Title:
ANTIBODY-DRUG CONJUGATE
Document Type and Number:
WIPO Patent Application WO/2023/163227
Kind Code:
A1
Abstract:
The present invention provides a linker, a linker/payload, an antibody-drug conjugate, and an antitumor drug that are novel. Specifically, the present invention provides an antibody-drug conjugate that is represented by general formula (I), a pharmaceutically acceptable salt thereof, or a hydrate of either of these. (In the formula, A is an antibody residue that results from excluding, from an antibody that can target tumor cells, an antibody-internal functional group that relates to bonding with a linker; B is a divalent group that is derived from the aforementioned antibody-internal functional group; a is an integer from 1 to 10; D is an antitumor drug residue that results from removing one hydrogen atom or one hydroxyl group from an arbitrary location in an antitumor drug molecule, an analogue thereof, or a derivative of either of these; L is a linker that links B and D; and at least one of D and L has at least one lactonyl group in an arbritrary location as a substituent or a protective group.)
Inventors:
TSUZAKI YASUNORI (JP)
MIZUNO GEN (JP)
KASHIWAGI TAKAMASA (JP)
TANAKA MASAYUKI (JP)
SHIMIZU HAYATO (JP)
AGA YASUHIRO (JP)
NONOUCHI SHINPEI (JP)
TOKUNAGA YASUNORI (JP)
MATSUSHITA TAKASHI (JP)
KIMURA TOMIO (JP)
MIZUNO GEN (JP)
KASHIWAGI TAKAMASA (JP)
TANAKA MASAYUKI (JP)
SHIMIZU HAYATO (JP)
AGA YASUHIRO (JP)
NONOUCHI SHINPEI (JP)
TOKUNAGA YASUNORI (JP)
MATSUSHITA TAKASHI (JP)
KIMURA TOMIO (JP)
Application Number:
PCT/JP2023/007414
Publication Date:
August 31, 2023
Filing Date:
February 28, 2023
Export Citation:
Assignee:
UBE CORP (JP)
International Classes:
A61K47/68; A61K31/337; A61K31/357; A61K31/407; A61K31/4375; A61K31/4745; A61K31/475; A61K31/513; A61K31/537; A61K31/5513; A61K31/5517; A61K31/675; A61K31/7034; A61K31/7036; A61K31/706; A61K38/07; A61K38/14; A61K39/395; A61K45/00; A61P35/00; C07K2/00; C07K14/435; C07K16/30; C07K19/00
Domestic Patent References:
| WO2014061277A1 | 2014-04-24 |
Foreign References:
| US20200115326A1 | 2020-04-16 |
Other References:
XIAO DIAN, ZHAO LEI, XIE FEI, FAN SHIYONG, LIU LIANQI, LI WEI, CAO RUIYUAN, LI SONG, ZHONG WU, ZHOU XINBO: "A bifunctional molecule-based strategy for the development of theranostic antibody-drug conjugate", THERANOSTICS, IVYSPRING INTERNATIONAL PUBLISHER, AU, vol. 11, no. 6, 1 January 2021 (2021-01-01), AU , pages 2550 - 2563, XP093087170, ISSN: 1838-7640, DOI: 10.7150/thno.51232
KYOJI TSUCHIKAMA, ZHIQIANG AN: "Antibody-drug conjugates: recent advances in conjugation and linker chemistries", PROTEIN & CELL, SPRINGER ASIA, BEIJING, CN, vol. 9, no. 1, 1 January 2018 (2018-01-01), Beijing, CN , pages 33 - 46, XP055461467, ISSN: 1674-800X, DOI: 10.1007/s13238-016-0323-0
LIU LIANQI, XIE FEI, XIAO DIAN, XU XIN, SU ZHENG, WANG YANMING, FAN SHIYONG, ZHOU XINBO, LI SONG: "Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates", DRUG DELIVERY, ACADEMIC PRESS, ORLANDO, FL., US, vol. 28, no. 1, 1 January 2021 (2021-01-01), US , pages 2603 - 2617, XP093087176, ISSN: 1071-7544, DOI: 10.1080/10717544.2021.2008053
