Azacitidine 100 mg Injection, Powder, Lyophilized, For Solution, 1 injection
Past resolved recalls for this product (1)
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Nucleoside Metabolic Inhibitor class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Azacitidine is used to treat myelodysplastic syndrome (a group of conditions in which the bone marrow produces blood cells that are misshapen and does not produce enough healthy blood cells). Azacitidine is in a class of medications called demethylation agents. It works by helping the bone marrow to produce normal blood cells and by killing abnormal cells in the bone marrow.
Read the full MedlinePlus article ↗- Yes, azacitidine is a type of cancer treatment, though it works a bit differently from traditional chemotherapy. Instead of just killing cancer cells outright, it also reprograms h...
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- They contain the same active ingredient, but you absolutely cannot swap one for the other. Onureg tablets and the injectable forms are approved for completely different conditions,...
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Supplement & herbal interactions
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII 94255I6E2T
Sodium phosphate dibasic dihydrate is a salt that helps control the acidity level of a medicine. It acts as a buffer and pH regulator to keep the medication stable and effective.
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UNII 593YOG76RN
A salt made from sodium and phosphate that helps regulate acidity and maintain proper pH balance in the medicine. It also acts as a buffer to keep the product stable.
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UNII C151H8M554
A natural sugar derived from sugar cane or sugar beets. It's used as a sweetener, filler, and binder to improve taste, add bulk, and help hold tablet or capsule ingredients together.
3 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | $52.79 | — |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
| Medicare Part B allowsASP · J9025 | $0.401 / J9025 unit | — |
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🧾 Billing & reimbursement
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Azacitidine 100 mg 00143-9606-01 | Hikma | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mg 00781-3491-94 | Sandoz | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 16714-0927-01 | NorthStar | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 16729-0306-10 | Accord | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 31722-0365-31 | Camber | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 43598-0305-62 | Dr. | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 43598-0465-62 | Dr. | 1 injection | — | AP | FDA listed | — |
| Azacitidine Azacitidine 100 mg 43598-0678-11 | Dr. | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg/50mL 43817-0906-01 | Panacea | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mg/4mL 55150-0393-01 | Eugia | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mg 58458-0002-02 | Reliance | 1 vial | — | AP | FDA listed | — |
| Vidaza 100 mg 59572-0102-01 | Celgene | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 60505-6271-01 | Apotex | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg/30mL 63323-0771-39 | Fresenius | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mgthis 68001-0313-56 | BluePoint | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 68001-0527-54 | BluePoint | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 68001-0620-54 | BluePoint | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 69539-0112-01 | MSN | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 70069-0857-01 | Somerset | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mg 70121-1237-01 | Amneal | 1 injection | — | — | FDA listed | — |
| Azacitidine 100 mg 71288-0115-30 | Meitheal | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mg 71288-0153-95 | Meitheal | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mg 72485-0201-01 | Armas | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 72572-0020-01 | Civica, | 1 injection | — | AP | FDA listed | — |
| Azacitidine 100 mg 75907-0225-11 | Dr. | 1 vial | — | AP | FDA listed | — |
| Azacitidine 100 mg 83774-0102-01 | Pilnova | 1 injection | — | AP | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
The FDA lists approved generic versions of this medicine, but that does not always mean a pharmacy can get one today. Patent rules, launch agreements, supply and pricing can affect when generics actually arrive.
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 68001-0313-56 You're viewing this | 1 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION in 1 CARTON (68001-313-56) | 2017-07-01 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | ✓ Available |
| Medicaid utilization (CMS SDUD) | ✓ Available |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE 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 ).
1.1Myelodysplastic 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). 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.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION 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 ). The recommended starting dosage for the first treatment cycle, for all patients regardless of baseline hematology values, is Azacitidine for Injection 75 mg/m2 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 ( 2.4 , 2.5 , 2.6 ).
2.1Important 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) ] .
2.2First 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.
