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L-OddC prodrugs for cancer

A cancer and drug delivery technology, applied in the field of nucleoside compounds for the treatment of cancer, can solve the problems of low systemic clearance rate, high toxicity, slow concentration, etc., and achieve the effect of improving bioavailability

Active Publication Date: 2009-09-16
UNIV OF GEORGIA RES FOUND INC
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Problems solved by technology

However, although troxitabine exhibits a relatively long intracellular retention time and low systemic clearance, pharmacokinetic studies indicate that it accumulates slowly in cancer cells compared to nucleosides transported by other vehicles
3 Troxatabine, like most other anticancer nucleosides, is a hydrophilic agent and must be administered intravenously in a frequent dose schedule, which may result in greater toxicity than a single dose schedule

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  • L-OddC prodrugs for cancer
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  • L-OddC prodrugs for cancer

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[0021] The term "patient" or "subject" as used throughout refers to an animal, usually a mammal and preferably a human, to whom treatment, including prophylactic treatment, is provided with the composition of the invention. For treatment of an infection, condition or disease state specific to a patient in a particular animal (eg, human), the term patient refers to that particular animal.

[0022] As used herein, unless otherwise stated, the term "compound" refers to any specific chemical compound disclosed herein. When used in this context, the term generally refers to a single compound, preferably a (L-beta anomer) prodrug of the nucleoside L-OddC or various racemates or enrichments of the L-OddC prodrug form Enantiomerically enriched (enantiomerically enriched at least 75%, 85%, 95%, 98%, 99%, 99+%, 100%), as otherwise described herein. The compounds of the present invention have little if any toxicity to host cells in the treatment of cancer and have shown unexpected resul...

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Abstract

The main drawback in the use of most nucleoside anticancer agents originates from their hydrophilic nature, of which property requires a high and frequent dosage for an intravenous administration. Unlike other nucleoside anti-tumor agents, troxacitabine appears to predominantly enter tumor cells by passive diffusion rather then by using nucleoside transporters, although this may be model dependent. Accordingly, in the present work, a small library of twenty troxacitabine prodrugs has been synthesized using a parallel approach in order to evaluate the relationship between the lipophilicity of the prodrugs and their antitumor activity. Biological evaluation of the prodrugs on two non-small cell lung cancer cell lines (A549 and SW1573) and in pancreatic cell lines clearly showed better antitumor activity than that of troxacitabine, with IC50 values in the nanomolar range.

Description

field of invention [0001] The present invention relates to nucleoside compounds useful in the treatment of cancer, especially non-small cell lung cancer and pancreatic cancer. The present invention relates to the use of certain prodrug forms of L-OddC or troxacitabine for the treatment of cancer, particularly non-small cell lung and pancreatic cancer. [0002] related application [0003] This application claims priority to U.S. Provisional Application US60 / 842,085, filed September 1, 2006, entitled "Prodrugs of Troxatabine for the Treatment of Cancer, Especially Non-Small Cell Lung Cancer", which is incorporated in its entirety This article is for reference. Background of the invention [0004] Troxatyl TM ; L-OddC; (-)-2'-deoxy-3'-oxacytidine) 1 It is the first L-nucleoside analogue that has demonstrated anticancer activity and is currently in a pivotal Phase II / III clinical trial for the third line treatment of acute myeloid leukemia (AML) Evaluated and conducted a p...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675
CPCA61K31/675A61P1/18A61P11/00A61P35/00A61P35/02A61K31/513
Inventor 戴维·C·K·丘
Owner UNIV OF GEORGIA RES FOUND INC
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