azacitidine exposure, so a clinically important interaction is not expected.
Cytochrome P450 inhibitors or inducers
A clinically important metabolic interaction is considered unlikely because azacitidine is not substantially metabolised through CYP enzymes.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.