2.3Subsequent Treatment Cycles for Adults Repeat cycles every 4 weeks. The dose may be increased to 100 mg/m 2 if no beneficial effect is seen after 2 treatment cycles and if no toxicity other than nausea and vomiting has occurred. It is recommended that patients be treated for a minimum of 4 to 6 cycles.
However, complete or partial response may require additional treatment cycles. Treatment may be continued as long as the patient continues to benefit. Monitor patients for hematologic response and renal toxicities [ see Warnings and Precautions (5.4) ] and delay or reduce dosage if necessary as described below.
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.
2.4Dosage Adjustment Based on Hematology Laboratory Values For adult patients with baseline (start of treatment) WBC greater than or equal to 3 x10 9 /L, ANC greater than or equal to 1.5 x10 9 /L, and platelets greater than or equal to 75 x10 9 /L, adjust the dose as follows, based on nadir counts for any given cycle: Nadir Counts % Dose in the Next Course ANC (x10 9 /L) Less than 0.5 0.5 to
1.5 Greater than
1.5Platelets (x10 9 /L) Less than 25 25 to 50 Greater than 50 50% 67% 100% For adult patients whose baseline counts are WBC less than 3 x10 9 /L, ANC less than 1.5 x10 9 /L, or platelets less than 75 x10 9 /L, base dose adjustments on nadir counts and bone marrow biopsy cellularity at the time of the nadir as noted below, unless there is clear improvement in differentiation (percentage of mature granulocytes is higher and ANC is higher than at onset of that course) at the time of the next cycle, in which case continue the current dose.
WBC or Platelet Nadir % decrease in counts from baseline Bone Marrow Biopsy Cellularity at Time of Nadir (%) 30 to 60 15 to 30 Less than 15 50 to 75 Greater than 75 % Dose in the Next Course 100 50 33 75 50 33 If a nadir as defined in the table above has occurred, give the next course 28 days after the start of the preceding course, provided that both the WBC and the platelet counts are greater than 25% above the nadir and rising. If a greater than 25% increase above the nadir is not seen by day 28, reassess counts every 7 days.
If a 25% increase is not seen by day 42, reduce the scheduled dose by 50%. 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…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS For injection: 100 mg as a lyophilized powder in single-dose vial for reconstitution. For Injection: 100 mg as a lyophilized powder in single-dose vial for reconstitution ( 3 ).
⛔ Contraindications ▾
4 CONTRAINDICATIONS Azacitidine for Injection is contraindicated in patients with advanced malignant hepatic tumors [ see Warnings and Precautions (5.3) ]. a known hypersensitivity to azacitidine. Advanced malignant hepatic tumors ( 4 ). Hypersensitivity to azacitidine ( 4 ).
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS 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 : Can cause fetal harm. Advise patients of reproductive potential of the potential risk to a fetus and to use effective contraception ( 5.6 , 8.1 , 8.3 ).
5.1Risks 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) ].
5.2Anemia, Neutropenia and Thrombocytopenia Azacitidine for Injection causes anemia, neutropenia and thrombocytopenia. Monitor complete blood counts frequently for response and/or toxicity, at a minimum, prior to each dosing cycle. After administration of the recommended dosage for the first cycle, adjust dosage for subsequent cycles based on nadir counts and hematologic response [ see Dosage and Administration (2.4) ] .
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.
5.3Hepatic Toxicity in Patients with Severe Pre-existing Hepatic Impairment Because Azacitidine for Injection is potentially hepatotoxic in patients with severe pre-existing hepatic impairment, caution is needed in patients with liver disease. Patients with extensive tumor burden due to metastatic disease have been reported to experience progressive hepatic coma and death during azacitidine treatment, especially in such patients with baseline albumin less than 30 g/L. Azacitidine for Injection is contraindicated in patients with advanced malignant hepatic tumors [ see Contraindications (4) ] .
Monitor liver chemistries prior to initiation of therapy and with each cycle. Safety and effectiveness of Azacitidine for Injection in patients with MDS and hepatic impairment have not been studied as these patients were excluded from the clinical trials. 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.
