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Decitabine

Medically reviewed by Drugs.com. Last updated on Mar 22, 2020.

Pronunciation

(de SYE ta been)

Index Terms

  • 5-Aza-2'-deoxycytidine
  • 5-Aza-dCyd
  • Deoxyazacytidine
  • Dezocitidine

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Dacogen: 50 mg (1 ea)

Generic: 50 mg (1 ea)

Solution Reconstituted, Intravenous [preservative free]:

Generic: 50 mg (1 ea)

Brand Names: U.S.

  • Dacogen

Pharmacologic Category

  • Antineoplastic Agent, Antimetabolite
  • Antineoplastic Agent, DNA Methylation Inhibitor

Pharmacology

Decitabine is a hypomethylating agent. After phosphorylation, decitabine is incorporated into DNA and inhibits DNA methyltransferase causing hypomethylation and subsequent cell death (within the S-phase of the cell cycle).

Distribution

~63 to 89 L/m2 (Cashen 2008)

Metabolism

Possibly via deamination by cytidine deaminase

Half-Life Elimination

~0.5 to 0.6 hours

Use: Labeled Indications

Myelodysplastic syndromes: Treatment of myelodysplastic syndromes (MDS), including previously treated and untreated, de novo and secondary MDS of all French-American-British (FAB) subtypes (refractory anemia, refractory anemia with ringed sideroblasts, refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia) and intermediate-1, intermediate-2, and high-risk International Prognostic Scoring System (IPSS) groups

Off Label Uses

Acute myeloid leukemia

Data from a multicenter phase 2 study and a multicenter open-label phase 3 trial in patients ≥60 years of age support the use of decitabine for the treatment of newly diagnosed acute myeloid leukemia (AML) [Cashen 2010], [Kantarjian 2012]. Data from a large multicenter phase 1b study support the use of decitabine (in combination with venetoclax) for the treatment of newly diagnosed AML in patients ≥65 years of age, including those with poor-risk cytogenetics and TP53 mutations [DiNardo 2019]. Data from a single-institution uncontrolled study support the use of decitabine for the treatment of AML in patients with unfavorable-risk cytogenic profiles and/or TP53 mutations [Welch 2016].

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosing: Adult

Acute myeloid leukemia, newly diagnosed (off-label use): IV:

Adults ≥60 years of age: 20 mg/m2 over 1 hour once daily for 5 days every 28 days until relapse, disease progression, or unacceptable toxicity (Cashen 2010; Kantarjian 2012).

Adults ≥65 years of age: 20 mg/m2 once daily for 5 days every 28 days (in combination with venetoclax) until relapse, disease progression, or unacceptable toxicity (DiNardo 2018; DiNardo 2019).

Acute myeloid leukemia, with unfavorable-risk cytogenetics and/or TP53 mutation: 20 mg/m2 once daily for 10 days every 28 days for at least 2 cycles, although 3 or more cycles may be required (Welch 2016) or 20 mg/m2 once daily for 5 days every 28 days (in combination with venetoclax) until relapse, disease progression, or unacceptable toxicity (DiNardo 2018; DiNardo 2019).

Myelodysplastic syndromes: IV:

3-day regimen: 15 mg/m2 over 3 hours every 8 hours (45 mg/m2/day) for 3 days (Kantarjian 2006); repeat every 6 weeks upon hematologic recovery (ANC ≥1,000/mm3 and platelets ≥50,000/mm3); treatment is recommended for a minimum of 4 cycles (complete or partial response may take longer than 4 cycles).

5-day regimen: 20 mg/m2 over 1 hour once daily for 5 days (Steensma 2009); repeat every 4 weeks upon hematologic recovery (ANC ≥1,000/mm3 and platelets ≥50,000/mm3); treatment is recommended for a minimum of 4 cycles (complete or partial response may take longer than 4 cycles).

Higher-risk myelodysplastic syndromes (CMML subtype): 20 mg/m2 once daily for 5 days every 4 weeks; patients were assessed after 4 cycles, responders continued for an additional 2 cycles; patients who completed 6 cycles could continue with maintenance decitabine (Santini 2018). Refer to protocol for additional details.

