Title:
CONJUGATE IN WHICH FL118 DRUG IS LINKED TO ACID-SENSITIVE LINKER, AND IMMUNOCONJUGATE USING SAME
Document Type and Number:
WIPO Patent Application WO/2022/015110
Kind Code:
A1
Abstract:
The present invention relates to a conjugate in which an FL118 drug is linked to an acid-sensitive linker, and an immunoconjugate using same. In the present invention, one or more FL118 drugs of chemical formula 1 are linked to an antibody or an antigen-binding site-containing fragment thereof through an acid-sensitive linker, and after being targeted to cancer cells by an antigen-binding site that targets an antigen of the cancer cells, the acid-sensitive linker is decomposed in an acidic environment around cancer (pH ≤ 7) so that at least a part of the FL118 drug of chemical formula 1 is liberated, the free FL118 drug of chemical formula 1 penetrates the cell membrane and migrates into cells, and the FL118 drug of chemical formula 1 inhibits the action of an efflux pump, and thus the free FL118 drug of chemical formula 1 is concentrated in the cells.
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Inventors:
JUNG DOO YOUNG (KR)
LEE JIN SOO (KR)
CHO HYUN YONG (KR)
CHOI SHIN HEI (KR)
LEE BYEONG SUNG (KR)
LEE JIN SOO (KR)
CHO HYUN YONG (KR)
CHOI SHIN HEI (KR)
LEE BYEONG SUNG (KR)
Application Number:
PCT/KR2021/009204
Publication Date:
January 20, 2022
Filing Date:
July 16, 2021
Export Citation:
Assignee:
PINOTBIO INC (KR)
International Classes:
A61K47/68; A61K47/54; A61P35/00; C07F7/18
Domestic Patent References:
| WO2012058666A2 | 2012-05-03 |
Foreign References:
| US20170360770A1 | 2017-12-21 | |||
| US20180170944A1 | 2018-06-21 |
Other References:
LING XIANG, LIU XIAOJUN, ZHONG KAI, SMITH NICHOLAS, PREY JOSHUA, LI FENGZHI: "FL118, a novel camptothecin analogue, overcomes irinotecan and topotecan resistance in human tumor xenograft models", AM J TRANSL RES, vol. 7, no. 10, 1 January 2015 (2015-01-01), pages 1765 - 1781, XP055887850
ZHANG YIXUAN; YIN RUIJUAN; WU GUANZHAO; YU MINGMING; LIU JIANNAN; WANG XUETING; LIU XUEMENG; GUAN HUASHI; YU RILEI; JIANG TAO: "Self-assembling nanoparticles of dually hydrophobic prodrugs constructed from camptothecin analogue for cancer therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 200, 30 April 2020 (2020-04-30), AMSTERDAM, NL , XP086205559, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2020.112365
CANCER SCI, vol. 107, 2016, pages 1039 - 1046
N ENGL J MED, vol. 382, 2020, pages 610 - 621
ZHANG YIXUAN; YIN RUIJUAN; WU GUANZHAO; YU MINGMING; LIU JIANNAN; WANG XUETING; LIU XUEMENG; GUAN HUASHI; YU RILEI; JIANG TAO: "Self-assembling nanoparticles of dually hydrophobic prodrugs constructed from camptothecin analogue for cancer therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 200, 30 April 2020 (2020-04-30), AMSTERDAM, NL , XP086205559, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2020.112365
CANCER SCI, vol. 107, 2016, pages 1039 - 1046
N ENGL J MED, vol. 382, 2020, pages 610 - 621
Attorney, Agent or Firm:
KIM, Kyeongkyo et al. (KR)
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