Depsipeptide for therapy of kidney cancer

Inventors

Naoe, YoshinoriBates, Susan E.

Assignees

HEALTH AND HUMAN SERVICES GOVERNMENT OF UNITED STATES REPRESENTED BY SECRETARY DEPARTMENT OFAstellas Pharma IncUS Department of Health and Human Services

Publication Number

US-8673888-B2

Publication Date

2014-03-18

Expiration Date

2023-03-27

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Abstract

The present invention provides a therapeutic agent of kidney cancer, which comprises FK228 of the formula (I) or a salt thereof. FK228 or a salt thereof, which is an active ingredient in the present invention, shows a superior antitumor activity in vivo against kidney cancer.

Core Innovation

The invention provides a therapeutic agent for kidney cancer comprising FK228 or its salt, which exhibits superior antitumor activity in vivo against kidney cancer, including in human patients. FK228, also referred to as a compound of formula (I), and its stereoisomer FR901228 (formula (II)) are potent histone deacetylase inhibitors that have demonstrated effectiveness in suppressing kidney cancer growth when administered to mammals, particularly humans.

The problem solved by the invention is the lack of demonstrated antitumor activity in vivo against kidney cancer despite prior knowledge of FK228’s antitumor effects in vitro. Substances exhibiting antitumor activity in vitro do not necessarily exhibit such activity in vivo, creating difficulty in applying these substances directly as therapeutic agents. The invention addresses the unmet need to confirm in vivo efficacy against kidney tumors, which had not been previously reported.

Claims Coverage

The patent contains three independent claims covering methods of treating kidney cancer, methods of suppressing cancerous tumor growth in vivo, and the use of specific compounds as therapeutic agents against kidney cancer.

Method of treating kidney cancer with a compound of formula (I)

Administering an effective amount of a compound of formula (I) or its salt to a mammal in need thereof to treat kidney cancer.

Method of suppressing growth of kidney cancer tumors in vivo

Administering an effective amount of a compound of formula (I) or its salt to a mammal in vivo (including humans) to suppress growth of kidney cancer tumors.

Use of a compound of formula (I) for producing a therapeutic agent for kidney cancer

Employing a compound of formula (I) or its salt for producing a therapeutic agent that exhibits antitumor activity in vivo specifically for treating kidney cancer.

The independent claims focus on the therapeutic application of FK228 compounds and their salts in treating kidney cancer through effective administration in mammals, particularly humans, emphasizing suppression of tumor growth and production of therapeutic agents with confirmed in vivo antitumor activity.

Stated Advantages

Shows superior antitumor activity not only in vitro but also in vivo for kidney cancer.

Demonstrated effectiveness in human patients with kidney cancer.

Potent histone deacetylase inhibitory activity contributing to therapeutic effect.

Documented Applications

Therapeutic agent for treating kidney cancer in mammals including humans.

Pharmaceutical compositions containing FK228 or its salts as active ingredients for kidney cancer treatment.

Methods of administering FK228 or its salts via various routes such as intravenous, intramuscular, or oral administration for kidney cancer therapy.

Combination treatment with FK228 and retinoic acid for enhanced therapeutic effect.

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