ULAND Y. LAU, LAUREN T. BENOIT, NICOLE S. STEVENS, KIM K. EMMERTON, MARGO ZAVAL, JULIA H. COCHRAN, PETER D. SENTER: "Lactone Stabilization is Not a Necessary Feature for Antibody Conjugates of Camptothecins", MOLECULAR PHARMACEUTICS, AMERICAN CHEMICAL SOCIETY, US, vol. 15, no. 9, 4 September 2018 (2018-09-04), US , pages 4063 - 4072, XP055618626, ISSN: 1543-8384, DOI: 10.1021/acs.molpharmaceut.8b00477
SHINO MANABE: "Development and Current Status of Antibody-drug conjugate (ADC)", DRUG DELIVERY SYSTEM, vol. 34, no. 1, 1 January 2019 (2019-01-01), pages 10 - 21, XP093087000
ANAMI YASUAKI, YAMAZAKI CHISATO M., XIONG WEI, GUI XUN, ZHANG NINGYAN, AN ZHIQIANG, TSUCHIKAMA KYOJI: "Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice", NATURE COMMUNICATIONS, vol. 9, no. 1, 28 June 2018 (2018-06-28), XP093084676, DOI: 10.1038/s41467-018-04982-3
DI, L. ; KERNS, E.H. ; HONG, Y. ; CHEN, H.: "Development and application of high throughput plasma stability assay for drug discovery", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER, NL, vol. 297, no. 1-2, 13 June 2005 (2005-06-13), NL , pages 110 - 119, XP027624001, ISSN: 0378-5173
KYOJI TSUCHIKAMA, ZHIQIANG AN: "Antibody-drug conjugates: recent advances in conjugation and linker chemistries", PROTEIN & CELL, SPRINGER ASIA, BEIJING, CN, vol. 9, no. 1, 1 January 2018 (2018-01-01), Beijing, CN , pages 33 - 46, XP055461467, ISSN: 1674-800X, DOI: 10.1007/s13238-016-0323-0
LIU LIANQI, XIE FEI, XIAO DIAN, XU XIN, SU ZHENG, WANG YANMING, FAN SHIYONG, ZHOU XINBO, LI SONG: "Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates", DRUG DELIVERY, ACADEMIC PRESS, ORLANDO, FL., US, vol. 28, no. 1, 1 January 2021 (2021-01-01), US , pages 2603 - 2617, XP093087176, ISSN: 1071-7544, DOI: 10.1080/10717544.2021.2008053
ULAND Y. LAU, LAUREN T. BENOIT, NICOLE S. STEVENS, KIM K. EMMERTON, MARGO ZAVAL, JULIA H. COCHRAN, PETER D. SENTER: "Lactone Stabilization is Not a Necessary Feature for Antibody Conjugates of Camptothecins", MOLECULAR PHARMACEUTICS, AMERICAN CHEMICAL SOCIETY, US, vol. 15, no. 9, 4 September 2018 (2018-09-04), US , pages 4063 - 4072, XP055618626, ISSN: 1543-8384, DOI: 10.1021/acs.molpharmaceut.8b00477
SHINO MANABE: "Development and Current Status of Antibody-drug conjugate (ADC)", DRUG DELIVERY SYSTEM, vol. 34, no. 1, 1 January 2019 (2019-01-01), pages 10 - 21, XP093087000
ANAMI YASUAKI, YAMAZAKI CHISATO M., XIONG WEI, GUI XUN, ZHANG NINGYAN, AN ZHIQIANG, TSUCHIKAMA KYOJI: "Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice", NATURE COMMUNICATIONS, vol. 9, no. 1, 28 June 2018 (2018-06-28), XP093084676, DOI: 10.1038/s41467-018-04982-3
DI, L. ; KERNS, E.H. ; HONG, Y. ; CHEN, H.: "Development and application of high throughput plasma stability assay for drug discovery", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER, NL, vol. 297, no. 1-2, 13 June 2005 (2005-06-13), NL , pages 110 - 119, XP027624001, ISSN: 0378-5173
Attorney, Agent or Firm:
YAMAO, Norihito et al. (JP)
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