Lower-risk myelodysplastic syndromes (off-label dosing): 20 mg/m2 over 1 hour once daily for 3 days; repeat every 4 weeks when possible; continue until disease progression or unacceptable toxicity (Jabbour 2017). Refer to protocol for dosage adjustment details.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Adjustment for Toxicity

Myelodysplastic syndromes: IV:

Hematologic toxicity: ANC <1,000/mm3 and platelets <50,000/mm3: Delay subsequent decitabine treatment cycles until hematologic recovery to ANC ≥1,000/mm3 and platelets ≥50,000/mm3.

3-day regimen: Hematologic toxicity lasting >6 weeks: Delay the next decitabine cycle and reduce the next dose as follows:

Hematologic toxicity lasting >6 weeks but <8 weeks: Delay decitabine dose for up to 2 weeks and upon re-initiation, temporarily reduce decitabine dose to 11 mg/m2 every 8 hours (33 mg/m2/day) for 3 days (99 mg/m2/cycle).

Hematologic toxicity lasting >8 weeks but <10 weeks: Assess bone marrow for disease progression; in the absence of disease progression, delay decitabine dose for up to 2 more weeks and reduce decitabine dose to 11 mg/m2 every 8 hours (33 mg/m2/day) for 3 days (99 mg/m2/cycle); maintain or increase decitabine dose with subsequent cycles if clinically indicated.

Nonhematologic toxicity:

Active or uncontrolled infection: Temporarily withhold decitabine; do not resume decitabine until after resolution.

Reconstitution

IV: Reconstitute vial with 10 mL of room temperature SWFI to a concentration of 5 mg/mL. Further dilute for infusion. If product will be administered within 15 minutes, dilute with room temperature (20°C to 25°C [68°F to 77°F]) NS or D5W to a final concentration of 0.1 to 1 mg/mL. If administration will be delayed >15 minutes, dilute with cold (2°C to 8°C [36°F to 46°F]) NS or D5W to a final concentration of 0.1 to 1 mg/mL.

Administration

IV: Infuse over 1 to 3 hours (depending on dosing regimen). For the treatment of myelodysplastic syndromes, infuse over 3 hours (15 mg/m2 dose) or over 1 hour (20 mg/m2 dose). Premedication with antiemetics is recommended (according to the manufacturer). For the treatment of acute myeloid leukemia (off-label use), decitabine has been infused over 1 hour (Cashen 2010; Kantarjian 2012).

SubQ (off-label route): Subcutaneous administration of the 5-day decitabine regimen has been reported in a limited number of patients with higher-risk myelodysplastic syndromes; however, the complete response rate was lower in the subcutaneous arm compared to the 5-day regimen administered IV (Kantarjian 2007a; Kantarjian 2007b). Other schedules of subcutaneous decitabine have been reported in a small study in patients with low- or intermediate-risk myelodysplastic syndromes (Garcia-Manero 2013). Multiple subcutaneous injections may be required to administer a single dose (depending on institutional subcutaneous volume policy).

Storage

Store intact vials at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Solutions diluted for infusion in NS or D5W may be stored for up to 4 hours prior to infusion refrigerated at 2°C to 8°C (36°F to 46°F) if prepared with cold infusion fluids. Infusion should begin within 15 minutes of preparation if room temperature infusion solutions are utilized.

Drug Interactions

BCG (Intravesical): Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Cedazuridine: May increase the serum concentration of Cytidine Deaminase Substrates. Avoid combination

Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. Monitor therapy

Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Avoid combination

CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. Monitor therapy

Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Consider therapy modification

Dipyrone: May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased Avoid combination

Lenograstim: Antineoplastic Agents may diminish the therapeutic effect of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Consider therapy modification

Lipegfilgrastim: Antineoplastic Agents may diminish the therapeutic effect of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Consider therapy modification

Mesalamine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Monitor therapy

Palifermin: May enhance the adverse/toxic effect of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy. Consider therapy modification

Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Monitor therapy

Adverse Reactions

>10%:

Cardiovascular: Edema (5% to 18%), heart murmur (16%), hypotension (6% to 11%), peripheral edema (25% to 27%)

Dermatologic: Cellulitis (9% to 12%), ecchymoses (9% to 22%), erythema of skin (5% to 14%), pallor (23%), pruritus (9% to 11%), skin lesion (5% to 11%), skin rash (11% to 19%)

Endocrine & metabolic: Hyperglycemia (6% to 33%), hyperkalemia (13%), hypoalbuminemia (24%), hypokalemia (12% to 22%), hypomagnesemia (5% to 24%), hyponatremia (19%)

