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NEW MOLECULARLY TARGETED DRUG FOR TREATING MALIGNANT TUMORS

Foreign code F160008659
File No. (S2014-1065-N0)
Posted date Feb 5, 2016
Country WIPO
International application number 2015JP065749
International publication number WO 2015198797
Date of international filing Jun 1, 2015
Date of international publication Dec 30, 2015
Priority data
  • P2014-130925 (Jun 26, 2014) JP
Title NEW MOLECULARLY TARGETED DRUG FOR TREATING MALIGNANT TUMORS
Abstract The present invention addresses the problem of providing a new molecularly targeted drug that targets RPL29, a ribosomal protein that has enhanced expression in malignant tumor cells. With regard to a molecularly targeted drug that targets RPL29, the present invention addresses the problem of providing an antitumor drug that has a higher efficacy on RPL29. Provided is a molecularly targeted drug comprising an antibody or peptide vaccine for RPL29, said molecularly targeted drug characterized in that the drug targets a segment of 5 or more amino acid residues within the amino acid sequence that constitutes the RPL29 protein, that is, a segment contained either in SEQ ID NO. 1 of the sequence listing or in an amino acid sequence contained in SEQ ID NO. 1 that has 1 or more amino acid residue deletions, substitutions, insertions, or additions.
Outline of related art and contending technology BACKGROUND ART
Molecular target drugs include current for malignant tumors, liver cancer or renal cancer used Sorafenib, used to patients with colorectal cancer bevacizumab or cetuximab (Bevacizumab) (Cetuximab), lung cancer (Erlotinib) gefitinib or erlotinib used (Gefitinib), such as breast cancer (Trastuzumab) trastuzumab used have been developed and are a number of drugs are, used in clinical practice. Each drug to the target material may include, for example cancer kinase, vascular endothelial growth factor (Vascular Endothelial Growth Factor: VEGF), epidermal growth factor receptor (Epidermal Growth Factor Receptor: EGFR), protein HER2(human epidermal growth factor receptor type2) and the like. However, molecular targets for drug is malignant tumor, a skin disorder or alimentary canal perforation, interstitial pneumonia, severe side effects such as death from liver failure have been reported example. Therefore, a higher level of safety has been desired the advent of molecular target drugs.
Healthy person also malignant tumor (cancer) and several thousands of daily can be said to be the cell, but are not necessarily all the onset. Autoimmune hepatitis (Autoimmune hepatitis: AIH) 0.7% / years (Aliment Pharmacol Ther 2006 liver carcinogenesis rate; 24:1197) and have been reported, chronic hepatitis C 3% / year rate of liver carcinogenesis (Ann Intern Med 1999; 131:174) are clearly inferior to low rates.
Ribosomal protein RPL29(Ribosomal protein L29) is in, (non-patent document 1) colon cancer, hepatocellular carcinoma (non-patent document 2), (non-patent document 3) gastric cancer, thyroid cancer (non-patent document 4), such as breast cancer (non-patent document 5) and a variety of malignant tumor cells when increased expression has been reported. RPL29 Is expressed inside the cell expressing the cell surface at the same time also be a membrane protein, RPL29 decreases the expression and apoptosis of the cells is increased in thatacoustic (non-patent document 6), cells induced to differentiate (non-patent document 1) are reported.
The invention relates to a molecular target drug for malignant tumors, targeting molecules target medicine RPL29 studied is reported. Daily healthy person also can be several thousands of cancer cells even though it is said that the, not necessarily all the onset of a cancer or not, autoimmune hepatitis (AIH) rate and liver carcinogenesis have been reported and 0.7% / years, 3% / years of chronic hepatitis C are clearly inferior to the low rates have been reported. Then, auto-immune disease in the patient serum, may inhibit the growth of malignant tumor cells in the presence of immunoglobulin (IgG) confirmed, targeting the RPL29 anti-RPL29 antibody disclosed (patent document 1). Anti-RPL29 antibody titers in the patent document 1 as an index of the inspection method for malignant tumor disclosed.
Scope of claims (In Japanese)請求の範囲 [請求項1]
RPL29に対する抗体又はペプチドワクチンからなる分子標的薬であって、RPL29タンパク質を構成するアミノ酸配列のうち、配列表の配列番号1に示すアミノ酸配列の部分、又は配列番号1に示すアミノ酸配列のうち1若しくは複数個のアミノ酸残基が欠失、置換、導入若しくは付加されたアミノ酸配列の部分を標的とし、配列番号1に示すアミノ酸配列のうち、第41番目のR(アルギニン)から第159番目のE(グルタミン酸)で特定されるアミノ酸配列から選択され、少なくとも5個のアミノ酸残基を含む部分を標的とすることを特徴とする分子標的薬。

