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Anticancer agent

外国特許コード F170009202
整理番号 AF12-12WO
掲載日 2017年9月12日
出願国 欧州特許庁(EPO)
出願番号 13758278
公報番号 2837387
公報番号 2837387
出願日 平成25年3月5日(2013.3.5)
公報発行日 平成27年2月18日(2015.2.18)
公報発行日 令和2年7月29日(2020.7.29)
国際出願番号 JP2013055927
国際公開番号 WO2013133253
国際出願日 平成25年3月5日(2013.3.5)
国際公開日 平成25年9月12日(2013.9.12)
優先権データ
  • 特願2012-052334 (2012.3.8) JP
  • 2013JP55927 (2013.3.5) WO
発明の名称 (英語) Anticancer agent
発明の概要(英語) According to the present invention, an anticancer agent is provided that has as an active ingredient thereof a human antibody light chain that demonstrates cytotoxicity against cancer cells and particularly lung cancer cells. The anticancer agent of the present invention primarily comprises: a human antibody º-type light chain in the form of a dimer in which the variable region is composed of a polypeptide represented by the amino acid sequence of SEQ ID NO: 1, 9 or 13 or an amino acid sequence in which one or a plurality of amino acids have been added, deleted or substituted in these amino acid sequences; or, a human antibody º-type light chain in the form of a monomer in which the variable region is composed of a polypeptide represented by the amino acid sequence of SEQ ID NO: 19 or an amino acid sequence in which one or a plurality of amino acids have been added, deleted or substituted in the amino acid sequence.
従来技術、競合技術の概要(英語) BACKGROUND ART
Antibodies are composed of heavy chains (H chains) and light chains (L chains). The heavy chains and light chains are composed of a variable region (VR) and a constant region (CR), and the variable region has a complementarity determining region (CDR). Moreover, antibody light chains are classified into κ chains and λ chains.
In recent years, attention has been focused on antibodies having an enzyme-like activity, namely, antibody enzymes. Since antibody enzymes have both the ability of antibodies to accurately recognize molecules and the activity of enzymes, they are expected to be applied in numerous fields, including medicine, the chemical industry and the food industry. In particular, since antibody enzymes exhibit high specificity for a target molecule and are able to impair target molecules due to their enzyme activity, they are expected to serve as superior anticancer agents that demonstrate few adverse side effects.
The inventors of the present invention have heretofore conducted various innovative researches on antibody enzymes (see, for example, Patent Document 1). Antibody enzymes having complete human sequences have conventionally been unable to be obtained with the exception of the Bence-Jones Protein (BJP) obtained from multiple myeloma patients. Since there are few multiple myeloma patients and only a small amount of BJP that has enzyme activity, it was difficult to acquire a human antibody enzyme. However, since human antibody enzymes are predicted to demonstrate few adverse side effects when administered to a human body, pharmaceutical companies both at home and overseas are awaiting the development of a useful human antibody enzyme.
Prior Art Documents
Patent Documents
Patent Document 1: Japanese Unexamined Patent Application, First Publication No. 2006-197930
The international patent application published under reference WO2011/102517 discloses antiviral agents comprising an antibody κ-type light chain against rabies virus and which have particular enzymatic activities.
特許請求の範囲(英語) [claim1]
1. A pharmaceutical composition for use in the treatment of lung cancer by eradicating cancer cells or suppressing or inhibiting a proliferation of the cancer cells, comprising:
(1) a human antibody κ-type light chain in the form of a dimer in which a variable region is composed of a polypeptide represented by

an amino acid sequence of SEQ ID NO: 9, or
an amino acid sequence having an identity of 95% or more with the amino acid sequence of SEQ ID NO: 9 and having the same CDRs as the amino acid sequence of SEQ ID NO: 9; or
(2) a human antibody κ-type light chain in the form of a monomer in which a variable region is composed of a polypeptide represented by

an amino acid sequence of SEQ ID NO: 19, or
an amino acid sequence having an identity of 95% or more with the amino acid sequence of SEQ ID NO: 19 and having the same CDRs as the amino acid sequence of SEQ ID NO: 19; wherein the CDRs in the amino acid sequence of SEQ ID NO: 9 consist of the 24th to 40th amino acid residues, the 56th to 62nd amino acid residues, and the 95th to 102nd amino acid residues; and
wherein the CDRs in the amino acid sequence of SEQ ID NO: 19 consist of the 24th to 39th amino acid residues, the 55th to 61st amino acid residues, and the 94th to 101st amino acid residues.

[claim2]
2. A pharmaceutical composition for use according to claim 1, wherein
the human antibody κ-type light chain of (1) above is a human antibody κ-type light chain in the form of a dimer composed of a polypeptide represented by

an amino acid sequence of SEQ ID NO: 10, or
an amino acid sequence having an identity of 95% or more with the amino acid sequence of SEQ ID NO: 10 and having the same CDRs as the amino acid sequence of SEQ ID NO: 10; or
the human antibody κ-type light chain of (2) above is a human antibody κ-type light chain in the form of a monomer composed of a polypeptide represented by an amino acid sequence in which cysteine at position 219 has been deleted or substituted by an amino acid other than cysteine in the amino acid sequence of SEQ ID NO: 20, or an amino acid sequence having an identity of 95% or more with this amino acid sequence and having the same CDRs as the amino acid sequence of SEQ ID NO: 20; wherein the CDRs in the amino acid sequence of SEQ ID NO: 10 consist of the 24th to 40th amino acid residues, the 56th to 62nd amino acid residues, and the 95th to 102nd amino acid residues; and
wherein the CDRs in the amino acid sequence of SEQ ID NO: 20 consist of the 24th to 39th amino acid residues, the 55th to 61st amino acid residues, and the 94th to 101st amino acid residues.
  • 出願人(英語)
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
  • 発明者(英語)
  • HIFUMI EMI
  • UDA TAIZO
国際特許分類(IPC)
指定国 Contracting States: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
参考情報 (研究プロジェクト等) CREST Establishment of Innovative Manufacturing Technology Based on Nanoscience AREA
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