Phase I and pharmacokinetic studies of DON.
Cancer Treat Rep
; 65(11-12): 1031-6, 1981.
Article
em En
| MEDLINE
| ID: mdl-7296548
ABSTRACT
DON, a glutamine antagonist, was administered iv to 26 patients with advanced cancer either once every 3 wks or daily for 3 days every 3 wks to determine toxicity and to look for evidence of therapeutic effect. Total doses ranged from 150 to 600 mg/m2. The single-day schedule produced intolerable nausea and vomiting and no evidence of cytotoxicity at 450-550 mg/m2 given over 10 mins or over 4 hrs. On the 3-day schedule, patients had tolerable gastrointestinal toxic effects at total doses up to 480 mg/m2 given in three equally divided doses by 10-min infusion. This dose also produced cytotoxic activity manifested as transient mild leukopenia and, rarely, thrombocytopenia. No objective responses were seen. Analysis of the plasma elimination of DON demonstrated dose-dependent pharmacokinetic behavior. The parent compound was not detectable in the urine of any patient, indicating extensive metabolism of the drug.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Azo
/
Diazo-Oxo-Norleucina
/
Neoplasias
Limite:
Female
/
Humans
/
Male
Idioma:
En
Revista:
Cancer Treat Rep
Ano de publicação:
1981
Tipo de documento:
Article