Title:
ANTI-TUMOR PHARMACEUTICAL COMPOSITION COMPRISING EZH2 INHIBITOR AND SD1 INHIBITOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/108563
Kind Code:
A1
Abstract:
Provided is a pharmaceutical composition for enhancing the anti-tumor effect of an EZH2 inhibitor. The pharmaceutical composition comprises an EZH2 inhibitor and an SD1 inhibitor, wherein the SD1 inhibitor enhances the effect of the EZH2 inhibitor on a solid tumor. Further provided are a related preparation of the pharmaceutical composition and the use thereof in the preparation of an anti-tumor drug. Experimental results show that when the EZH2 inhibitor GSK126 and the SD1 inhibitor MF-438 are used in combination for treating B16F10 and SMMC7721 cells, it is found that the combination with MF-438 can indeed significantly enhance the inhibitory effect of GSK126 on cell proliferation. The pharmaceutical composition provides a new idea for clinically safely, effectively, conveniently and economically using the EZH2 inhibitor for treating a solid tumor, and has good clinical application prospects.
Inventors:
XUE LIXIANG (CN)
GUO ZHENGYANG (CN)
ZHANG TENGRUI (CN)
WANG YAN (CN)
SUN YAN (CN)
GONG YUEQING (CN)
GUO ZHENGYANG (CN)
ZHANG TENGRUI (CN)
WANG YAN (CN)
SUN YAN (CN)
GONG YUEQING (CN)
Application Number:
PCT/CN2021/138893
Publication Date:
June 22, 2023
Filing Date:
December 16, 2021
Export Citation:
Assignee:
UNIV PEKING THIRD HOSPITAL (CN)
International Classes:
A61K45/06; A61K31/501; A61P35/00; A61K31/496
Foreign References:
| US20210137934A1 | 2021-05-13 | |||
| CN108136011A | 2018-06-08 | |||
| CN105541801A | 2016-05-04 |
Other References:
ZHU, YONGXIA ET AL.: "Research Progress of Methyltransferase EZH2 in The Pathogenesis and Treatment of Malignant Tumors", JOURNAL OF CANCER CONTROL AND TREATMENT, vol. 34, no. 10, 31 October 2021 (2021-10-31), XP009547117
PISANU MARIA ELENA; NOTO ALESSIA; DE VITIS CLAUDIA; MORRONE STEFANIA; SCOGNAMIGLIO GIOSUè; BOTTI GERARDO; VENUTA FEDERICO; DI: "Blockade of Stearoyl-CoA-desaturase 1 activity reverts resistance to cisplatin in lung cancer stem cells", CANCER LETTERS, NEW YORK, NY, US, vol. 406, 7 August 2017 (2017-08-07), US , pages 93 - 104, XP085165366, ISSN: 0304-3835, DOI: 10.1016/j.canlet.2017.07.027
DAI, SHUANG ET AL.: "Progression of SCD1 Inhibitor as an Antitumor Reagent for Human Cancers", CHINA JOURNAL OF MODERN MEDICINE, vol. 28, no. 16, 30 June 2018 (2018-06-30), XP093072895
LEGER, S. ; BLACK, W.C. ; DESCHENES, D. ; DOLMAN, S. ; FALGUEYRET, J.P. ; GAGNON, M. ; GUIRAL, S. ; HUANG, Z. ; GUAY, J. ; LEBLANC: "Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438)", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 20, no. 2, 15 January 2010 (2010-01-15), Amsterdam NL , pages 499 - 502, XP026812518, ISSN: 0960-894X
PISANU MARIA ELENA; NOTO ALESSIA; DE VITIS CLAUDIA; MORRONE STEFANIA; SCOGNAMIGLIO GIOSUè; BOTTI GERARDO; VENUTA FEDERICO; DI: "Blockade of Stearoyl-CoA-desaturase 1 activity reverts resistance to cisplatin in lung cancer stem cells", CANCER LETTERS, NEW YORK, NY, US, vol. 406, 7 August 2017 (2017-08-07), US , pages 93 - 104, XP085165366, ISSN: 0304-3835, DOI: 10.1016/j.canlet.2017.07.027
DAI, SHUANG ET AL.: "Progression of SCD1 Inhibitor as an Antitumor Reagent for Human Cancers", CHINA JOURNAL OF MODERN MEDICINE, vol. 28, no. 16, 30 June 2018 (2018-06-30), XP093072895
LEGER, S. ; BLACK, W.C. ; DESCHENES, D. ; DOLMAN, S. ; FALGUEYRET, J.P. ; GAGNON, M. ; GUIRAL, S. ; HUANG, Z. ; GUAY, J. ; LEBLANC: "Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438)", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 20, no. 2, 15 January 2010 (2010-01-15), Amsterdam NL , pages 499 - 502, XP026812518, ISSN: 0960-894X
Attorney, Agent or Firm:
BEIJING CEMO LEADER INTELLECTUAL PROPERTY AGENCY (CN)
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