azacitidine at a glance
Medicine class
Antineoplastic antimetabolite and DNA methyltransferase inhibitor.
Available forms
Film-coated tablets and powder prepared as a subcutaneous injection. Oral and injectable azacitidine are not interchangeable.
Monitoring
Regular blood counts are essential. Kidney and liver tests are also required, particularly with injectable treatment.
What is azacitidine used for?
The licensed role depends on the formulation; oral and injectable products must not be substituted for one another.
Injectable azacitidine treats adults unsuitable for haematopoietic stem-cell transplantation who have intermediate-2 or high-risk myelodysplastic syndromes, specified chronic myelomonocytic leukaemia, or specified acute myeloid leukaemia.
Oral azacitidine is maintenance therapy for adults with acute myeloid leukaemia in complete remission, including remission with incomplete blood-count recovery, when stem-cell transplantation is not being pursued.
How does azacitidine work?
Azacitidine is incorporated into RNA and DNA. It inhibits DNA methyltransferase, alters gene activity and disrupts RNA, DNA and protein production. These effects can promote more normal blood-cell development and inhibit or kill abnormal dividing cells in the bone marrow.
azacitidine preparations and strengths
Tablet
Route: Oral
Strengths: 200 mg, 300 mg
Injection
Route: Parenteral
Strengths: 25 mg/mL
How to take azacitidine
Follow the formulation-specific instructions from the specialist cancer team.
Swallow oral tablets whole with water. They may be taken with or without food and must not be split, crushed, dissolved or chewed.
Injectable azacitidine is prepared and given under the skin by a healthcare professional, usually in the upper arm, thigh or abdomen. Injection sites should be rotated, avoiding tender, bruised, red or hardened areas.
Anti-sickness treatment may be prescribed.
azacitidine side effects
Common or expected effects
- Low white cells, red cells or platelets, causing infection risk, tiredness, breathlessness, bruising or bleeding
- Nausea, vomiting, diarrhoea, constipation or abdominal discomfort
- Fatigue, weakness and reduced appetite
- Fever, respiratory infections or pneumonia
- Joint, muscle, back or limb pain
- Injection-site pain, redness or skin reaction with injectable treatment
Get urgent medical advice
- Fever or other signs of serious infection, including pneumonia or sepsis
- Unusual, heavy or persistent bleeding
- Severe allergic reaction with breathing difficulty or facial swelling
- Differentiation syndrome, which may cause fever, breathlessness, swelling, rapid weight gain, low blood pressure or kidney problems
- Kidney failure, severe liver problems, tumour lysis syndrome or necrotising soft-tissue infection
azacitidine in pregnancy
Azacitidine may harm an unborn baby and is generally not recommended during pregnancy unless specialist assessment finds it clearly necessary. Effective contraception is required during treatment and for a period afterwards. Tell the specialist team immediately if pregnancy occurs.
azacitidine while breastfeeding
Breastfeeding is contraindicated during oral or injectable azacitidine treatment because serious effects in a breastfed child cannot be excluded.
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.
Common questions about azacitidine
Answers are fully visible for fast scanning and source review.
Are oral azacitidine and azacitidine injections interchangeable?
No. They contain the same active ingredient but produce different exposure and have different licensed roles.
Can azacitidine tablets be taken with food?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.