5.4Renal Toxicity Renal toxicity ranging from elevated serum creatinine to renal failure and death have been reported in patients treated with intravenous azacitidine in combination with other chemotherapeutic agents for non-MDS conditions. In addition, renal tubular acidosis, defined as a fall in serum bicarbonate to less than 20 mEq/L in association with an alkaline urine and hypokalemia (serum potassium less than 3 mEq/L) developed in 5 patients with CML (an unapproved use) treated with azacitidine and etoposide.
Monitor serum creatinine and electrolytes prior to initiation of therapy and with each cycle. If unexplained reductions in serum bicarbonate less than 20 mEq/L or elevations of BUN or serum creat…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in labeling: 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 Actavis at 1-888-838-2872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience 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. The data described below reflect exposure to azacitidine in 443 MDS patients from 4 clinical studies. Study 1 was a supportive-care controlled trial (subcutaneous administration), Studies 2 and 3 were single arm studies (one with subcutaneous administration and one with intravenous administration), and Study 4 was an international randomized trial (subcutaneous administration) [ see Clinical Studies (14) ] .
In Studies 1, 2 and 3, a total of 268 patients were exposed to azacitidine, including 116 exposed for 6 cycles (approximately 6 months) or more and 60 exposed for greater than 12 cycles (approximately one year). Azacitidine was studied primarily in supportive-care controlled and uncontrolled trials (n=150 and n=118, respectively). The population in the subcutaneous studies (n=220) was 23 to 92 years old (mean 66.4 years), 68% male, and 94% white, and had MDS or AML.
The population in the intravenous study (n=48) was 35 to 81 years old (mean 63.1 years), 65% male, and 100% white. Most patients received average daily doses between 50 and 100 mg/m 2 . In Study 4, a total of 175 patients with higher-risk MDS (primarily RAEB and RAEB-T subtypes) were exposed to azacitidine.
Of these patients, 119 were exposed for 6 or more cycles, and 63 for at least 12 cycles. The mean age of this population was 68.1 years (ranging from 42 to 83 years), 74% were male, and 99% were white. Most patients received daily azacitidine doses of 75 mg/m 2 .
Most Commonly Occurring Adverse Reactions (Subcutaneous or Intravenous Route) in Adult Patients with MDS : nausea, anemia, thrombocytopenia, vomiting, pyrexia, leukopenia, diarrhea, injection site erythema, constipation, neutropenia, ecchymosis. The most common adverse reactions by intravenous route also included petechiae, rigors, weakness and hypokalemia. Adverse Reactions Most Frequently (Greater Than 2%) Resulting in Clinical Intervention (Subcutaneous or Intravenous Route) in Adult Patients with MDS : Discontinuation : leukopenia, thrombocytopenia, neutropenia.
Dose Held : leukopenia, neutropenia, thrombocytopenia, pyrexia, pneumonia, febrile neutropenia. Dose Reduced : leukopenia, neutropenia, thrombocytopenia. Table 1 presents adverse reactions occurring in at least 5% of patients treated with azacitidine (subcutaneous) in Studies 1 and 2.
It is important to note that duration of exposure was longer for the azacitidine-treated group than for the observation group; patients received azacitidine for a mean of 11.4 months while mean time in the observation arm was 6.1 months. Table 1: Most Frequently Observed Adverse Reactions (Greater Than or Equal To 5% in All Subcutaneous Azacitidine-Treated Patients; Studies 1 and 2) Number (%) of Patients Body System Adverse Reaction a All Azacitidine b Observation c (N=220) (N=92) a Multiple t…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS 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 .
8.1Pregnancy 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 estimated background risk of major birth defects and miscarriage in the indicated population is unknown. 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% to 4% and 15% to 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. Developmental abnormalities in the brain have been detected in mice given azacitidine on or before gestation day 15 at doses of ~3 to 12 mg/m 2 (approximately 4% to 16% the recommended human daily dose on a mg/m 2 basis).
