作者: A. Setanoians , P. Wilson , M. A. Graham , V. Auzannet , G. A. Chadwick
DOI:
关键词:
摘要: Abstract N-Debenzoyl-N-tert-butoxycarbonyl-10-deacytyl taxol (Taxotere, RP 56976) is a semisynthetic analogue of taxol, prepared from noncytotoxic precursor extracted the needles European yew tree (Taxus baccata L.). It has broad spectrum antitumor activity against variety transplantable tumors in mice. In vitro cytotoxicity assays suggest that it 2–5-fold more potent than taxol. this phase I study Taxotere was administered by 24 h i.v. infusion at 3-week intervals. Thirty patients with solid refractory to conventional therapy were treated; 70 courses doses ranging 10 90 mg/m2. Grade 4 neutropenia and grade 3 mucositis dose limiting but reversible The pattern toxicity similar heavily pretreated compared 7 who had received maximum one previous chemotherapy regimen. Alopecia occurred 55 mg/m2 above. Other mild toxicities included phlebitis, diarrhea, emesis, sensory peripheral neuropathy, these neither dose-limiting nor clearly dose-related. One patient treated an anaphylactoid reaction following second Taxotere. No cardiovascular observed. partial or complete responses documented. Plasma concentrations determined high-performance liquid chromatography, end-of-fusion levels tolerated exceeded drug which are cytotoxic vitro. for as 24-h