Cytarabine (4 brand names, 3 dosage forms, 2 routes)
Available dosage forms: INJECTABLE, POWDER, INJECTABLE, LIPOSOMAL.
Routes of administration: INJECTION, INTRAVENOUS.
Brand Names
- CYTARABINE
- CYTOSAR-U
- DEPOCYT
- VYXEOS
Boxed Warning
• VYXEOS has different dosage recommendations than daunorubicin hydrochloride injection, cytarabine injection, daunorubicin citrate liposome injection, and cytarabine liposome injection. Verify drug name and dose prior to preparation and administration to avoid dosing errors [see Warnings and Precautions (5.1)].
Indications and Usage
VYXEOS is indicated for the treatment of newly diagnosed therapy-related acute myeloid leukemia (t-AML) or AML with myelodysplasia-related changes (AML-MRC) in adults and pediatric patients 1 year and older.
Contraindications
The use of VYXEOS is contraindicated in patients with the following: •History of serious hypersensitivity reaction to cytarabine, daunorubicin, or any component of the formulation [see Warnings and Precautions ( 5.4 )].
Adverse Reactions
The following adverse reactions are discussed in greater detail in other sections of the labeling: •Hemorrhage [see Warnings and Precautions (5.2)] •Cardiotoxicity [see Warnings and Precautions (5.3)] •Hypersensitivity Reactions [see Warnings and Precautions (5.4)] •Copper Overload [see Warnings and Precautions (5.5)] •Tissue Necrosis [see Warnings and Precautions (5.6)]
Mechanism of Action
VYXEOS (daunorubicin and cytarabine) liposome for injection is a liposomal formulation of daunorubicin and cytarabine at a fixed 1:5 molar ratio. The 1:5 molar ratio of daunorubicin:cytarabine has been shown to have synergistic effects at killing leukemia cells in vitro and in murine models. Daunorubicin has antimitotic and cytotoxic activity, which is achieved by forming complexes with DNA, inhibiting topoisomerase II activity, inhibiting DNA polymerase activity, affecting regulation of gene expression, and producing DNA-damaging free radicals. Cytarabine is a cell cycle phase-specific antineoplastic agent, affecting cells only during the S-phase of cell division. Cytarabine acts primarily through inhibition of DNA polymerase. Based on animal data, the liposomes enter and persist in the bone marrow, where they are taken up intact by bone marrow cells. In leukemia-bearing mice, the liposomes are taken up by leukemia cells to a greater extent than by normal bone marrow cells. After cellular internalization, liposomes undergo degradation releasing cytarabine and daunorubicin within the intracellular environment.