EZH1/2 dual inhibitor-containing pharmaceutical composition to be used as a combination drug
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Publication Number
US-12390455-B2
Publication Date
2025-08-19
Expiration Date
Abstract
An object of the present invention is to provide a combination drug having an EZH1/2 dual inhibitor in combination with another medical agent and exerting an excellent anticancer effect. Provided is a combination drug having an EZH1/2 dual inhibitor in combination with another medical agent and exerting an excellent anticancer effect.
Core Innovation
The invention relates to a cancer-treatment pharmaceutical composition that combines an EZH1/2 dual inhibitor, valemetostat, represented by formula (I), or a pharmaceutically acceptable salt thereof. In particular embodiments, the pharmaceutically acceptable salt is a p-toluenesulfonate salt designated as Compound A. The document further places this EZH1/2 dual inhibitor in combination with an immune checkpoint inhibitor.
The document discloses treatment of cancer in a patient in need thereof by administering the compound of formula (I) or a pharmaceutically acceptable salt thereof together with an immune checkpoint inhibitor in combination. The combination administration addresses cancer therapy through the use of the formula (I) compound and the immune checkpoint inhibitor.
The document further specifies immune checkpoint inhibitor targets and examples, including anti-PD-1, anti-PD-L1, and anti-CTLA-4, and named antibodies such as nivolumab, pembrolizumab, avelumab, atezolizumab, durvalumab, and ipilimumab. The combination is described in relation to both hematological cancers and solid cancers.
Claims Coverage
The independent claim set covers a cancer-treatment method based on administering a formula (I) EZH1/2 dual inhibitor together with an immune checkpoint inhibitor. Across the dependent claims, the coverage includes timing of administration, a specific pharmaceutically acceptable salt form, and immune checkpoint inhibitor target classes and named agents.
Cancer treatment by combination of formula (I) and an immune checkpoint inhibitor
A method for treating cancer in a patient in need thereof, comprising administering a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and an immune checkpoint inhibitor in combination.
Same time or different times administration relationship
The method specifies administering the compound represented by formula (I) or a pharmaceutically acceptable salt together with the immune checkpoint inhibitor, either at the same time or at different times.
p-Toluenesulfonate salt of the formula (I) compound
The method is carried out using a pharmaceutically acceptable p-toluenesulfonate salt of the formula (I) compound.
Immune checkpoint inhibitor selected from anti-PD-1/PD-L1/CTLA-4 antibodies
The method is carried out using an immune checkpoint inhibitor selected from anti-PD-1, anti-PD-L1, or anti-CTLA-4 antibodies.
Named immune checkpoint inhibitor drugs
The method is carried out using an immune checkpoint inhibitor selected from nivolumab, pembrolizumab, avelumab, atezolizumab, durvalumab, or ipilimumab.
Overall, the claim coverage centers on administering a formula (I) EZH1/2 dual inhibitor or pharmaceutically acceptable salt with an immune checkpoint inhibitor in combination, with dependent features specifying timing, a p-toluenesulfonate salt, and checkpoint targeting classes and named agents.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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