AZACITIDINE

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.

AbsorptionAzacitidine is rapidly absorbed after subcutaneous administration; the peak plasma azacitidine concentration of 750 ± 403 ng/ml occurred in 0.5 hour after subcutaneous administration.

DistributionThe bioavailability of subcutaneous azacitidine relative to intravenous azacitidine is approximately 89%, based on area under ...

14.1 Myelodysplastic Syndromes (MDS) Study 1 was a randomized, open-label, controlled trial carried out in 53 U.S. sites compared the safety and efficacy of subcutaneous Azacitidine plus supportive care with supportive care alone ("observation") in adult patients with any of the five FAB subtypes of myelodysplastic syndromes (MDS): refractory anemia (RA), RA with ringed sideroblasts (RARS), RA with excess blasts (RAEB), RAEB in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL). RA and RARS patients were included if they met one or more of the following criteria: required pac...

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 Shilpa Medicare Limited 1-888-557-1212 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. The following...

Advanced Malignant Hepatic Tumors ( 4.1 ). Hypersensitivity to Azacitidine or Mannitol ( 4.2 ). 4.1 Advanced Malignant Hepatic Tumors Azacitidine is contraindicated in patients with advanced malignant hepatic tumors [see Warnings and Precautions (5.3) ]. 4.2 Hypersensitivity to Azacitidine or Mannitol Azacitidine is contraindicated in patients with a known hypersensitivity to azacitidine or manni...

Risks of Substitution with Other Azacitidine Products : Do not substitute Azacitidine 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 Syn...