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Published in:

01-08-2002 | Review Article

Clinical Pharmacokinetics of Cytarabine Formulations

Authors: Akinobu Hamada, Takeo Kawaguchi, Masahiro Nakano

Published in: Clinical Pharmacokinetics | Issue 10/2002

Abstract

Cytarabine (cytosine arabinoside, Ara-C) is an effective chemotherapeutic agent for the treatment of acute myelogenous leukaemia and lymphocytic leukaemias. As cytarabine is an S-phase-specific drug, prolonged exposure of cells to cytotoxic concentrations is critical to achieve maximum cytotoxic activity. However, the activity of cytarabine is decreased by its rapid deamination to the biologically inactive metabolite uracil arabinoside. This rapid deamination is the reason for the ongoing search for effective formulations and derivatives of cytarabine that cannot be deaminated and exhibit better pharmacokinetic parameters.

Protection of cytarabine from fast degradation and elimination has been investigated by encapsulating the drug into pharmaceutically acceptable carriers. Cytarabine derivatives have shown promise in vitro and in animal models. For example, ancitabine (cyclocytidine), enocitabine and cytarabine ocfosfate have been used clinically in Japan. Cytarabine encapsulated into multivesicular liposomes has been approved in several countries for the intrathecal treatment of lymphomatous meningitis.

Although many compounds have been investigated, few cytarabine derivatives are currently available for clinical use. Further research is needed to improve the efficacy of cytarabine against haematological and solid tumours.

Use of tradenames is for product identification only and does not imply endorsement.

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Title: Clinical Pharmacokinetics of Cytarabine Formulations
Authors: Akinobu Hamada
Takeo Kawaguchi
Masahiro Nakano
Publication date: 01-08-2002
Publisher: Springer International Publishing
Published in: Clinical Pharmacokinetics / Issue 10/2002
Print ISSN: 0312-5963
Electronic ISSN: 1179-1926
DOI: https://doi.org/10.2165/00003088-200241100-00002

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Clinical Pharmacokinetics of Cytarabine Formulations

Abstract

Keynote webinar | Spotlight on medication adherence

Springer Medicine

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