High Efficacy of Intravenous Gimatecan on Human Tumor Xenografts.

Abstract:

BACKGROUND/AIM: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. MATERIALS AND METHODS:The antitumor activity of gimatecan delivered i.v. q4dx4 was evaluated in nude mice bearing human tumors and compared to clinically available anticancer drugs. RESULTS: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. CONCLUSION: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.

journal_name

Anticancer Res

journal_title

Anticancer research

authors

DE Cesare M

doi

10.21873/anticanres.12917

subject

Has Abstract

pub_date

2018-10-01 00:00:00

pages

5783-5790

issue

10

eissn

0250-7005

issn

1791-7530

pii

38/10/5783

journal_volume

38

pub_type

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