WO2024023641 - METHODS OF TRICYCLIC AKR1C3 DEPENDENT KARS INHIBITOR DOSING FIELD OF THE INVENTION

National phase entry:
Publication Number WO/2024/023641
Publication Date 01.02.2024
International Application No. PCT/IB2023/057314
International Filing Date 18.07.2023
Title **
[English] METHODS OF TRICYCLIC AKR1C3 DEPENDENT KARS INHIBITOR DOSING FIELD OF THE INVENTION
[French] MÉTHODES ASSOCIÉES À L'ADMINISTRATION D'UN INHIBITEUR TRICYCLIQUE DE KARS DÉPENDANT DE AKR1C3 DE L'INVENTION
Applicants **
NOVARTIS AG
Inventors
FRYER, Christy
KATTENHORN, Lisa
MCLAUGHLIN, Margaret Elise
STONEHOUSE, Jeffrey
MAACKE, Heiko
L'EPICIER-SANSREGRET, Laurent
Priority Data
63/369,399   26.07.2022   US
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Quotation for National Phase entry

Country StagesTotal
China Filing, Examination, Granting5285
EPO Filing, Examination, Granting102725
Japan Filing, Examination, Granting4870
South Korea Filing, Examination, Granting7758
USA Filing, Examination, Granting28190
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Total: 148,828

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Abstract[English] The present invention relates to methods of identifying a subject for treatment with or treating a subject with a tricyclic AKR1C3 dependent KARS inhibitor of formula (I), or a pharmaceutically acceptable salt thereof. The methods may comprise determining in a subject sample a level of at least one of the following biomarkers: AKR1C3, NFE2L2, KEAP1, or CUL3, wherein an elevated level of the biomarker identifies the subject as being in need of treatment; or detecting in a subject sample a somatic mutation in at least one of the following genes: NFE2L2, KEAP1, or CUL3, wherein detecting the somatic mutation identifies the subject as being in need of treatment.[French] La présente invention concerne des méthodes d'identification d'un sujet à des fins de traitement, ou des méthodes de traitement d'un sujet avec un inhibiteur tricyclique de KARS dépendant de AKR1C3 de formule (I), ou avec un sel de qualité pharmaceutique de celui-ci. Les méthodes peuvent comprendre la détermination, dans un échantillon prélevé chez le sujet, d'un niveau d'au moins l'un des biomarqueurs suivants : AKR1C3, NFE2L2, KEAP1 ou CUL3, un niveau élevé du biomarqueur indiquant que le sujet a besoin d'un traitement ; ou la détection dans un échantillon prélevé chez le sujet d'une mutation somatique touchant au moins l'un des gènes suivants : NFE2L2, KEAP1 ou CUL3, la détection de la mutation somatique indiquant que le sujet a besoin d'un traitement.

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