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1. (WO2018087401) COMBINATION OF A BRD4 INHIBITOR AND AN ANTIFOLATE FOR THE THERAPY OF CANCER

Pub. No.:    WO/2018/087401    International Application No.:    PCT/EP2017/079225
Publication Date: Fri May 18 01:59:59 CEST 2018 International Filing Date: Wed Nov 15 00:59:59 CET 2017
IPC: A61K 31/5025
A61K 31/519
A61K 31/551
A61K 45/06
G01N 33/00
G01N 33/574
Applicants: CEMM - FORSCHUNGSZENTRUM FÜR MOLEKULARE MEDIZIN GMBH
Inventors: SDELCI, Sara
KUBICEK, Stefan
Title: COMBINATION OF A BRD4 INHIBITOR AND AN ANTIFOLATE FOR THE THERAPY OF CANCER
Abstract:
The present invention relates to the combination of a BRD4 inhibitor with an antifolate (particularly an MTHFD1 inhibitor) for use in the treatment or prevention of cancer. The invention also relates to an antifolate (particularly an MTHFD1 inhibitor) for use in resensitizing a BRD4 inhibitor-resistant cancer to the treatment with a BRD4 inhibitor. The invention further provides a pharmaceutical composition comprising a BRD4 inhibitor, an antifolate (particularly an MTHFD1 inhibitor), and a pharmaceutically acceptable excipient. Moreover, the invention provides a method of assessing the susceptibility or responsiveness of a subject to the treatment with a BRD4 inhibitor, wherein the subject has been diagnosed as suffering from cancer or is suspected of suffering from cancer, the method comprising determining the level of nuclear folate and/or the level of expression of MTHFD1 in a sample obtained from the subject.