Τόμος 10 (1996) – Τεύχος 2 – Άρθρο 1 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 10 (1996) – Issue 2 – Article 1 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title Water-insoluble camptothecin analogues as anticancer and antiviral drugs and in clinical studies
Author Panayotis Pantazis

The Stehlin Foundation for Cancer Research at St. Joseph Hospital, Houston, Texas 77003, USA

Citation Pantazis, P.: Water-insoluble camptothecin analogues as anticancer and antiviral drugs and in clinical studies, Epitheorese Klin. Farmakol. Farmakokinet. 10(2): 51-74 (1996)
Publication Date Received for publication: 2 May 1996

Accepted for publication: 20 June 1996

Full Text Language English
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Keywords Camptothecin, combination treatment, antivirus activity, clinical trials.
Other Terms review article
Summary The plant product camptothecin (CRT) and several of its water-soluble derivatives have demonstrated an unprecedented curative activity against human tumors grown as xenografts in immunodeficient athymic mice. The molecular target of CPT is the nuclear enzyme topoisomerase I (topo I) which is involved in several vital cellular functions including division. Further, other cellular factors can regulate the CPVs cytotoxic activity which appears to be selectively directed against malignant but not against non-malignant cells. Studies with cultured cells have shown that the antitumor activity of CPT can be enhanced by other anticancer drugs, agents that induce topo I phosphorylation, ionizing radiation and hyperthermia. Also, CPT is a potent inducer for differentiation of several human leukemia cell lines. Finally, studies with cultured cells and animals have shown that CPT can interrupt functions of DNA and RNA viruses that cause diseases in animals and human, presumably by interfering with topo I activities required for some viral functions. Early results of clinical trials, currently in progress, have shown remarkable response of several human tumors to CPT. In addition, our laboratory’s efforts are directed toward development of parameters/conditions that will protect and/or enhance the antitumor activity of the CPT molecule, while minimizing the drug-induced toxic effects.
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