st-1481 and Astrocytoma

The lipophilic, orally bioavailable camptothecin analogue gimatecan is characterized by improved efficacy over conventional camptothecins on human tumor xenografts. Gimatecan produced excellent outcomes orally with prolonged, low-dose, daily treatments. The aim of this study was to assess the antitumor efficacy of i.v. administered gimatecan.. The antitumor activity of gimatecan delivered i.v. q4dx4 was evaluated in nude mice bearing human tumors and compared to clinically available anticancer drugs.. Intravenous administration of gimatecan showed superior efficacy with remarkable achievements at well tolerated doses. Moreover, prolonged treatments with i.v. administered gimatecan showed efficacy in models of cancer refractory to current therapeutic approaches, like an orthotopic brain tumor.. Although the oral route is practical for gimatecan administration, the results support the interest in developing a suitable i.v. formulation in an attempt to further exploit the therapeutic potential of the compound.

Topics: Administration, Oral; Animals; Apoptosis; Astrocytoma; Bone Neoplasms; Camptothecin; Cell Proliferation; Colonic Neoplasms; Female; Humans; Mice; Mice, Nude; Tumor Cells, Cultured; Xenograft Model Antitumor Assays