pharmacopeia
GET
/api/v1/drug/azacitidine

Mechanism of action

Sourced from openFDA

Azacitidine for injection is a pyrimidine nucleoside analog of cytidine. Azacitidine for injection is believed to exert its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow.

DNA MethyltransferaseNucleic Acid Synthesis

Indications

Sourced from openFDA
  • Azacitidine for injection is a nucleoside metabolic inhibitor indicated for the treatment of: Adult patients with the following FAB myelodysplastic syndrome (MDS) subtypes: Refractory anemia (RA) or refractory anemia with ringed sideroblasts (RARS) (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts (RAEB), refractory anemia with excess blasts in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL). ( 1.1) 1.1 Myelodysplastic Syndromes (MDS) Azacitidine for injection is indicated for treatment of adult patients with the following French-American- British (FAB) myelodysplastic syndrome subtypes: refractory anemia (RA) or refractory anemia with ringed sideroblasts (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts (RAEB), refractory anemia with excess blasts in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL).ICD-10: C95.90, D64.9

Contraindications

Sourced from openFDA
  • Advanced Malignant Hepatic Tumors ( 4.1 ) . Hypersensitivity to Azacitidine or Mannitol (4 .2 ) .contraindicated

Dosage & administration

Sourced from openFDA

Do not substitute azacitidine for injection for oral azacitidine. The indications and dosing regimen for azacitidine for injection differ from that of oral azacitidine ( 2.1 , 5.1 ). MDS: The recommended starting dosage for the first treatment cycle, for all patients regardless of baseline hematology values, is Azacitidine for injection75 mg/m 2 daily for 7 days to be administered by subcutaneous injection or intravenous infusion. See full prescribing information for schedule for subsequent cycles. Premedicate for nausea and vomiting ( 2.2 ). Continue treatment as long as the patient continues to benefit( 2.3 ). Monitor all patients for hematologic response and for renal toxicity; delay or reduce dosage as appropriate ( 2.3 , 2.6 , 2.7 ). 2.1 Important Administration Information Do not substitute azacitidine for injection for oral azacitidine. The indications and dosing regimen for azacitidine for injection differ from that of oral azacitidine [see Warnings and Precautions ( 5.1 )] 2.2 First Treatment Cycle for Adults The recommended starting dose for the first treatment cycle, for all patients regardless of baseline hematology laboratory values, is 75 mg/m 2 subcutaneously or intravenously, daily for 7 days. Premedicate patients for nausea and vomiting. Obtain complete blood counts, liver chemistries and serum creatinine prior to the first dose. 2.3 Subsequent Treatment Cycles for Adults Repeat cycles every 4 weeks.

Warnings & precautions

Sourced from openFDA

Risks of Substitution with Other Azacitidine Products: Do not substitute azacitidine for injection for oral azacitidine ( 2.1 , 5.1 ). Anemia, Neutropenia and Thrombocytopenia: Monitor complete blood counts (CBC) frequently ( 5.2 ). Hepatotoxicity: Patients with severe preexisting hepatic impairment are at higher risk for toxicity ( 5.3 ). Renal Toxicity: Monitor patients with renal impairment for toxicity since azacitidine and its metabolites are primarily excreted by the kidneys ( 5.4 ). Tumor Lysis Syndrome: Azacitidine for injection may cause fatal or serious tumor lysis syndrome, including in patients with MDS. Assess baseline risk and monitor and treat as appropriate ( 5.5 ). Embryo-Fetal Toxicity: Azacitidine for injection can cause fetal harm. Advise female patients and male patients with female partners of reproductive potential of the potential risk to a fetus and to use effective contraception ( 5.6 ). 5.1 Risks of Substitution with Other Azacitidine Products Due to substantial differences in the pharmacokinetic parameters [see Clinical Pharmacology ( 12.3 )] , the recommended dose and schedule for azacitidine for injection are different from those of oral azacitidine products. Treatment of patients using azacitidine for injection at the recommended dosage of oral azacitidine may result in a fatal adverse reaction. Treatment of patients using oral azacitidine at the doses recommended for azacitidine for injection may not be effective. Do not substitute azacitidine for injection for oral azacitidine [see Dosage and Administration ( 2.1 )] .

