Phase I and Pharmacokinetic Study of Temozolomide on a Daily-for-5-Days Schedule in Patients With Advanced Solid Malignancies
作者： Lisa A. Hammond , John R. Eckardt , Sharyn D. Baker , S. Gail Eckhardt , Margaret Dugan
DOI: 10.1200/JCO.1999.17.8.2604
关键词: Pharmacokinetics 、 Internal medicine 、 Pharmacology 、 Chemotherapy 、 Temozolomide 、 Oncology 、 Toxicity 、 Half-life 、 Dose–response relationship 、 Medicine 、 Pharmacodynamics 、 Neutropenia
摘要: PURPOSE: To determine the principal toxicities, characterize pharmacokinetics (PKs) and pharmacodynamics (PDs) of temozolomide (TMZ) on a daily-for-5-days schedule, recommend dose for subsequent disease-directed studies in both minimally pretreated (MP) heavily (HP) patients. PATIENTS AND METHODS: Patients received TMZ as single oral daily 5 consecutive days every 28 days. doses were escalated from 100 to 150, 150 200 mg/m2/d separate cohorts MP HP PK plasma was sampled 1 5. concentrations analyzed pertinent parameters related toxicities PD analyses. RESULTS: Twenty-four patients treated with 85 courses TMZ. Thrombocytopenia neutropenia dose-limiting (DLTs) this schedule. The cumulative rate severe myelosuppressive effects unacceptably high at exceeding absorbed rap...
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