Gastrointestinal: Abdominal pain (14%), anorexia (16% to 23%), constipation (30% to 35%), decreased appetite (8% to 16%), diarrhea (28% to 34%), dyspepsia (10% to 12%), nausea (40% to 42%), stomatitis (11% to 12%), vomiting (16% to 25%)

Hematologic & oncologic: Anemia (31% to 82%), febrile neutropenia (20% to 29%; grades 3/4: 23%), leukopenia (6% to 28%), lymphadenopathy (12%), neutropenia (38% to 90%; grades 3/4: 87%), oral mucosal petechiae (13%), petechia (12% to 39%), thrombocytopenia (27% to 89%; grades 3/4: 85%)

Hepatic: Hyperbilirubinemia (14%), increased serum alkaline phosphatase (11%)

Local: Localized tenderness (11%)

Nervous system: Anxiety (9% to 11%), chills (16%), confusion (8% to 12%), dizziness (18% to 21%), fatigue (46%), headache (23% to 28%), hypoesthesia (11%), insomnia (14% to 28%), lethargy (12%), pain (5% to 13%), rigors (22%)

Neuromuscular & skeletal: Arthralgia (17% to 20%), asthenia (15%), back pain (17% to 18%), limb pain (18% to 19%)

Respiratory: Cough (27% to 40%), dyspnea (29%), epistaxis (13%), pharyngitis (16%), pneumonia (20% to 22%), rales (8% to 14%)

Miscellaneous: Fever (6% to 53%)

1% to 10%:

Cardiovascular: Acute cardiorespiratory failure (<5%), acute myocardial infarction (<5%), atrial fibrillation (<5%), cardiac failure (5%), cardiomyopathy (<5%), chest discomfort (7%), chest pain (≤6%), chest wall pain (7%), hypertension (6%), pulmonary embolism (<5%), supraventricular tachycardia (<5%), tachycardia (8%)

Dermatologic: Alopecia (8%), catheter-site erythema (5%), excoriation of skin (5%), facial swelling (6%), night sweats (5%), urticaria (6%), xeroderma (8%)

Endocrine & metabolic: Decreased serum bicarbonate (5%), decreased serum total protein (5%), dehydration (6% to 8%), hypochloremia (6%), increased lactate dehydrogenase (8%), increased serum bicarbonate (6%), weight loss (9%)

Gastrointestinal: Abdominal distention (5%), cholecystitis (<5%), dysphagia (5% to 6%), gastroesophageal reflux disease (5%), gingival hemorrhage (8%), gingival pain (<5%), glossalgia (5%), hemorrhoids (8%), loose stools (7%), mucosal swelling (9%), oral candidiasis (6%), oral changes (soft tissue: 6%), oral mucosa ulcer (lip: 5%), tongue ulcer (7%), toothache (6%), upper abdominal pain (5% to 6%)

Genitourinary: Dysuria (6%), urethral bleeding (<5%), urinary frequency (5%), urinary tract infection (7%)

Hematologic & oncologic: Bone marrow depression (<5%), hematoma (5%), pancytopenia (5%), postprocedural hemorrhage (<5%), splenomegaly (<5%), thrombocythemia (5%), upper gastrointestinal hemorrhage (<5%)

Hepatic: Ascites (10%), decreased serum bilirubin (5%), increased serum aspartate aminotransferase (10%)

Hypersensitivity: Anaphylaxis (<5%), hypersensitivity reaction (<5%), transfusion reaction (7%)

Infection: Abscess (peridiverticular, <5%), bacteremia (5%), candidiasis (10%), fungal infection (<5%), sepsis (<5%), staphylococcal bacteremia (8%), staphylococcal infection (7%), tooth abscess (5%)

Local: Catheter infection (8%), catheter pain (5%), catheter site hemorrhage (<5%), swelling at injection site (5%)

Nervous system: Depression (9%), falling (8%), intracranial hemorrhage (<5%), malaise (5%), mental status changes (<5%), mouth pain (5%), myasthenia (5%)

Neuromuscular & skeletal: Muscle spasm (7%), musculoskeletal pain (≤6%; includes discomfort), myalgia (5% to 9%), ostealgia (6%)

Ophthalmic: Blurred vision (6%)

Otic: Otalgia (6%)

Renal: Acute renal failure (<5%), increased blood urea nitrogen (10%)