Adverse reactions

Sourced from openFDA

The following adverse reactions are described in other labelingsections: Anemia, Neutropenia and Thrombocytopenia [see Warnings and Precautions ( 5.2 )] Hepatotoxicity in Patients with Severe Pre-existing Hepatic Impairment [see Warnings and Precautions ( 5.3 )] Renal Toxicity [see Warnings and Precautions ( 5.4 )] Tumor Lysis Syndrome [see Warnings and Precautions ( 5.5 )] Most common adverse reactions (>30%) in adult patients with MDS by subcutaneous route are: nausea, anemia, thrombocytopenia, vomiting, pyrexia, leukopenia, diarrhea, injection site erythema, constipation, neutropenia and ecchymosis. Most common adverse reactions by intravenous route also included petechiae, rigors, weakness and hypokalemia ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Dr. REDDY’S LABORATORIES Inc., at 1-888-375-3784 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical TrialsExperience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. MDS The data described below reflect exposure to azacitidine for injection in 443 patients with MDS from 4 clinical studies.

Use in specific populations

Sourced from openFDA

• Lactation: Advise not to breastfeed ( 8.2 ). Pediatric use information is approved for Celgene Corporation's Vidaza (azacitidine for injection). However, due to Celgene Corporation's marketing exclusivity rights, this drug product is not labeled with that information. 8.1 Pregnancy Risk Summary Based on its mechanism of action and findings in animals, azacitidine for injection can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )]. There are no data on the use of azacitidine in pregnant women. Azacitidine was teratogenic and caused embryo-fetal lethality in animals at doses lower than the recommended human daily dose (see Data). Advise pregnant women of the potential risk to the fetus. The background rate of major birth defects and miscarriage is unknown for the indicated population. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%-4% and 15%-20%, respectively. Data Animal Data Early embryotoxicity studies in mice revealed a 44% frequency of intrauterine embryonal death (increased resorption) after a single IP (intraperitoneal) injection of 6 mg/m 2 (approximately 8% of the recommended human daily dose on a mg/m 2 basis) azacitidine on gestation day 10.

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetics of azacitidine were studied in 6 adult patients with MDS following a single 75 mg/m 2 subcutaneous dose and a single 75 mg/m 2 intravenous dose. Absorption Azacitidine is rapidly absorbed after subcutaneous administration; the peak plasma azacitidine concentration of 750 ± 403 ng/ml occurred in 0.5 hour after subcutaneous administration.

Overdosage

Sourced from openFDA

One case of overdose with azacitidine for injection was reported during clinical trials. A patient experienced diarrhea, nausea, and vomiting after receiving a single intravenous dose of approximately 290 mg/m 2 , almost 4 times the recommended starting dose. The events resolved without sequelae, and the correct dose was resumed the following day. In the event of overdosage, the patient should be monitored with appropriate blood counts and should receive supportive treatment, as necessary. There is no known specific antidote for azacitidine for injection overdosage.

Approval history

Sourced from openFDA
  • May 19, 2004NDANDA050794Bristol-myers
  • Sep 16, 2013ANDAANDA201537Dr Reddys
  • Apr 29, 2016NDANDA208216Actavis Llc
  • Sep 29, 2016ANDAANDA207518Shilpa Medicare
  • Jun 23, 2017ANDAANDA207234Natco Pharma Ltd
  • Jul 2, 2018ANDAANDA207475Accord Hlthcare
  • Jun 8, 2020ANDAANDA209337Eurohlth Intl Sarl
  • Sep 1, 2020NDANDA214120Bristol

