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Therapeutic combination comprising a cdks inhibitor and an antineoplastic agent

An anti-tumor agent and inhibitor technology, which can be used in anti-tumor drugs, drug combinations, medical preparations containing active ingredients, etc., and can solve problems such as increased cancer incidence.

Active Publication Date: 2011-06-22
NERVIANO MEDICAL SERVICES SRL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, altered expression of cyclin E and cdks has been observed in tumor cells, and deletion of the cdk inhibitor p27 KIP gene in mice has also been shown to lead to increased incidence of cancer

Method used

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  • Therapeutic combination comprising a cdks inhibitor and an antineoplastic agent
  • Therapeutic combination comprising a cdks inhibitor and an antineoplastic agent
  • Therapeutic combination comprising a cdks inhibitor and an antineoplastic agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: In vitro cytotoxic activity of combinations with gemcitabine

[0047] Implant the exponentially growing A2780 human ovarian cancer cell line and incubate at 37°C in a humidified 5% CO 2 Cultivated under atmosphere. After 24 hours, a scalar dose of a compound of formula (I) as defined above is added to the medium for 24 hours, the cells are washed and gemcitabine is added for 1 hour. Cells were then washed and counted 72 hours after the first treatment. Cell proliferation was measured by an intracellular ATP monitoring system. Cell proliferation was compared to control cells. Calculate the concentration that inhibits 50% cell proliferation (IC 50 ).

[0048] The Combination Index (C.I.) is calculated using a computer program for the analysis of effects of multiple drugs based on the Chou-Talalay equation for mutually non-exclusive drugs (Adv Enzyme Regul 1984; 22:27-55), where C.I. and effects.

[0049] The results obtained with the drugs alone and in c...

Embodiment 2

[0053] Example 2: In vitro cytotoxic activity of combination with oxaliplatin

[0054] Implant the exponentially growing A2780 human ovarian cancer cell line and incubate at 37°C in a humidified 5% CO 2 Cultivated under atmosphere. After 24 hours, a scalar dose of oxaliplatin is added to the medium for 1 hour, the cells are washed and the compound of formula (I) is added for 24 hours. Cells were then washed and counted 72 hours after the first treatment. Cell proliferation was measured by an intracellular ATP monitoring system. Cell proliferation was compared to control cells. Calculate the concentration that inhibits 50% cell proliferation (IC 50 ).

[0055] The Combination Index (C.I.) is calculated using a computer program for the analysis of effects of multiple drugs based on the Chou-Talalay equation for mutually non-exclusive drugs (Adv Enzyme Regul 1984; 22:27-55), where C.I. and effects.

[0056] The results obtained with the drugs alone and in combination are s...

Embodiment 3

[0060] Example 3: In vitro cytotoxic activity of combinations with SN-38

[0061] SN38 is the active metabolite of irinotecan, which is obtained by hydrolysis of irinotecan. Implant the exponentially growing A2780 human ovarian cancer cell line and incubate at 37°C in a humidified 5% CO 2 Cultivated under atmosphere. After 24 hours, a scalar dose of SN-38 is added to the medium for 1 hour, the cells are washed and the compound of formula (I) is added for 24 hours. Cells were then washed and counted 72 hours after the first treatment. Cell proliferation was measured by an intracellular ATP monitoring system. Cell proliferation was compared to control cells. Calculate the concentration that inhibits 50% cell proliferation (IC 50 ).

[0062] The Combination Index (C.I.) is calculated using a computer program for the analysis of effects of multiple drugs based on the Chou-Talalay equation for mutually non-exclusive drugs (Adv Enzyme Regul 1984; 22:27-55), where C.I. and eff...

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PUM

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Abstract

The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of alkylating or alkylating-like agents, antimetabolite agents and topoisomerase I inhibitors, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.

Description

technical field [0001] The present invention generally relates to the field of cancer treatment, and more specifically, provides an antitumor composition having a synergistic or additive antitumor effect, comprising a cdks inhibitor and an alkylating agent or an alkylating agent and / or an antimetabolite and / or or topoisomerase I inhibitors. Background technique [0002] It is well known that progression throughout the cell cycle is governed by a series of checkpoint controls, also called checkpoints, regulated by a family of enzymes called cyclin-dependent kinases (cdks). In turn, the cdks themselves are regulated at many levels, such as binding to cyclins. [0003] Coordinated activation and inactivation of different cyclin / cdk complexes is necessary for normal progression throughout the cell cycle. Control of critical G1-S and G2-M transitions by differential cyclin / cdk activation. In G1, cyclin D / cdk4 and cyclin E / cdk2 are thought to mediate S-phase initiation. Progre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K45/06A61P35/00A61K31/282A61K31/4188A61K31/4745A61K31/513A61K31/53A61K31/7068
CPCA61K31/53A61K31/513A61K31/4188A61K45/06A61K31/7068A61K31/519A61K31/282A61K31/4745A61K31/495A61K31/555A61P35/00A61P43/00A61K2300/00
Inventor M·塞欧梅A·马斯格里奥V·D·克罗西E·派森逖
Owner NERVIANO MEDICAL SERVICES SRL
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