Open AccessAssessment of Cytosine Arabinoside as an Antiviral Agent in Humans
Author(s) -
Lauter Cb,
Bailey Ej,
Lerner Am
Publication year - 1974
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.6.5.598
Subject(s) - pharmacokinetics , pharmacology , cytosine , cytarabine , dose , cytotoxicity , herpes simplex virus , idoxuridine , urine , clinical trial , human cytomegalovirus , in vitro , virology , biology , medicine , virus , immunology , leukemia , dna , biochemistry
Cytotoxicity, minimal inhibitory concentrations of herpesviruses, and pharmacokinetic studies of cytosine arabinoside (ara-C) were done. Ara-C compared favorably with idoxuridine in in vitro studies of antiviral activity versus herpes simplex, varicella-zoster, and cytomegalovirus. However, ara-C was 10 times more toxic to tissue cultures, and concentrations in serum and urine of three patients who were given ara-C at acceptable dosages (1 mg/kg per day) were not measurable by our assay. These studies predict that ara-C is not likely to be a useful antiviral agent in humans because its therapeutic to toxic ratio approaches unity. These predictions of little clinical efficacy seem now to have been confirmed by clinical trails in humans. Pharmacokinetic studies outlined here should precede and help formulate controlled clinical trials of potential antiviral agents in humans.