DACOGEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DACOGEN (DACOGEN).
Decitabine is a hypomethylating agent that incorporates into DNA and inhibits DNA methyltransferase, resulting in hypomethylation of DNA and subsequent gene reactivation.
| Metabolism | Primarily metabolized by deamination by cytidine deaminase in the liver and extrahepatic tissues; not significantly metabolized by CYP450 enzymes. |
| Excretion | Renal excretion of unchanged drug and metabolites: approximately 90% of total clearance. Biliary/fecal excretion: <10%. |
| Half-life | Terminal elimination half-life: approximately 1.5 hours at steady state. Short half-life necessitates daily administration in current regimens. |
| Protein binding | Plasma protein binding: 92-96% (primarily albumin). |
| Volume of Distribution | Volume of distribution: approximately 22 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Intravenous: 100%. Oral (not clinically used): approximately 10-20% due to first-pass metabolism. |
| Onset of Action | Intravenous: clinical response may be observed after 1-2 cycles (each cycle 5 days every 4 weeks). Oral (not approved): not applicable. |
| Duration of Action | Duration varies: epigenetic effects persist beyond drug presence, but re-dosing required every cycle; single dose effect lasts hours to days. |
| Action Class | Antimetabolites |
| Brand Substitutes | Deczuba 50mg Injection, Mylodec 50mg Injection, Decintas 50 Injection, Decitas Injection, Decita Injection |
15 mg/m² intravenously over 3 hours every 8 hours for 3 consecutive days, repeated every 6 weeks for a minimum of 4 cycles.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-49 mL/min: No data; use with caution. GFR <30 mL/min: Not recommended. |
| Liver impairment | Child-Pugh Class B or C: No data; use with caution. |
| Pediatric use | Safety and efficacy not established; no standard dosing. |
| Geriatric use | No specific dose adjustment recommended; monitor for increased toxicity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DACOGEN (DACOGEN).
| Breastfeeding | No data on DACOGEN excretion in human milk. However, due to potential for serious adverse reactions (myelosuppression, carcinogenesis) in the breastfed infant, breastfeeding is contraindicated during treatment and for at least 2 weeks after the last dose. M/P ratio unknown. |
| Teratogenic Risk | DACOGEN (decitabine) is contraindicated in pregnancy. Based on its mechanism of action and animal studies, it is teratogenic across all trimesters. In first trimester, high risk of embryolethality and major malformations (neural tube defects, skeletal anomalies). Second and third trimester exposure may cause fetal growth restriction, myelosuppression, and developmental delay. Effective contraception must be used during treatment and for at least 6 months after the last dose. |
■ FDA Black Box Warning
WARNING: Myelosuppression. DACOGEN can cause severe myelosuppression, including neutropenia, thrombocytopenia, and anemia. Monitor complete blood counts and provide supportive care as needed.
| Serious Effects |
["Hypersensitivity to decitabine or any component of the formulation."]
| Precautions | ["Myelosuppression: Monitor blood counts regularly.","Hepatotoxicity: Elevated liver enzymes have been reported; monitor hepatic function.","Pulmonary toxicity: Rare cases of interstitial lung disease and acute respiratory distress syndrome.","Embryo-fetal toxicity: Can cause fetal harm; advise females of reproductive potential to use effective contraception.","Tumor lysis syndrome: Monitor patients at risk."] |
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| Fetal Monitoring | If inadvertent exposure occurs during pregnancy, perform serial fetal ultrasound (anatomy scan, growth) and consider amniocentesis for karyotype if structural anomalies found. Monitor maternal complete blood counts (CBC) every 1-2 weeks due to myelosuppression risk. Assess liver and renal function prior to each cycle. |
| Fertility Effects | DACOGEN may impair fertility in both males and females based on animal studies showing testicular atrophy and ovarian effects. In humans, oligospermia, azoospermia, and amenorrhea have been reported. Effects may be irreversible. Pre-treatment sperm banking and oocyte cryopreservation should be discussed. |