Drug intelligence / Profile preview

liposome-encapsulated cytarabine (cytarabine liposome)

Development stage
Unknown
Lead developer
SkyePharma
Modality
Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intrathecal
01

Overview

Cytarabine liposome is a sustained-release, liposomal formulation of the pyrimidine nucleoside analog cytarabine, specifically designed for intrathecal administration. It utilizes the DepoFoam multivesicular liposome technology to encapsulate cytarabine, which significantly extends the drug's half-life in the cerebrospinal fluid (CSF) compared to standard cytarabine, allowing for a dosing schedule of once every two weeks. As an antimetabolite, cytarabine is converted intracellularly into cytarabine triphosphate, which competes with deoxycytidine triphosphate for incorporation into DNA and inhibits DNA polymerase, thereby halting DNA synthesis and inducing apoptosis in rapidly dividing cells. While it was FDA-approved for the treatment of lymphomatous meningitis, the product was discontinued from the market in recent years due to manufacturing complexities. It has also been extensively studied for central nervous system (CNS) prophylaxis in leukemias such as acute lymphoblastic leukemia (ALL).

Brand names
DepoCyteDepoCyt
Other names
liposomal cytarabineliposome-encapsulated cytarabineDepoFoam cytarabine
02

Targets

TOP2A (DNA topoisomerase II)DNA polymerase family

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