Drug intelligence / Profile preview

high-dose cytarabine

Development stage
Phase 4
Modality
Small Molecules
Administration
Intravenous, Subcutaneous, Intrathecal
01

Overview

High-dose cytarabine refers to a specific administration regimen of the chemotherapy drug cytarabine. Cytarabine is a pyrimidine analog and an antimetabolite that functions by interfering with DNA synthesis. Once inside the cell, it is converted into its active triphosphate form, ara-CTP, which then competes with cytidine to be incorporated into DNA. This incorporation inhibits DNA polymerase, leading to the termination of DNA chain elongation and ultimately halting DNA replication, primarily affecting rapidly dividing cells during the S-phase of the cell cycle. High-dose regimens, typically involving doses of 2-3 g/m² every 12 hours, are commonly employed in the treatment of hematologic malignancies such as acute myeloid leukemia (AML) and acute lymphocytic leukemia (ALL) to achieve greater efficacy, particularly in certain aggressive subtypes. While effective, this regimen is associated with increased toxicity, notably cerebellar damage.

Brand names
Cytosar-UDepocytTarabine PFSArasidBiobinCytabinCytarineCytrosarOncotar
Other names
cytosine arabinoside
02

Targets

RNR (Ribonucleotide reductase)DNADNA polymerase family

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