FDA shortages

View JSON

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

  • Azacitidine, Injection, 100 mg (NDC 16729-306-10)Active
    Sponsor: Accord Healthcare Inc.
    Updated
  • Azacitidine, Injection, 100 mg (NDC 43598-305-62)Active
    Sponsor: Dr. Reddy's Laboratories, Inc.
    Updated
  • Azacitidine, Injection, 100 mg (NDC 68001-313-56)Active
    Sponsor: Teva Pharmaceuticals USA, Inc. · Reason: Other
    Updated
  • Azacitidine, Injection, 100 mg (NDC 72485-201-01)Active
    Sponsor: Armas Pharmaceuticals Inc · Reason: Other
    Updated
  • Azacitidine, Injection, 100 mg/ Vial (NDC 0143-9606-01)Active
    Sponsor: Hikma Pharmaceuticals USA, Inc. · Reason: Demand increase for the drug
    Updated
  • Azacitidine, Injection, 100 mg/30 mL (NDC 63323-771-39)Active
    Sponsor: Fresenius Kabi USA, LLC
    Updated
  • Azacitidine, Injection, 100 mg/30 mL (NDC 71288-115-30)Active
    Sponsor: Meitheal Pharmaceuticals, Inc.
    Updated
  • Azacitidine, Injection, 100 mg/4 mL (NDC 55150-393-01)Active
    Sponsor: Eugia US LLC · Reason: Demand increase for the drug
    Updated
  • Vidaza, Injection, 100 mg (NDC 59572-102-01)Active
    Sponsor: Bristol Myers Squibb Co.
    Updated

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
28,770 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Death3,31912%
  2. 2Febrile Neutropenia2,89410%
  3. 3Acute Myeloid Leukaemia2,1657.5%
  4. 4Pneumonia1,9646.8%
  5. 5Off Label Use1,9386.7%
  6. 6Neutropenia1,8506.4%
  7. 7Pyrexia1,6085.6%
  8. 8Thrombocytopenia1,5085.2%
  9. 9Myelosuppression1,4675.1%
  10. 10Anaemia1,3184.6%
  11. 11Sepsis1,2304.3%
  12. 12Platelet Count Decreased1,2094.2%
  13. 13Drug Ineffective1,1774.1%
  14. 14Infection1,0843.8%
  15. 15Pancytopenia1,0203.5%

Literature

View JSON

Recent PubMed references pinned to Azacitidine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 1,264 ClinicalTrials.gov registrations naming Azacitidine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Azacitidine work?
Azacitidine for injection is a pyrimidine nucleoside analog of cytidine. Azacitidine for injection is believed to exert its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow.
What is Azacitidine used for?
According to FDA labeling, Azacitidine carries indications including: Azacitidine for injection is a nucleoside metabolic inhibitor indicated for the treatment of: Adult patients with the following FAB myelodysplastic syndrome (MDS) subtypes: Refractory anemia (RA) or refractory anemia with ringed sideroblasts (RARS) (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts (RAEB), refractory anemia with excess blasts in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL). ( 1.1) 1.1 Myelodysplastic Syndromes (MDS) Azacitidine for injection is indicated for treatment of adult patients with the following French-American- British (FAB) myelodysplastic syndrome subtypes: refractory anemia (RA) or refractory anemia with ringed sideroblasts (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts (RAEB), refractory anemia with excess blasts in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Azacitidine?
Azacitidine is classified as Pyrimidine analogues, Nucleoside Metabolic Inhibitor, DNA Methyltransferase Inhibitors, Nucleic Acid Synthesis Inhibitors, DNA Methylation Decrease.
What are the brand names for Azacitidine?
Azacitidine is marketed under brand names including Onureg, Vidaza.
What are the contraindications for Azacitidine?
Azacitidine labeling lists contraindications including: Advanced Malignant Hepatic Tumors ( 4.1 ) . Hypersensitivity to Azacitidine or Mannitol (4 .2 ) .. Always consult the full prescribing information and a clinician.
Note. Data for azacitidine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients