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Title:
CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND MEK INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2021/206167
Kind Code:
A1
Abstract:
Provided is a novel combination therapy that exhibits an excellent antitumor effect and combines an FGFR-inhibiting compound with an MEK inhibitor. An antitumor agent contains (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an effective ingredient and is administered in combination with an MEK inhibitor.

Inventors:
HIRAI HIROSHI (JP)
MATSUOKA KAZUAKI (JP)
MIURA AKIHIRO (JP)
Application Number:
PCT/JP2021/015032
Publication Date:
October 14, 2021
Filing Date:
April 09, 2021
Export Citation:
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Assignee:
TAIHO PHARMACEUTICAL CO LTD (JP)
International Classes:
A61K31/519; A61K31/4184; A61K31/4523; A61K45/00; A61P35/00; A61P43/00; C07D487/04
Domestic Patent References:
WO2015008839A12015-01-22
WO2005121142A12005-12-22
WO2005051906A22005-06-09
WO2007044515A12007-04-19
WO2003077914A12003-09-25
WO2006045514A12006-05-04
WO2002006213A22002-01-24
WO2007014011A22007-02-01
Other References:
KALYUKINA, M. ET AL.: "TAS-120 Cancer Target Binding:Defining Reactivity and I Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure", CHEMMEDCHEM, vol. 14, no. 2019, pages 494 - 500, XP055863996
MERIC-BERNSTAM F., ARKENAU H., TRAN B., BAHLEDA R., KELLEY R., HIERRO C., AHN D., ZHU A., JAVLE M., WINKLER R., HE H., HUANG J., G: "Efficacy of TAS-120, an irreversible fibroblast growth factor receptor (FGFR) inhibitor, in cholangiocarcinoma patients with FGFR pathway alterations who were previously treated with chemotherapy and other FGFR inhibitors", ANNALS OF ONCOLOGY, vol. 29, no. suppl.5, 1 June 2018 (2018-06-01), NL , pages v100, XP055864000, ISSN: 0923-7534, DOI: 10.1093/annonc/mdy149
BOCKORNY, B. ET AL.: "RAS-MAPK Reactivation Facilitates Acquired Resistance 1-29 in FGFR1- Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR-MEK Blockade", MOLECULAR CANCER THERAPEUTICS, vol. 17, no. 7, 2018, pages 1526 - 1539, XP055864003
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Attorney, Agent or Firm:
SAEGUSA & PARTNERS (JP)
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