Azacitidine tablets are an innovative anti metabolic and demethylating drug. Azacitidine is a pyrimidine nucleoside analogue of cytidine, which exerts its demethylation effect by inhibiting DNA/RNA methyltransferase and is widely used in the treatment of hematological malignancies.

1、 Drug name

Azacitidine tablets, trade name: ONUREG.

2、 Indications

Used for the continued treatment of adult acute myeloid leukemia (AML) patients who achieve first complete response (CR) or complete response with incomplete recovery of blood cell count (CRi) after receiving intensive induction chemotherapy and are unable to complete intensive curative treatment.

3、 Specifications

200mg。

4、 Main components

Active ingredient: Azacitidine.

5、 Usage and dosage

1. Once a day, follow the doctor's advice for specific dosage, take orally, and can be taken with or separately from food.

2. Every 28 days is a cycle, and medication is administered continuously from the 1st to the 14th day of each cycle.

3. Treatment should be continued until the disease progresses or intolerable toxicity occurs.

4. Antiemetics should be used 30 minutes before each administration in the first two cycles. If there is no nausea or vomiting after 2 cycles, antiemetic drugs can be discontinued.

5. If the absolute neutrophil count (ANC) on the first day of the cycle is less than 0.5Gi/L, delay the start of the cycle until ANC ≥ 0.5Gi/L.

6、 Dose adjustment (based on adverse reactions)

1. Neutrophils<0.5Gi/L (Day 1 of cycle): Suspend administration and restore to ≥ 0.5Gi/L at the original dose.

2. Fever accompanied by neutrophils<1Gi/L:

First time: pause and resume at the original dose after reaching ≥ 1Gi/L.

Two consecutive cycles occur: reduce to 200mg after recovery; if the reduction still occurs, shorten the course of treatment by 7 days; If it is sent again, stop using it.

3. Platelets<50Gi/L with bleeding:

First time: pause and resume at the original dose after reaching ≥ 50Gi/L.

Two consecutive cycles occur: reduce to 200mg after recovery; if the reduction still occurs, shorten the course of treatment by 7 days; If it is sent again, stop using it.

4. Grade 3 or 4 nausea/vomiting: pause, resume at the original dose after recovering to ≤ Grade 1; If recurrence occurs, reduce to 200mg after recovery; if it persists, shorten the course of treatment by 7 days; If you continue or resend, stop using.

7、 Medication precautions

1. ONUREG cannot be used as a substitute for intravenous or subcutaneous injection of azacitidine, as their indications and dosages are different.

2. Take at approximately the same time every day.

3. If missed or not taken on time, it should be taken as soon as possible on the same day and restored to the original plan the next day; Do not take two doses on the same day.

4. If vomiting occurs after taking the medication, do not take it again on the same day and take it according to the original plan the next day.

5. It should be swallowed whole and should not be cut, crushed, or chewed.

6. This product is a dangerous drug. If it comes into contact with the skin, it should be thoroughly washed with soapy water immediately. If it comes into contact with mucous membranes, it should be rinsed with water immediately.

8、 Medication for special populations

1. Pregnancy: May cause fetal harm. It is recommended that women with fertility use effective contraception during treatment and for at least 6 months after the last dose; Men should use effective contraception during treatment and for at least 3 months after the last dose. Pregnancy testing should be conducted before treatment.

2. Breastfeeding: It is not recommended to breastfeed during the treatment period and within one week after the last dose.

3. Children: Safety and efficacy have not yet been determined.

4. Elderly: In the QUAZAR study, 72% of patients were ≥ 65 years old, and no overall difference was observed.

5. Renal insufficiency: Patients with severe renal insufficiency (CLcr15-29mL/min) should be monitored for adverse reactions more frequently, without the need for pre adjustment of dosage, but adjustments can be made based on adverse reactions.

6. Liver dysfunction: Mild or moderate liver dysfunction does not require dose adjustment; Severe liver dysfunction has not been studied.

9、 Adverse reactions (≥ 10%)

Nausea, vomiting, diarrhea, fatigue/weakness, constipation, upper respiratory tract infection, pneumonia, abdominal pain, joint pain, decreased appetite, febrile neutropenia, dizziness, skin infection, limb pain.

Serious adverse reactions include pneumonia (8%), febrile neutropenia (7%), and sepsis (6%, including 1 death).

10、 Contraindications

Individuals with a history of severe allergies to azacitidine or any of its components.

11、 Drug interactions

1. The combination with omeprazole (proton pump inhibitor) can increase the AUC of azacitidine by 19%, but has no effect on Cmax.

2. Azacitidine does not inhibit CYP enzymes and does not induce CYP1A2, CYP2C19, CYP3A.

3. Non P-gp, BCRP, OAT1, OAT3, OATP1B1, OATP1B3, OCT2 substrates or inhibitors.

12、 Storage method

Bottled: Store at 20-25 ℃ (68-77 ℃), sealed, and keep the original desiccant canister.

Azacitidineinformation