Respiratory: Abnormal breath sounds (5% to 10%), hemoptysis (<5%), hypoxia (10%), mycobacterium avium complex (<5%), paranasal sinus congestion (5%), pharyngolaryngeal pain (8%), pleural effusion (5%), post nasal drip (5%), pulmonary aspergillosis (<5%), pulmonary edema (6%), pulmonary infection (pseudomonas: <5%), pulmonary infiltrates (<5%), pulmonary signs and symptoms (crepitations: 5%), respiratory tract infection (<5%), sinusitis (5% to 6%), upper respiratory tract infection (10%)

Miscellaneous: Mass (pulmonary, <5%), postoperative pain (<5%)

Frequency not defined: Hepatic: Abnormal hepatic function tests

Postmarketing:

Dermatologic: Sweet’s syndrome (acute febrile neutrophilic dermatosis)

Hematologic & oncologic: Differentiation syndrome

Warnings/Precautions

Concerns related to adverse effects:

• Bone marrow suppression: Myelosuppression (neutropenia, thrombocytopenia, and anemia) commonly occurs with decitabine, including Grades 3 and 4 neutropenia, thrombocytopenia, and neutropenic fever; may be serious or fatal. Monitor blood counts (including platelets) at baseline, prior to each cycle, and as needed to monitor response and for toxicity. Myelosuppression and worsening neutropenia are more common in first two treatment cycles and may not correlate with progression of underlying myelodysplastic syndromes. Hematologic toxicity may require dose reduction, treatment delay, discontinuation, growth factor support, and/or antimicrobial agents. Monitor for infection.

• Hepatitis B reactivation: The American Society of Clinical Oncology hepatitis B screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends hepatitis B virus (HBV) screening with hepatitis B surface antigen (HBsAg), hepatitis B core antibody (anti-HBc), total Ig or IgG, and antibody to hepatitis B surface antigen (anti-HBs) prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow up.

Monitoring Parameters

Monitor CBC with differential and platelets (prior to treatment and with each cycle; more frequently if needed); liver enzymes (prior to treatment initiation and periodically); serum creatinine (prior to treatment initiation and periodically). Hepatitis B virus screening with hepatitis B surface antigen (HBsAg), hepatitis B core antibody (anti-HBc), total Ig or IgG, and antibody to hepatitis B surface antigen (anti-HBs) prior to beginning systemic anticancer therapy (ASCO [Hwang 2020]). Evaluate pregnancy status prior to treatment in females of reproductive potential. Monitor for signs/symptoms of infection.

Reproductive Considerations

Evaluate pregnancy status prior to therapy. Females of reproductive potential should use effective contraception during treatment and for 6 months after the last decitabine dose. Males with female partners of reproductive potential should use effective contraception during treatment and for 3 months after the last decitabine dose.

Pregnancy Considerations

Based on the mechanism of action and information from animal reproduction studies, decitabine may cause fetal harm if exposure occurs during pregnancy. Information related to the use of decitabine in pregnancy is limited.

Patient Education

What is this drug used for?

• It is used to treat a health problem called myelodysplastic syndrome (MDS).

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Abdominal pain

• Nausea

• Vomiting

• Heartburn

• Loss of strength and energy

• Fatigue

• Mouth irritation

• Mouth sores

• Night sweats

• Weight loss

• Injection site irritation

• Muscle spasms

• Painful extremities

• Constipation

• Diarrhea

• Trouble sleeping

• Lack of appetite

• Itching

• Bone pain

• Muscle pain

• Joint pain

• Anxiety

• Hair loss

• Back pain

• Weight loss

• Night sweats

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Infection

• Bleeding like vomiting blood or vomit that looks like coffee grounds; coughing up blood; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any severe bleeding or persistent bleeding.

• Pinpoint red spots on skin

• High blood sugar like confusion, fatigue, more thirst, hunger, passing a lot of urine, flushing, fast breathing, or breath that smells like fruit.

• Fluid and electrolyte problems like mood changes, confusion, muscle pain or weakness, abnormal heartbeat, severe dizziness or passing out, fast heartbeat, more thirst, seizures, loss of strength and energy, lack of appetite, unable to pass urine or change in amount of urine produced, dry mouth, dry eyes, or nausea or vomiting.

• Severe headache

• Dizziness

• Passing out

• Vision changes

• Pale skin

• Red spots on skin

• Yellow skin or eyes

• Swollen glands

• Shortness of breath

• Swelling

• Blurred vision

• Trouble swallowing

• Chest pain

• Fast heartbeat

• Numbness and tingling

• Depression

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.