Coactivator-associated arginine methyltransferase 1 (CARM1) inhibitors: a patenting perspective (2018-present)

CARM1 (Coactivator-associated arginine methyltransferase 1), also known as PRMT4 (Protein Arginine Methyltransferase 4), is a type I PRMT that regulates gene expression by methylating both histone and non-histone substrates. Its overexpression and functional dysregulation have been linked to the progression of several cancer types, including breast, prostate, and hematological malignancies, positioning CARM1 as a compelling target for therapeutic intervention. In this scenario, the development of selective and potent CARM1 inhibitors holds great promise for the treatment of cancer by modulating epigenetic pathways and altering oncogenic transcriptional programs. However, designing effective inhibitors is challenging due to the conserved nature of the PRMT catalytic domain and the need for high selectivity to minimize off-target effects.

This review aims at giving an overview of the recent patent literature of CARM1 inhibitors between 2018 and 2025. WIPO, EPO, USPTO, and SciFinder databases were used for the search of patents.

Although the development of selective CARM1 inhibitors presents significant challenges, it remains a highly promising endeavor due to its potential to greatly advance anticancer drug discovery. Various strategies, including PROTACs can be employed to inactivate the protein, leading to antitumor effects.