In rats, azacitidine was clearly embryotoxic when given IP on gestation days 4 to 8 (postimplantation) at a dose of 6 mg/m 2 (approximately 8% of the recommended human daily dose on a mg/m 2 basis), although treatment in the preimplantation period (on gestation days 1 to 3) had no adverse effect on the embryos. Azacitidine caused multiple fetal abnormalities in rats after a single IP dose of 3 to 12 mg/m 2 (approximately 8% the recommended human daily dose on a mg/m 2 basis) given on gestation day 9, 10, 11 or 12. In this study azacitidine caused fetal death when administered at 3 to 12 mg/m 2 on gestation days 9 and 10; average live animals per litter was reduced to 9% of control at the highest dose on gestation day 9.
Fetal anomalies included: CNS anomalies (exencephaly/encephalocele), limb anomalies (micromelia, club foot, syndactyly, oligodactyly), and others (micrognathia, gastroschisis, edema, and rib abnormalities).
8.2Lactation Risk Summary There is no information on the presence of azacitidine or its metabolites in human milk, the effects on a breast-fed child, or the effects on milk production. Because many drugs are excreted in human milk and because of the potential for tumorigenicity shown for azacitidine in animal studies [ see Nonclinical Toxicology (13.1) ] and the potential for serious adverse reactions in a breastfeed child, advise women not to breastfeed during treatment with Azacitidine for Injection and for 1 week after the last dose.
8.3Females and Males of Reproductive Potential Based on its mechanism of action and findings in animals, Azacitidine for Injection can cause fetal harm when administered to a pregnant woman [ see Use in Specific Populations (8.1) ] . Pregnancy Testing Verify the pregnancy status of females of reproductive potential prior to initiating Azacitidine for Injection. Contraception Females Advise females of reproductive potential to use effective contraception during treatment with Azacitidine for Injection and for 6 months after the last dose [ see Use in Specific Populations (8.1) and Clinical Pharmacology (12.3) ] .
Males Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective contraception during treatment with Azacitidine for Injection and for 3 months after the last dose [ see Nonclinical T…
🆘 Overdosage ▾
10 OVERDOSAGE One case of overdose with azacitidine 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.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Azacitidine is a pyrimidine nucleoside analog of cytidine. Azacitidine is believed to exert its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow. The concentration of azacitidine required for maximum inhibition of DNA methylation in vitro does not cause major suppression of DNA synthesis.
Hypomethylation may restore normal function to genes that are critical for differentiation and proliferation. The cytotoxic effects of azacitidine cause the death of rapidly dividing cells, including cancer cells that are no longer responsive to normal growth control mechanisms. Non-proliferating cells are relatively insensitive to azacitidine.
12.2Pharmacodynamics 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.
12.3Pharmacokinetics The area under the curve (AUC) and peak concentration (C max ) of subcutaneous administration of azacitidine in patients with cancer were approximately dose proportional within the dose range of 25 mg/m 2 (0.33 times the lowest approved recommended dosage) to 100 mg/m 2 (the maximum approved recommended dosage). The mean and standard deviation (SD) of C max was 750 ± 403 ng/mL after a single subcutaneous administration of 75 mg/m 2 azacitidine. Multiple dosing at the recommended dose-regimen does not result in drug accumulation.
Absorption Azacitidine is rapidly absorbed after subcutaneous administration with a median time to C max (T max ) of 0.5 hour. The bioavailability of subcutaneous azacitidine relative to intravenous azacitidine is approximately 89%, based on AUC. Distribution Mean volume of distribution following intravenous dosing is 76 ± 26 L.
Elimination Mean apparent subcutaneous clearance is 167 ± 49 L/hour and mean half-life after subcutaneous administration is 41 ± 8 minutes. Excretion Published studies indicate that urinary excretion is the primary route of elimination of azacitidine and its metabolites. Following intravenous administration of radioactive azacitidine to 5 cancer patients, the cumulative urinary excretion was 85% of the radioactive dose.
Fecal excretion accounted for less than 1% of administered radioactivity over 3 days. Mean excretion of radioactivity in urine following subcutaneous administration of 14 C-azacitidine was 50%. The mean elimination half-lives of total radioactivity (azacitidine and its metabolites) were similar after intravenous and subcutaneous administrations, about 4 hours.