[請求項2]
請求項1に記載の分子標的薬が、配列表の配列番号1に示すアミノ酸配列の第146番目のQ(グルタミン)から159番目のE(グルタミン酸)、第81番目のV(バリン)から第135番目のA(アラニン)、又は第41番目のR(アルギニン)から第75番目のL(ロイシン)で特定されるいずれかのアミノ酸配列から選択され、各アミノ酸配列における連続する少なくとも5個のアミノ酸残基を含む部分を標的とすることを特徴とする、請求項1に記載の分子標的薬。

[請求項3]
分子標的薬の標的部位が、以下の配列番号24、21、24、22、23及び25に示すいずれかのアミノ酸配列から選択される部分である、請求項1に記載の分子標的薬。
pklgkrarariakg(配列番号24)
qapkrtqaptkase(配列番号21)
mrfakkhnkkglkk(配列番号22)
lvkpkevkpkipkg(配列番号23)
rlcrpkakakakak(配列番号25)

[請求項4]
分子標的薬が抗体であり、以下の配列番号24、21、24、22、23及び25に示すいずれかのアミノ酸配列における連続した少なくとも5アミノ酸残基をエピトープとして認識することを特徴とする抗RPL29抗体からなる、請求項1又は3に記載の分子標的薬。
pklgkrarariakg(配列番号24)
qapkrtqaptkase(配列番号21)
mrfakkhnkkglkk(配列番号22)
lvkpkevkpkipkg(配列番号23)
rlcrpkakakakak(配列番号25)

[請求項5]
分子標的薬がペプチドワクチンであり、以下の配列番号24、21、24、22、23及び25に示すいずれかのアミノ酸配列における連続した少なくとも5アミノ酸残基を含む、RPL29に対するペプチドワクチンからなる、請求項1又は3に記載の分子標的薬。
pklgkrarariakg(配列番号24)
qapkrtqaptkase(配列番号21)
mrfakkhnkkglkk(配列番号22)
lvkpkevkpkipkg(配列番号23)
rlcrpkakakakak(配列番号25)

[請求項6]
請求項1~5のいずれか1に記載の分子標的薬を有効成分として含む抗悪性腫瘍剤。

[請求項7]
悪性腫瘍が、膵癌、乳癌、肺腺癌、大腸癌、肝細胞癌、胃癌、甲状腺癌、卵巣癌、唾液腺腺様嚢胞癌、前立腺癌、バーキットリンパ腫、急性骨髄性白血病、粘液性脂肪肉腫、膠芽腫、胞巣状横紋筋肉腫、ウィルムス腫瘍、乏突起膠細胞腫、副腎皮質癌、多発性骨髄腫、結節性リンパ球優位型ホジキンリンパ腫、形質細胞白血病、髄芽腫、B細胞性慢性リンパ性白血病、肺線癌、肺扁平上皮癌、II型子宮内膜癌、びまん性大細胞型B細胞リンパ腫、食道癌、末梢T細胞リンパ腫、未分化大細胞型リンパ腫、ユーイング肉腫及び前駆T細胞リンパ芽球性白血病から選択される一種又は複数種である、請求項6に記載の抗悪性腫瘍剤。

[請求項8]
悪性腫瘍が、膵癌、乳癌、肺腺癌及び大腸癌から選択される一種又は複数種である、請求項7に記載の抗悪性腫瘍剤。

  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY
  • Inventor
  • MIYAKE, Yasuhiro
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG

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