Early phase II trial of oral vorinostat in relapsed or refractory breast, colorectal, or non-small cell lung cancer

Investigational New Drugs - Tập 26 - Trang 483-488 - 2008
Johan Vansteenkiste1, Eric Van Cutsem2, Herlinde Dumez3, Cong Chen4, Justin L. Ricker4, Sophia S. Randolph4, Patrick Schöffski3
1Respiratory Oncology Unit (Pulmonology), University Hospital Gasthuisberg, Leuven, Belgium
2Digestive Oncology Unit, University Hospital Gasthuisberg, Leuven, Belgium
3Department of General Medical Oncology, University Hospital Gasthuisberg, Leuven, Belgium
4Merck Research Laboratories, Whitehouse Station, USA

Tóm tắt

Vorinostat (Zolinza®) is a histone deacetylase inhibitor that has demonstrated activity in patients with advanced solid tumors in phase I trials. A multicenter, open-label phase II trial of oral vorinostat 200, 300 or 400 mg bid for 14 days followed by a 7-day rest until disease progression or intolerable toxicity was conducted. Patients with measurable, relapsed or refractory breast or non-small cell lung cancer who had received ≥1 prior therapy or colorectal cancer who had received ≥2 prior therapies were eligible. The response rate, safety and tolerability were evaluated. Sixteen patients (median age, 62 years; median 5.5 prior therapies) were enrolled. Six patients received 400 mg bid, six received 300 mg bid and four received 200 mg bid (14 days/3 weeks). Dose-limiting toxicities (DLTs) at the 400 or 300 mg bid levels were anorexia, asthenia, nausea, thrombocytopenia, vomiting, and weight loss. No DLTs were observed at the 200 mg bid level. Disease stabilization was observed in eight patients, but there were no confirmed responses. The median TTP was 33.5 days. Eleven patients discontinued due to clinical adverse experiences (AEs). The most common drug-related AEs were anorexia (81%), fatigue (62%), nausea (62%), diarrhea (56%), vomiting (56%), thrombocytopenia (50%) and weight loss (50%). Drug-related AEs ≥ grade 3 included thrombocytopenia (50%), anemia (12%), asthenia (12%) and nausea (12%). Vorinostat in a daily oral schedule for 14 days/3 weeks was tolerable at 200 mg bid only, and no responses were observed in this study. Most patients, however, had limited drug exposure which did not allow a reliable efficacy analysis.

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