Specific Populations The effects of hepatic impairment, gender, or race/ethnicity on the pharmacokinetics of intravenous and subcutaneous azacitidine have not been studied. Pediatric Patients 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.
Patients with Renal Impairment In adult patients with cancer, the pharmacokinetics of azacitidine in 6 patients with normal renal function (CLcr >80 mL/min) and 6 patients with severe renal impairment (CLcr <30 mL/min) were compared following daily subcutaneous dosing (Days 1 through 5) at 75 mg/m 2 /day. Severe renal impairment increased azacitidine exposure by approximately 70% after single and 41% after multiple subcutaneous administrations.). This increase in exposure was not correlated with an increase in adverse events.
The exposure was similar to exposure in patients with normal renal function receiving 100 mg/m 2 . Drug Interaction Studies No formal clinical drug interaction studies with azacitidine have been conducted. In vitro Studies Cytochrome P450 (CYP) Enzymes: An in vitro study at azacitidine concentrations up to 100 μM (IV C max = 10.6 μM) in human liver microsom…
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied Azacitidine for Injection is supplied as 100 mg of lyophilized powder in single-dose vials packaged in cartons of 1 vial (NDC 68001-313-56). Storage Store unreconstituted vials at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Discard unused portion.
Handling and Disposal Azacitidine for Injection is a hazardous drug. Follow applicable special handling and disposal procedures. 1 Sterile, Nonpyrogenic, Preservative-free.
This vial stopper is not made with natural rubber latex.
📋 Description ▾
11 DESCRIPTION Azacitidine is a nucleoside metabolic inhibitor. The molecular formula is C 8 H 12 N 4 O 5 . The molecular weight is 244.
Azacitidine is 4-amino-1-β-D-ribofuranosyl-s-triazin-2(1H)-one. The structural formula is as follows: Azacitidine is a white to almost white powder. Azacitidine was found to be insoluble in acetone, ethanol, and methyl ethyl ketone; slightly soluble in ethanol/water (50/50), propylene glycol, and polyethylene glycol; sparingly soluble in water, water saturated octanol, 5% dextrose in water, N-methyl-2-pyrrolidone, normal saline and 5% Tween 80 in water; and soluble in dimethylsulfoxide (DMSO).
Azacitidine for Injection is supplied in a sterile form for reconstitution as a suspension for subcutaneous injection or reconstitution as a solution with further dilution for intravenous infusion. Each vial of Azacitidine for Injection contains 100 mg of azacitidine, 170 mg sucrose, monosodium phosphate monohydrate and disodium hydrogen phosphate, dihydrate as a sterile lyophilized powder. 9dca4f01-figure-01
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Hepatic Toxicity in Patients with Severe Pre-Existing Hepatic Impairment Instruct patients to inform their healthcare provider about any underlying liver disease [ see Warnings and Precautions (5.3) ]. Renal Toxicity Instruct patients to inform their healthcare provider about any underlying renal disease [ see Warnings and Precautions (5.4) ]. Embryo-Fetal Toxicity Advise pregnant women and females of reproductive potential of the potential risk to a fetus.
Advise females of reproductive potential to inform their healthcare provider of a known or suspected pregnancy [ see Warnings and Precautions (5.6) and Use in Specific Populations (8.1) ] . Advise females of reproductive potential to use effective contraception during treatment with Azacitidine for Injection and for 6 months after the last dose [ see Use in Specific Populations (8.3) ]. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with Azacitidine for Injection and for 3 months after the last dose [ see Use in Specific Populations (8.3) ] .
Lactation Advise women not to breastfeed during treatment with Azacitidine for Injection and for 1 week after the last dose [ see Use in Specific Populations (8.2) ]. Infertility Advise males and females of the potential for reduced fertility from Azacitidine for Injection [ see Use in Specific Populations (8.3) and Nonclinical Toxicology (13.1) ]. Manufactured In Romania By: Sindan Pharma SRL 11 Ion Mihalache Blvd.
Bucharest 1, Romania 011171 For BluePoint Laboratories Rev. E 12/2024