Phase I study of 3′-deamino-3′-(2-methoxy-4-morpholinyl)doxorubicin (FCE 23762, PNU 152243) administered on a daily ×3 schedule

Background 3′-Deamino-3′-(2-methoxy-4-morpholinyl)doxo-rubicin (FCE 23762, PNU 152243) is a highly lipophilic doxo rubicin derivative which possesses potent in vitro and in vivo antitumor activity. Previous phase I studies had been conducted using a single bolus every 28 days. Patients and methods We conducted a phase I study of FCE 23762 on a daily ×3 every 28 days schedule. Thirty patients received 68 cycles of therapy at 5 dose levels (200–600 μg/m2/d). Results Prolonged neutropenia and thrombocytopenia were the dose-limiting toxicities. Other nonhematological toxicities included nausea and vomiting, anorexia, fatigue and transient elevations of serum creatinine and hepatic transaminases. No cardiac toxicity was demonstrated. There were no partial or complete antitumor responses. Conclusion The recommended phase II dose using the schedule defined in this study is 500 μg/m2/d × 3.